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  • Articles  (1,419)
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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    Journal of mathematical biology 22 (1985), S. 105-115 
    ISSN: 1432-1416
    Keywords: ESS ; evolution ; game dynamics ; population genetics ; sexual populations ; strategies
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Mathematics
    Notes: Abstract As an extension of the concept of an evolutionarily stable strategy (ESS) evolutionarily stable sets are introduced, i.e. sets of equilibrium strategies (EQS) which have much of the properties of an ESS. They are primarily used with evolutionary game models that allow a continuum of EQSs, none of which can be an ESS, but also include common ESSs as a special case. For a large class even of nonlinear models it can be shown that the standard dynamics converge towards some equilibrium point in an ES set if started within a neighbourhood of the set. Important applications of ES sets include e.g. mixed-strategist models and evolutionary game models in sexual populations.
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  • 2
    ISSN: 1432-1424
    Keywords: charybdotoxin ; erythrocytes ; iodination ; kinetics ; peptides ; potassium channels ; scorpions
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Summary Two charybdotoxin peptides were purified from venom of the Israeli scorpion,Leiurus quinquestriatus hebraeus. Microsequencing of the most abundant toxin, ChTX-Lq1, revealed identity with the 37-residue peptide previously sequenced by Gimenez-Gallego et al. [Gimenez-Gallego, G., et al.,Proc. Natl. Acad. Sci. USA 85:3329–3333 (1988)]. Sequence data on the minor peptide, ChTX-Lq2, showed substantial homology to ChTX-Lq1 with differences observed at eight positions. These two charybdotoxin sequences, along with that of noxiustoxin, define a distinct family of scorpion peptide toxins with activity against K+ channels. Both charybdotoxin homologs inhibited Ca2+-dependent K+ efflux from human erythrocytes with similar potency,K 0.5∼-40nm. In planar bilayer assays of single K(Ca) channels from rat muscle, ChTX-Lq1 and ChTX-Lq2 blocked with intrinsicK d's of 1.3 and 43nm, respectively, in the presence of 50mm external KCl. A new application of dwell-time histogram analysis of single-channel blocking events was used to characterize the kinetic homogeneity of toxin samples and the blocking kinetics of ChTX derivatives. The lower blocking affinity of ChTX-Lq2 was the combined result of a faster dissociation rate and a slower association rate as compared to ChTX-Lq1. The blocking activity of two mono-iodinated derivatives of ChTX-Lq1 was also analyzed. Blocked dwell-time histograms of the iodinated peptides were characterized by predominately brief (0.2–2 sec) blocking events in comparison to the native toxin (20 sec). Histogram analysis revealed that mono-iodination of ChTX-Lq1 impairs blocking activity by adverse effects on both dissociation and association rate constants. Frequency density histograms of single channel blocking events provide a sensitive assay of toxin purity suitable for quantitating structure-activity relationships of charybdotoxin derivatives.
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  • 3
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    The journal of membrane biology 76 (1983), S. 289-297 
    ISSN: 1432-1424
    Keywords: neuron ; internal perfusion ; Mn current ; kinetics ; Ca blocker
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Summary Characteristics of currents carried by Mn2+ and other divalent cations were studied in the isolated identified neuron in the circumesophageal ganglia ofHelix aspersa using a suction pipette technique which allows internal perfusion of the cell body and voltage clamp. Increases in [Mn2+] 0 induced not only saturation of the peak ofI Mn but also shifts theI–V relationships along the voltage axis to the more positive potentials. Internal perfusion with F−, which blocks Ca channels, depressedI Mn. Diltiazem, an organic Ca blocker, inhibitedI Mn over the entire range of theI–V relation without shifting the threshold and peak voltage of theI–V relation. Co2+, Ni2+, Cd2+ and La3+ also suppressedI Mn. Relative maximum peak currents of the divalent cations wereI Ba=I Sr〉I Ca〉I Mn=I Zn. Time constants for activation (τ m ) and inactivation (τ h ) of these cations were voltage dependent, and both time constants were greater in the sequence ofI Mn=I Zn〉I Ba=I Sr〉I Ca over the whole voltage range.
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  • 4
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    The journal of membrane biology 132 (1993), S. 167-178 
    ISSN: 1432-1424
    Keywords: red cell ; glucose transport protein ; GLUT1 ; kinetics ; rapid reactions ; tryptophan
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Summary The kinetics of the initial phases of d-glucose binding to the glucose transport protein (GLUT1) of the human red cell can be followed by stopped-flow measurements of the time course of tryptophan (trp) fluorescence enhancement. A number of control experiments have shown that the trp fluorescence kinetics are the result of conformational changes in GLUT1. One shows that nontransportable l-glucose has no kinetic response, in contrast to d-glucose kinetics. Other controls show that d-glucose binding is inhibited by cytochalasin B and by extracellular d-maltose. A typical time course for a transportable sugar, such as d-glucose, consists of a zero-time displacement, too fast for us to measure, followed by three rapid reactions whose exponential time courses have rate constants of0.5–100 sec+−1 at 20°C. It is suggested that the zero-time displacement represents the initial bimolecular ligand/GLUT1 association. Exponential 1 appears to be located at, or near, the external membrane face where it is involved in discriminating among the sugars. Exponential 3 is apparently controlled by events at the cytosolic face. Trp kinetics distinguish the K d of the epimer, d-galactose, from the K dfor d-glucose, with results in agreement with determinations by other methods. Trp kinetics distinguish between the binding of the α- and β-d-glucose anomers. The exponential 1 activation energy of the β-anomer, 13.6 ± 1.4 kcal mol+−1, is less than that of α-d-glucose, 18.4 ± 0.8 kcal mol+−1, and the two Arrhenius lines cross at ≈23.5°C. The temperature dependence of the kinetic response following α-d-glucose binding illustrates the interplay among the exponentials and the increasing dominance of exponential 2 as the temperature increases from 22.3 to 36.6°C. The existence of these interrelations means that previously acceptable approximations in simplified reaction schemes for sugar transport will now have to be justified on a point-to-point basis.
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  • 5
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    The journal of membrane biology 102 (1988), S. 225-234 
    ISSN: 1432-1424
    Keywords: erythrocytes ; valinomycin ; protonophore ; CCCP ; permeability ; kinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Summary A transport model for translocation of the protonophore CCCP across the red cell membrane has been established and cellular CCCP binding parameters have been determined. The time course of the CCCP redistribution across the red cell membrane, following a jump in membrane potential induced by valinomycin addition, has been characterized by fitting values of preequilibrium extracellular pHvs. time to the transport model. It is demonstrated, that even in the presence of valinomycin, the CCCP-anion is “well behaved,” in that the translocation can be described by simple electrodiffusion. The translocation kinetics conform to an Eyring transport model, with a single activation energy barrier, contrary to translocation across lipid bilayers, that is reported to follow a transport model with a plateau in the activation energy barrier. The CCCP anion permeability across the red cell membrane has been calculated to be close to 2.0×10−4 cm/sec at 37°C with small variations between donors. Thus the permeability of CCCP in the human red cell membrane deviates from that found in black lipid membranes, in which the permeability is found to be a factor of 10 higher.
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  • 6
    ISSN: 1432-1424
    Keywords: ion transport ; carriers ; lipid bilayers ; kinetics ; nonactin ; methylation ; macrotetralides
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Summary The effects of methylation on the rate constants of carrier-mediated ion transport have been studied on monooleindecane bilayers with K+, Rb+, NH 4 + , and TI+ ions, using the series of homologue carriers, nonactin, monactin, dinactin, trinactin, and tetranactin, each member of the series differing from the previous one by only one methyl group. Measurements of the amplitude and time constant of the current relaxation after a voltage jump over a large domain of voltage and permeant ion concentration, together with a computer curve-fitting procedure, have allowed us, without the help of steady-state current-voltage data, to deduce and compare the values of the various rate constants for ion transport: formation (k Ri) and dissociation (k Di) of the ion-carrier complex at the interface, translocation across the membrane interior of the carrier (k s) and the complex (k is). With the additional information from steady-state low-voltage conductance measurements, we have obtained the value of the aqueous phase-membrane and torus-membrane partition coefficient of the carrier ({ie191-1} and {ie191-2}). From nonactin to tetranactin with the NH 4 + ion,k is, and {ie191-3} are found to increase by factors of 5 and 3, respectively,k Di and {ie191-4} to decrease respectively by factors 8 and 2, whilek Ri andk s are practically invariant. Nearly identical results are found for K+, Rb+, and Tl+ ions.k Ri,k s andk is are quite invariant from one ion to the other except for Tl+ wherek Ri is about five times larger. On the other hand,k Di depends strongly on the ion, indicating that dissociation is the determining step of the ionic selectivity of a given carrier. The systematic variations in the values of the rate constants with increasing methylation are interpreted in terms of modifications of energy barriers induced by the carrier increasing size. Within this framework, we have been able to establish and verify a fundamental relationship between the variations ofk is andk Di with methylation.
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  • 7
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    The journal of membrane biology 69 (1982), S. 35-40 
    ISSN: 1432-1424
    Keywords: axon ; hydrostatic pressure ; K currents ; kinetics ; activation volume
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Summary The effect of pressure upon the delayed, K, voltage-clamp currents of giant axons from the squidLoligo vulgaris was studied in axons treated with 300nm TTX to block the early, Na, currents. The effect of TTX remained unaltered by pressure. The major change produced by pressures up to 62 MPa is a slowing down of the rising phase of the K currents by a time scaling factor which depends on pressure according to an apparent activation volume, ΔV∓, of 31 cm3/mole at 15°C; ΔV∓ increased to about 42 cm3/mole at 5°C. Pressure slightly increased the magnitude, but did not produce any obvious major change in the voltage dependence, of the steady-state K conductance estimated from the current jump at the end of step depolarizations of small amplitude (to membrane potentials,E, ≦20 mV) and relatively short duration. At higher depolarizations, pressure produced a more substantial increase of the late membrane conductance, associated with an apparent enhancement of a slow component of the K conductance which could not be described within the framework of the Hodgkin-Huxley (HH)n 4 kinetic scheme. The apparent ΔV∓ values that characterize the pressure dependence of the early component of the K conductance are very close to those that describe the effect of pressure on Na activation kinetics, and it is conceivable that they are related to activation volumes involved in the isomerization of the normal K channels. The enhancement of the slow component of membrane conductance by pressure implies either a large increase in the conductance of the ionic channels that are responsible for it or a strong relative hastening of their turn-on kinetics.
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  • 8
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    The journal of membrane biology 74 (1983), S. 85-94 
    ISSN: 1432-1424
    Keywords: sodium ; lithium ; chloride ; pH ; transport ; kinetics ; ion permeability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Summary Na+, Li+, K+, Rb+, Br−, Cl− and SO 4 2− transport were studied in brush border membrane vesicles isolated from rabbit jejunum., Li+ uptakes were measured by flameless atomic absorption spectroscopy, and all others were measured using isotopic flux and liquid scintillation counting. All uptakes were performed with a rapid filtration procedure. A method is presented for separating various components of ion uptake: 1) passive diffusion, 2) mediated transport and 3) binding. It was concluded that a Na+/H+ exchange mechanism exists in the jejunal brush border. The exchanger was inhibited with 300 μm amiloride or harmaline. The kinetic parameters for sodium transport by this mechanism depend on the pH of the intravesicular solution. The application of a pH gradient (pHin=5.5, pHout=7.5) causes an increase inJ max (50 to 125 pmol/mg protein·sec) with no change inK t (≈4.5mm). Competition experiments show that other monovalent cations, e.g. Li+ and NH 4 + , share the Na+/H+ exchanger. This was confirmed with direct measurements of Li+ uptakes. Saturable uptake mechanisms were also observed for K+, Rb+ and SO 4 2− , but not for Br−. TheJ max for K+ and Rb+ are similar to theJ max for Na+, suggesting that they may share a transporter. The SO 4 2− system appears to be a Na+/SO 4 2− cotransport system. There does not appear to be either a Cl−/OH− transport mechanism of the type observed in ileum or a specific Na+/Cl− symporter.
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  • 9
    ISSN: 1432-1424
    Keywords: sodium ; pyruvate ; transport ; proximal tubule ; kinetics ; kidney
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Summary The experiments reported in this paper aim at characterizing the carboxylic acid transport, the interactions of pyruvate and citrate with their transport sites and specificity. The study of these carriers was performed using isotopic solutes for the influx measurements in brush-border membrane vesicles under zerotrans conditions where the membrane potential was abolished with KCl preloading with valinomycin or equilibrium exchange conditions and Δψ=0. Under zerotrans condition and Δψ=0, the influence of pyruvate concentrations on its initial rates of transport revealed the existence of two families of pyruvate transport sites, one with a high affinity for pyruvate (K t =88 μm) and a low affinity for sodium (K t =57.7mm) (site I), the second one with a low affinity for pyruvate (K t =6.1mm) and a high affinity for sodium (K t =23.9mm) (site II). The coupling factor [Na]/[pyruvate] stoichiometry were determined at 0.25mm and 8mm pyruvate and estimated at 1.8 for site I, and 3 when the first and the second sites transport simultaneously. Under chemical equilibrium (Δψ≅0) single isotopic labeling, transport kinetics of pyruvate carrier systems have shown a double interaction of pyruvate with the transporter; the sodium/pyruvate stoichiometry also expressed according to a Hill plot representation wasn=1.7. The direct method of measuring Na+/pyruvate stoichiometry from double labeling kinetics and isotopic exchange, for a time course, gives an=1.67. Studies of transport specificity, indicate that the absence of inhibition of lactate transport by citrate and the existence of competitive inhibition of lactate and citrate transports by pyruvate leads to the conclusion that the low pyruvate affinity site can be attributed to the citrate carrier (tricarboxylate) and the high pyruvate affinity site to the lactate carrier (monocarboxylate).
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  • 10
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    The journal of membrane biology 108 (1989), S. 253-261 
    ISSN: 1432-1424
    Keywords: Chara ; Cl− ; cotransport ; reaction kinetic model ; pH ; kinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Summary H+-coupled transport in plant and fungal cells is relatively insensitive to external pH (pH o ). H+-coupled Cl− transport at the plasma membrane ofChara corallina was studied to explore the phenomena responsible for this insensitivity. Raising pH o from a control value of 7.5 to 9.0 results in a modest (2.5-fold) decline inJ max and increase inK m . Further increase in pH o results in a selective increase inJ max, in accordance with predictions from a reaction kinetic model of the transport system (Sanders, D., Hansen, U.-P., 1981.J. Membrane Biol. 58:139–153). Increase in cytosolic Cl− concentration ([Cl−] c ) also results in a selective decrease inJ max at pH o =7.5. Quantitative kinetic modeling of the results is not possible if it is assumed that the sole effect of pH o isvia mass action on the binding of external H+ to a transport site. If, instead, the dependence of cytosolic pH (pH c ) on pH o (Smith, F.A., 1984,J. Exp. Bot. 35:1525–1536) is taken into account along with the dependence of Cl− influx on pH c (Sanders, D., 1980,J. Membrane Biol. 53:129–141), then the observed modest changes in Michaelis parameters can be accommodated by a reaction kinetic model. The quantitative parameters of the model yield respective pK a s of the internal and external H+-binding sites=7.85 and 7.2, respective dissociation constants of the internal and external Cl−-binding sites=160 and 40 μm, and an additional, kinetically transparent, H+-binding site with a pK a 〉8.0. The quantitative model independently predicts the response ofJ max andK m to acidic conditions. The results are discussed in terms of the general physiological requirement that fluxes through H+-coupled transport systems are relatively insensitive to environmental variation in pH o . It is proposed that (i) the weak (but finite) dependence of pH c on pH o , coupled with (ii) the strong dependence of H+-coupled transport on pH c are instrumental in endowing H+-coupled transport systems with a relative insensitivity to variation in pH o . This hypothesis might also explain why pH c in plants and fungi is not acutely controlled with respect to variation of pH o .
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  • 11
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    The journal of membrane biology 110 (1989), S. 57-65 
    ISSN: 1432-1424
    Keywords: fluorescence ; water transport ; vasopressin ; kidney collecting tubule ; kinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Summary Water transport across the mammalian collecting tubule is regulated by vasopressin-dependent water channel insertion into and retrieval from the cell apical membrane. The time course of osmotic water permeability (P f ) following addition and removal of vasopressin (VP) and 8-Br-cAMP was measured continuously by quantitative fluorescence microscopy using an impermeant fluorophore perfused in the lumen. Cortical collecting tubules were subjected to a 120 mOsm bath-to-lumen osmotic gradient at 37°C with 10–15 nl/min lumen perfusion and 10–20 ml/min bath exchange rate. With addition of VP (250 μU/ml), there was a 23±3 sec (sem,n=16) lag in whichP f did not change, followed by a rise inP f (initial rate 1.4±0.2×10−4 cm/sec2) to a maximum of 265±10×10−4 cm/sec. With addition of 8-Br-cAMP (0.01–1mm) there was an 11±2 sec lag. For [8-Br-cAMP]=0.01, 0.1 and 1mm, the initial rate ofP f increase following the lag was (units 10−4 cm/sec2): 1.1±0.1, 1.2±0.1 and 1.7±0.3. MaximumP f was (units 10−4 cm/sec): 64±4, 199±9 and 285±11. With removal of VP,P f decreased to baseline (12×10−4 cm/sec) with aT 1/2 of 18 min; removal of 0.1 and 1mm 8-Br-cAMP gaveT 1/2 of 4 and 8.5 min. These results demonstrate (i) a brief lag in theP f response, longer for stimulation by VP than by 8-Br-cAMP, representing the transient build-up of biochemical intermediates proximal to the water channel insertion step, (ii) similar initialdP f /dt (water channel insertion) over a wide range of [8-Br-cAMP] and steady-stateP f values, and (iii) more rapidP f decrease with removal of 8-Br-cAMP than with VP. These pre-steady-state results define the detailed kinetics of the turn-on and turn-off of tubuleP f and provide kinetic evidence that the rate-limiting step for turn-on ofP f is not the step at which VP regulates steady-stateP f . If water channel insertion is assumed to be the rate-limiting step in the turn-on ofP f , these results raise the possibility that water channels must be activated following insertion into the apical membrane.
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  • 12
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    The journal of membrane biology 122 (1991), S. 251-258 
    ISSN: 1432-1424
    Keywords: patch-clamp ; plant vacuole ; single-channel inhibition ; kinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Summary Regulation of ion-channel activity must take place in order to regulate ion transport. In case of tonoplast ion channels, this is possible on both the cytoplasmic and the vacuolar side. Isolated vacuoles of youngVigna unguiculata seedlings show no or hardly any channel activity at tonoplast potentials 〉80 mV, in the vacuole-attached configuration. When the configuration is changed to an excised patch or whole vacuole, a fast (excised patch) or slow (whole vacuole) increase of inward rectifying channel activity is seen. This increase is accompanied by a shift in the voltage-dependent gating to less hyperpolarized potentials. In the whole vacuole configuration the level of inward current increases and also the activation kinetics changes. Induction of channel activity takes up to 20 min depending on the age of the plants used and the diameter of the vacuole. On the basis of the estimated diffusion velocities, it is hypothesized that a compound with a mol wt of 20,000 to 200,000 is present in vacuoles of young seedlings, which shifts the population of channels to a less voltage-sensitive state.
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  • 13
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    The journal of membrane biology 118 (1990), S. 233-242 
    ISSN: 1432-1424
    Keywords: Na channels ; skeletal muscle ; kinetics ; chloramine-T ; electrophysiology ; current inactivation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Summary Delays in the development of activation of Na currents were studied using voltage-clamped frog skeletal muscle fibers. Na currents elicited by a depolarizing voltage step from a hyperpolarized membrane potential were delayed in their activation when compared to Na currents elicited from the resting potential. The magnitude of the delay increased with larger hyperpolarizing potentials and decreased with larger depolarizing test potentials. Delays in activation observed following chloramine-T treatment that partially removes inactivation did not differ from delays observed before treatment. Longer exposures of the muscle fiber to chloramine-T led to a complete loss of inactivation, coincident with an elimination of the hyperpolarization-induced delays in activation. Steady-state slow inactivation was virtually unaffected by prolonged exposures of the fibers to chloramine-T that eliminated fast inactivation. The results show that chloramine-T acts at a number of sites to alter both activation and inactivation. Markov model simulations of the results show that chloramine-T alters fundamental time constants of the system by altering both activation and inactivation rate constants.
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  • 14
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    The journal of membrane biology 79 (1984), S. 41-51 
    ISSN: 1432-1424
    Keywords: glucose ; brush borders ; sodium cotransport ; kinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Summary Brush border membrane vesicles (BBMV) purified from steer jejunum were used to study the kinetics of sodiumd-glucose cotransport under voltage clamped, zero-trans conditions. When the initial rate of glucose transport (J gluc) was measured over a wide range of glucose concentrations ([S]=0.01–20mm), curvature of the Woolf-Augustinsson-Hofstee plots was seen, compatible with a diffusional and one major, high capacity (maximal transport rateJ max=5.8–8.8 nmol/mg·min) saturable system. Further studies indicated that changes incis [Na] altered theK t , but not theJ max, suggesting the presence of a rapid-equilibrium, ordered bireactant system with sodium adding first.Trans sodium inhibitedJ gluc hyperbolically. KCl-valinomycin diffusion potentials, inner membrane face positive, loweredJ gluc, while potentials of the opposite polarity raiseJ gluc. At low glucose concentrations ([S]〈0.05mm), a second, minor, high affinity transport system was indicated. Further evidence for this second saturable system was provided by sodium activation curves, which were hyperbolic when [S]=0.5mm, but were sigmoidal when [S]=.0.01mm. Simultaneous fluxes of22Na and [3H]glucose at 1mm glucose and 30mm NaCl yielded a cotransport-dependent flux ratio of 2∶1 sodium/glucose, suggestive of 1∶1 (Na/glucose) high capacity, low affinity system and a ∼3∶1 (Na/glucose) high affinity, low capacity system. Kinetic experiments with rabbit jejunal brush borders revealed two major Na-dependent saturable systems. Extravesicular (cis) Na changed theK t , but not theJ max of the major system.
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  • 15
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    The journal of membrane biology 69 (1982), S. 23-34 
    ISSN: 1432-1424
    Keywords: axon ; hydrostatic pressure ; Na currents ; kinetics ; temperature ; activation volume
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Summary The effects of hydrostatic pressures up to 62 MPa upon the voltage-clamp currents of intact squid giant axons were measured using mineral oil as the pressure transmitting medium. The membrane resistance and capacitance were not appreciably affected over the whole range of pressures explored. The predominant effect of pressure is to slow the overall kinetics of the voltage-clamp currents. Both the early (Na) currents and the delayed (K) ones were slowed down by approximately the same time scale factor, which was in the range of 2 to 3 when pressure was increased from atmospheric to 62 MPa. Finer details of the effects, most evident at moderate depolarizations, are: the apparent initial delay in the turn-on of Na currents is increased by pressureless than is the phase of steepest time variation, and the later decay is slowedmore than is the rising phase. The initial time course of the currents at high pressures can be made to overlap with that at normal pressure by a constant time compression factor, Θm, together with a small, voltage-dependent delay. In a given axon, Θm was fairly independent of voltage, and it increased exponentially with pressure according to an apparent activation volume, ΔV∓, ranging between 32 and 40 cm3/mole. ΔV∓ tended to decrease with increasing temperature. Contrary to what is observed for moderate or large depolarizations, the kinetics of Na inactivation produced by conditioning prepulses of −50 or −60 mV was little affected over the whole range of pressures explored. Inferences about the pressure dependence of the steady-state Na activation were made from the comparison of the plots of early peak currents,I p, versus membrane potential,E. The Na reversal potential,E Na, and the slope of the plots nearE Na did not change significantly with pressure, but the peak Na conductancevs. E relationship was shifted by about +9 mV upon increasing pressure to 62 MPa. Steady-state Na inactivation,h ∞, was slightly affected by pressure. At 62 MPa the midpoint potential of theh ∞ (E) curve,E h, was shifted negatively by about 4 mV, while the slope atE h decreased by about 38%. Under the tentative assumption that pressure directly affects the gating of Na channels, the Na activation data follows a simple Hodgkin-Huxley scheme if the opening of anm gate involves an activation volume of about 58 Å3 and a net volume increase of about 26 Å3. However, a self-consistent description of the totality of the effects of pressure on Na inactivation cannot be obtained within a similar simple context.
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  • 16
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    The journal of membrane biology 133 (1993), S. 145-160 
    ISSN: 1432-1424
    Keywords: Acetabularia ; K+ channels ; kinetics ; planar lipid bilayers ; voltage dependence
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Summary Plasma membrane from Acetabularia acetabulum was prepared by aqueous-polymer two-phase partitioning and incorporated into planar 1-palmitoyl-2-oleoyl phosphatidylethanolamine bilayers by stirring in the presence of a (cis∶trans) 325∶100 mm KCl gradient. Under these conditions five distinct K+-selective channels were observed which had unitary chord-conductances (determined between 30 mV either side of the reversal potential) and frequencies of incorporation (in parentheses) of 1,600 pS (26%), 485 pS (21%), 259 pS (53%), 140 pS (37%) and 27 pS (37%). Two Cl−-selective channels were also observed, which had unitary chord-conductances of 8 and 48 pS and were present in 21 and 16% of bilayers, respectively. The voltage dependencies of channel open probability (P o ), open-state time constant (τ o) and closed-state time constant (τ c) were determined for the 259, 140 and 27 pS K+ channels. The P o of all three channels increased with increasingly positive membrane potentials. Thus, since these channels were oriented with their extracellular face adjacent to the cis chamber, which was grounded, all would exhibit outward rectification in vivo. Changes in P o were effected by modulation of τ c in all channels, which shortened as membrane potentials became more positive, and also of τ o in the 140 and 27pS channels, which increased as membrane potentials became more positive. Extracellular (cis) KCl concentration (and/or the KCl gradient across the bilayer) affected the P o of all three K+ channels, shifting the P o /membrane potential relationship in the direction of the change in the potassium reversal potential. In all channels this was achieved largely by changes in τ c .
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  • 17
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    The journal of membrane biology 74 (1983), S. 175-182 
    ISSN: 1432-1424
    Keywords: kinetics ; transport inhibition ; noncompetitive ; competitive ; inhibition mechanism ; carrier model
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Summary A new analysis of the conventional carrier model shows that noncompetitive inhibitors can give rise to either competitive, noncompetitive or uncompetitive kinetics; the true mechanism and also the relative affinity of the inhibitor on each surface of the membrane can be decided from the patterns of inhibition observed in different transport experiments. The priciples governing the kinetics of inhibition apply to both reversible and irreversible inhibitors, for in either case the substrate may increase or decrease inhibition or be without effect. Ambiguity arises if the noncompetitive inhibitor acts on only one side of the membrane and if the substrate, in the course of being transported, alters the steady-state distribution of the carrier between inner and outer forms. In facilitated transport systems only equilibrium exchange should give rise to noncompetitive kinetics, whatever the location of the inhibitor. In active systems even the interpretation of exchange in the final steadystate is complicated if the energy-coupling mechanism produces a large displacement in the distribution of the free carrier or the substrate complex: the inhibition could be competitive or uncompetitive, depending on the location of the inhibitor. The actual mechanism is revealed in the uncoupled system.
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    The journal of membrane biology 90 (1986), S. 67-87 
    ISSN: 1432-1424
    Keywords: cotransport ; kinetics ; reaction kinetic model ; dual isotherm ; random binding ; slip
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    Topics: Biology , Chemistry and Pharmacology
    Notes: Summary Solute uptake in many cells is characterized by a series of additive Michaelis-Menten functions. Several explanations for these kinetics have been advanced: unstirred layers, transport across more than one membrane, effects of solute concentration on membrane potential, numerous carrier systems. Although each of these explanations might suffice for individual cases, none provides a comprehensive basis for interpretation of the kinetics. The most common mechanism of solute absorption involves cotransport of solute with a driver ion. A model is developed in which solute and driver ion bind randomly to a membrane-bound carrier which provides a single transmembrane pathway for transport. The kinetic properties of the model are explored with particular reference to its capacity to generate additive Michaelian functions for initial rate measurements of isotopic solute influx. In accord with previous analysis of ordered binding models (Sanders, D., Hansen, U.-P., Gradmann, D., Slayman, C.L. (1984)J. Membrane Biol. 77:123), the conventional assumption that transmembrane transit rate-limits transport has not been applied. Random binding carriers can exhibit single or multiple Michaelian kinetics in response to changing substrate concentration. These kinetics include high affinity/low velocity and low affinity/high velocity phases (so-called “dual isotherms”) which are commonly observed in plant cells. Other combinations of the Michaelis parameters can result incis-(substrate) inhibition. Despite the generality of the random binding scheme and the complexity of the underlying rate equation, a number of predictive and testable features emerge. If external driver ion concentration is saturating, single Michaelian functions always result and increasing internal substrate concentration causes uncompetitive inhibition of transport. Numerical analysis of the model in conditions thought to resemble those in many experiments demonstrates that small relative differences in a few key component rate constants of the carrier reaction cycle are instrumental in generation of dual isotherms. The random binding model makes the important prediction that the contributions of the two isotherms show opposing dependence on external concentration of driver ion as this approaches saturation. In the one case in which this dependence has been examined experimentally, the model provides a good description of the data. Charge translocation characteristics of the carrier can be determined from steady-state kinetic data on the basis of the response of substrate flux to modulation of internal driver ion concentration. The application of the model to dual isotherm kinetics is discussed in relation to “slip” models of cotransport, in which the carrier is assumed to have the capability to transport substrate alone or with the driver ion. A method for distinguishing between the two models is suggested on the basis of measurement of charge/solute transport stoichiometry as a function of external driver ion concentration.
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    Pure and applied geophysics 147 (1996), S. 367-375 
    ISSN: 1420-9136
    Keywords: Induced seismicity ; kinetics ; rock fracture ; rockburst ; earthquake
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    Topics: Geosciences , Physics
    Notes: Abstract Powerful seismic events, such as earthquakes and rockbursts, are caused by the accumulation of energy in rocks and loss of rock mass stability. Usually methods of their forecasting are based on the registration of anomalous behavior of geophysical fields. However an efficiency of this approach is low. The present paper proposes a kinetic approach to the description of rock fracture process, which can be used for the forecasting of seismic events and an investigation of structure and energy distributions in rock. 3-D and 1-D kinetic equations describing a process of cluster formation in rock were obtained. The equations are invariant to deformation conditions and to the scale level of events. They showed a good agreement with the results of field observations and laboratory experiments. It was also shown that these equations well describe the processes of earthquake, rockburst and rock sample failure preparation. Catalogues of rockbursts in mines were analyzed with the use of the kinetic equations to find out evidence of induced seismic events. The proposed approach makes it possible to reveal trends in rock behavior and thus predict the rock failure at different scale levels.
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    Cellular and molecular life sciences 41 (1985), S. 1231-1235 
    ISSN: 1420-9071
    Keywords: Sex ; recombination ; evolution ; parasites ; the Tangled Bank ; the Red Queen ; sex-allocation ; sexual selection ; sex determination
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    Cellular and molecular life sciences 41 (1985), S. 1235-1245 
    ISSN: 1420-9071
    Keywords: Sex ; evolution ; the Tangled Bank ; the Red Queen ; recombination experiments ; genotype × environment interactions
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  • 22
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    Cellular and molecular life sciences 44 (1988), S. 633-637 
    ISSN: 1420-9071
    Keywords: Morphogenesis ; evolution ; development
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    Cellular and molecular life sciences 46 (1990), S. 251-254 
    ISSN: 1420-9071
    Keywords: Bronchial tree ; evolution ; fractal ; lung airway ; morphogenesis ; renormalization group theory
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    Topics: Biology , Medicine
    Notes: Summary The mammalian lung exhibits features of a fractal tree: heterogeneity, self-similarity and the absence of a characteristic scale. The finite nature of the lung ultimately limits the range over which self-similarity scaling characteristics are applicable. However, generalization based on the scaling features of fractals, provides unique insight into geometric organization of anatomic structures. Furthermore, the mathematical theory of renormalization groups provides a description of the harmonically-modulated inverse power-law scaling observed for bronchial tree dimensions observed in different species. Compared to several mammalian species (dog, rat, hamster), the human lung shows marked differences in the phase of the harmonic modulation for both length and diameter measurements. These inter-species scaling differences suggest that evolutionary factors modify certain universal features of morphogenesis.
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    Cellular and molecular life sciences 46 (1990), S. 1106-1117 
    ISSN: 1420-9071
    Keywords: Genetic code ; eucaryotic cell ; evolution ; code ambiguity ; code universality ; convergence
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    Topics: Biology , Medicine
    Notes: Summary This article is a review of the rules used by eucaryotic cells to translate a nuclear messenger RNA into a polypeptide chain. The recent observation that these rules are not identical in two species of a same phylum indicates that they have changed during the course of evolution. Possible scenarios for such changes are presented.
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    Cellular and molecular life sciences 50 (1994), S. 987-1001 
    ISSN: 1420-9071
    Keywords: Hsp70 ; evolution ; gene duplication ; gene homology
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    Notes: Abstract The family of genes encoding heat shock proteins of about 70 kDa (hsp70) in vertebrates is reviewed under genetic aspects. After a detailed description of the various hsp70 genes more general characteristics of the organization and evolution of the multigene family are discussed.
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    Cellular and molecular life sciences 50 (1994), S. 521-523 
    ISSN: 1420-9071
    Keywords: Ancient DNA ; evolution ; conservation ; biology ; anthropology ; plant biology ; PCR (polymerase chain reaction)
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    Cellular and molecular life sciences 51 (1995), S. 454-464 
    ISSN: 1420-9071
    Keywords: Quantitative genetics ; life history ; evolution ; cladocera ; heritability ; Daphnia ; zooplankton
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    Topics: Biology , Medicine
    Notes: Abstract Quantitative genetic techniques are powerful tools for use in understanding the microevolutionary process. Because of their size, lifespan, and ease of culture, many zooplankton species are ideal for quantitative genetic approaches. As model systems, studies of zooplankton life histories are becoming increasingly used for examination of the central paradigms of evolutionary theory. Two of the fundamental empirical questions that zooplankton quantitative genetics studies can answer are: 1) How much genetic variance exists in natural populations for life history traits? 2) What is the empirical evidence for trade-offs that permeate life history theory based on optimality approaches? A review of existing data onDaphnia indicates substantial genetic variance for body size, clutch size, and age at first reproduction. Average broad-sense heritabilities for these three characters across 19 populations of 6 species are 0.31, 0.31, and 0.34, respectively. Although there is some discrepancy between the two pertinent studies that were designed to decompose the total genetic variance into its additive and non-additive components, a crude average seems to suggest that approximately 60% of the total genetic variance has an additive basis. The existing data are somewhat inconsistent with respect to presence/absence of trade-offs (negative genetic correlations) among life history traits. A composite of the existing data seems to argue against the existence of strong trade-offs between offspring size and offspring number, between present and future reproduction, and between developmental rate and fecundity. However, there is some evidence for a shift toward more negative (less positive) covariances in more stressful environments (e.g., low food). Zooplankton will prove to be very useful in future study in several important areas of research, including the genetics and physiology of aging, the importance of genotype-environment interaction for life history traits, and the evolution of phenotypic plasticity.
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  • 28
    ISSN: 1420-9071
    Keywords: Insect ; behaviour ; high-speed cinematography ; jumping ; electrophysiology ; evolution
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    Notes: Abstract The Indian antHarpegnathos saltator may be unique among insects in using its jumping capacity not only as an escape mechanism but also as a normal means of locomotion, and for catching its prey in flight. High-speed cinematography used to analyse the various phases of the jump suggests thatHarpegnathos employs a novel jumping mechanism to mediate these behaviours: namely the synchronous activation of its middle and hindlegs. Electrophysiological recordings from muscles or nerves in pairs of middle and hindlegs show remarkably synchronous activity during fictive jumping, supporting the synchronous activation hypothesis.Harpegnathos is not the only ant to jump, and a cladistic analysis suggests that jumping behaviour evolved independently three times during ant evolutionary history.
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    Cellular and molecular life sciences 41 (1985), S. 24-29 
    ISSN: 1420-9071
    Keywords: Pieridae ; Lepidoptera ; systematics ; evolution ; enzyme electrophoresis ; genetic differentiation
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    Topics: Biology , Medicine
    Notes: Summary Enzyme electrophoretic data show a remarkably high degree of genetic similarity within the European group ofnapi s.l. whereas genetic differences exist at several loci between the European and the North American taxa ofnapi s.l. It is concluded that the European taxa did not differentiate to the species level and form a phylogenetically young group. The North American taxa included in this study are specifically distinct from Europeannapi and separated much earlier. Within these North American taxamarginalis, oleracea andvirginiensis did undergo speciation. The data show a splitting of the genusPieris into three species groups, each genetically differentiated to the same level. The splitting ofPieris into two genera, as suggested by earlier investigators, is not supported here.
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    Cellular and molecular life sciences 41 (1985), S. 1471-1472 
    ISSN: 1420-9071
    Keywords: Phosphoglycerate mutase isozymes ; evolution ; gene duplication
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    Topics: Biology , Medicine
    Notes: Summary The phosphoglycerate mutase isozyme patterns from cyclostomata, cartilaginous and bony fish were analyzed. The observed patterns indicate that a duplication of a single ancestral gene coding for phosphoglycerate mutase took place during the evolution of the gnathostome vertebrates.
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    ISSN: 1420-9071
    Keywords: Spleen ; red pulp ; storage ; release ; morphology ; evolution ; structural characteristics
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    Cellular and molecular life sciences 42 (1986), S. 788-794 
    ISSN: 1420-9071
    Keywords: Electrostatic complementation ; evolution ; genetic code ; hydropathic complementation ; receptor imprinting
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    Cellular and molecular life sciences 42 (1986), S. 624-624 
    ISSN: 1420-9071
    Keywords: Egg pedicel ; evolution ; lacewings ; Hemerobiidae
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    Topics: Biology , Medicine
    Notes: Summary Brown lacewing eggs (Planipennia: Hemerobiidae) glued to the top of hairs of maize leaves can be seen as an intermediary evolutionary step between depositing the egg directly on the substrate (as in most neuropteroid families) and the protective behavioral adaptation of depositing the egg on a long thin pedicel (as e.g. in the Chrysopidae).
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    Cellular and molecular life sciences 47 (1991), S. 1104-1118 
    ISSN: 1420-9071
    Keywords: Transaminase ; decarboxylase ; serine hydroxymethyltransferase ; pyridoxal 5′-phosphate ; enzyme mechanism ; stereochemistry ; kinetics
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    Notes: Abstract Pyridoxal 5′-phosphate is a coenzyme for a number of enzymes which catalyse reactions at Cα of amino acid substrates including transaminases, decarboxylases and serine hydroxymethyltransferase. Using the X-ray coordinates for a transaminase, aspartate aminotransferase, and the results of stereochemical and mechanistic studies for decarboxylases and serine hydroxymethyltransferase, an active-site structure for the decarboxylase group is constructed. The structure of the active-site is further refined through active-site pyridoxyllysine peptide sequence comparison and a 3-D catalytic mechanism for the L-α-amino acid decarboxylases is proposed. The chemistry of serine hydroxymethyltransferase is re-examined in the light of the proposed decarboxylase mechanism.
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    Cellular and molecular life sciences 47 (1991), S. 791-803 
    ISSN: 1420-9071
    Keywords: Phytotoxins ; ecology ; phylogeny ; evolution ; biosynthesis ; coronatine ; phaseolotoxin ; rhizobitoxine ; syringomycin ; syringotoxin ; syringostatin ; tabtoxin ; tagetitoxin ; tropolone ; fireblight toxin ; thaxtomin ; 3-methylthiopropionic acid ; carboxylic acids ; Pseudomonas ; Xanthomonas ; Xanthomonas ; Streptomyces ; Erwinia ; Bradyrhizobium
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    Notes: Abstract This review attempts to rationalise what is known about bacterial phytotoxins and associate it with the ecology and possible evolution of the producing organisms. Study of non-toxin producing variants gives insight into the ecological role of the toxin. Elucidation of chemical structures of phytotoxins has shown that many exist as families of analogous compounds. Studies on the variation of chemical structures and how they are distributed across species and genera can lead to development of hypotheses on evolutionary relationships. Knowledge on biosynthetic pathways to tosins allows recognition of specific enzymatic steps involved in developing the characteristic features of the structures. Phytotoxins often have a potent biochemical activity, and in some cases the producing organism has associated mechanisms to prevent action of the toxin upon itself; in such cases toxigenesis is clearly not a chance event. The various aspects of bacterial toxigenesis indicate that bacterial phytotoxins are special secondary metabolic products that play beneficial roles to the producing organisms in their various ecological niches.
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  • 36
    ISSN: 1420-9071
    Keywords: Biological clock ; cell division cycle ; diaminopimelate ; evolution ; FSu ; lysine ; muramate ; muramyl dipeptide ; peptidoglycan ; sleep muropeptide ; tumor
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    Notes: Abstract Degradation products of peptidoglycan, the universal bacterial cell wall constituent, were previously found in animal tissues and urine. Reassessment and quantitative analysis of available data lead to an original concept, i.e. that eukaryotic cells synthesize peptidoglycan. We present a model in which this endogenously synthesized peptidoglycan is essential for the processes of eukaryotic cell division and sleep induction in animals. Genes for peptidoglycan metabolism, like those for lysine biosynthesis in plants, are probably inherited from endosymbiotic bacteria, the ancestors of mitochondria and chloroplasts. Corollaries of this concept, i.e. roles for peptidoglycan metabolism in tumor formation and in the biological clock, are supported by abundant evidence. We propose that many interactions between bacteria and eukaryotes are conditioned by their common genetic heritage.
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    Cellular and molecular life sciences 49 (1993), S. 1027-1036 
    ISSN: 1420-9071
    Keywords: Archaea (archaebacteria) ; extreme halophiles ; archaeol phospholipids ; archaeol glycolipids ; membrane function ; evolution
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    Notes: Abstract Archaebacteria (archaea) are comprised of three groups of prokaryotes: extreme halophiles, methanogens and thermoacidophiles (extreme thermophiles). Their membrane phospholipids and glycolipids are derived entirely from a saturated, isopranoid glycerol diether,sn-2,3-diphytanylglycerol (‘archaeol’) and/or its dimer, dibiphytanyldiglyceroltetraether (‘caldarchaeol’). In extreme halophiles, the major phospholipid is the archaeol analogue of phosphatidylglycerolmethylphosphate (PGP-Me); the glycolipids are sulfated and/or unsulfated glycosyl archaeols with diverse carbohydrate structure characteristic of taxons on the generic level. Biosynthesis of these archaeol-derived polar lipids occurs in a multienzyme, membrane-bound system that is absolutely dependent on high salt concentration (4 M). The highly complex biosynthetic pathways involve intermediates containing glycerol ether-linked C20-isoprenyl groups which are reduced to phytanyl groups to give the final saturated polar lipids. In methanogens, polar lipids are derived both from archaeol and caldarchaeol, and thermoacidophiles contain essentially only caldarchaeol-derived polar lipids. The function of these membrane polar lipids in maintaining the stability, fluidity and ionic properties of the cell membrane of extreme halophiles, as well as the evolutionary implications of the archaeol and caldarchaeol-derived structures will be discussed.
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    Cellular and molecular life sciences 48 (1992), S. 729-731 
    ISSN: 1420-9071
    Keywords: Urea cycle ; leech ; botryoidal tissue ; hirudineans ; evolution
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    Notes: Abstract Ornithine carbamoyltransferase (OCT) and arginase, but not arginine synthetase (AS), were detected in the body wall and gut tissues of the leech. The activities of these enzymes were not altered by starvation. The high activity of arginase in body wall is probably due to the association of the latter with botryoidal tissue. Hirudineans, which evolved from oligochaete ancestors, appear to have lost the citrulline-arginine segment of the urea cycle due to their ammonotelic mode of nitrogen excretion.
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    Cellular and molecular life sciences 40 (1984), S. 942-944 
    ISSN: 1420-9071
    Keywords: Insect hormones ; estradiol ; estriol ; evolution ; sex hormones
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    Topics: Biology , Medicine
    Notes: Summary Insects representing 5 different orders contain androgen and estrogen-like substances as determined by radioimmunoassay. Estradiol and estriol have been identified by gas chromatography-mass spectrometry. The presence of these steroids in insects suggests that the vertebrate sex hormones have an ancient evolutionary history.
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    Cellular and molecular life sciences 41 (1985), S. 1563-1564 
    ISSN: 1420-9071
    Keywords: Cytosine deaminase ; kinetics ; pyrophosphate ; orotidine monophosphate
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    Notes: Summary The maximal velocity of the reaction (Vmax) and the half-saturation constant (K0.5) values of theS. typhimurium cytosine deaminase were altered in the presence of its effectors, pyrophosphate and orotidine monophosphate. From the kinetics of orotidine monophosphate inhibition of cytosine deaminase, it was characterized as a mixed-type noncompetitive inhibitor.
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    Cellular and molecular life sciences 41 (1985), S. 145-152 
    ISSN: 1420-9071
    Keywords: Spleen ; evolution ; phylogeny ; ontogeny ; non-mammalian spleen ; mammalian spleen ; comparative macromorphology ; comparative micromorphology ; intralienal vessels ; extralienal vessels ; differentiation
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    Cellular and molecular life sciences 43 (1987), S. 1094-1099 
    ISSN: 1420-9071
    Keywords: Cognitive processes ; metabolism ; evolution ; biomathematical models ; cell proliferation ; cell growth
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    Notes: Summary A model for cellular proliferation is described according to which proliferation ensues when metabolism evolves towards commitment to DNA synthesis, and inhibition of proliferation occurs when enzymic interactions are iterated within a few metabolic pathways, another limiting factor being the supply of metabolites. The model successfully describes cellular growth and division as a ‘cognitive process’ based on interaction within enzymic elements and the genome, and affords an explanation in these terms of some empirical phenomena which have previously been understood only as isolated observations.
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    Cellular and molecular life sciences 43 (1987), S. 851-860 
    ISSN: 1420-9071
    Keywords: Social insects ; Isoptera ; caste differentiation ; reproductive biology ; evolution
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    Notes: Summary The hemimetabolous termites have a very different caste system from social Hymenoptera in which only true imagoes participate in all social tasks. In termites, the imagoes are restricted to reproduction. The termite solidiers have no equivalent in other social insects. They are unique both in their post-embryonic development and their exclusively defensive function. At maturity they keep their molting gland and therefore should be considered as stabilized, differentiated immatures. They appeared monophyletically, early in the evolution of termites. The definition of the worker caste and the current theories explaining its evolution are reexamined after a critical reappraisal of data on post-embryonic development. On the basis of ontogenic, morphologic and functional criteria, we define termite workers as individuals diverging early and irreversibly from the imaginal development, with a morphology typical of their caste but largely of larval appearance, and taking part in most of the social tasks. Such a truly eusocial worker caste is observed in all advanced phyla: Termitidae, Hodotermitidae, andSchedorhinotermes (Rhinotermitidae), but apparently also in one morphologically primitive termite,Mastotermes darwiniensis. This distribution can only be explained by postulating a polyphyletic origin of the worker caste in termites. In all other primitive termites, most of the work is done by temporary helpers (late larvae and nymphs). In these societies, pseudergates are redefined as individuals separating late from the imaginal line, functioning as workers, but not constituting the main working force in the natural society. The particularity of the caste system in termites results from two fundamental peculiarities of their post-embryonic development: -A certain dissociation of molt, growth, and differentiation. -A relative independence in the ontogeny of their different organs.
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    Cellular and molecular life sciences 50 (1994), S. 5-14 
    ISSN: 1420-9071
    Keywords: parental investment ; juvenile survival ; evolution ; gastropods ; molluscs ; ovoviviparity ; viviparity
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    Notes: Abstract Parental care in terrestrial gastropods includes the of oviposition sites, production of large, heavily-yolked eggs supplied with calcium carbonate, provisioning of hatchings with eggs in specis with facultative sibling cannibalism, egg retention, and ovoviviparity. Evidence for true viviparity is scarce in terrestrial gastropods, as it is for postlaying care of eggs, though external egg carrying on the shell occurs in a few species. Care of young has not been observed in any terrestrial gastropod species. Provisioning of eggs with nutrients and calcium carbonate might be the most common form of parental investment. Ovoviviparity allows terrestrial gastropods to persist in habitats otherwise unsuitable for oviparous species (e.g. exposed rock walls). An interspecific comparison demonstrates that egg-retaining and ovoviviparous species produce smaller clutches than oviparous species and suggests a cost of parental care.
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    Cellular and molecular life sciences 41 (1985), S. 1285-1296 
    ISSN: 1420-9071
    Keywords: Sex ; sex determination ; sex ratio ; evolution ; animals ; genetics
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    Notes: Summary Theories on the evolution of sex determining mechanisms are reviewed for male and female heterogamety, environmental sex determination, and briefly, haplo-diploidy and hermaphroditism. Because of their discrete and well-defined nature, sex determining mechanisms lend themselves to three types of evolutionary questions:what variety occurs and might be expected but does not occur,how do changes occur from one mechanism to another, andwhy do certain changes occur? All three approaches were illustrated for these different sex determining mechanisms. A generality emerging from these studies is that, at the level of selection on the sex ratio, there are no intrinsic problems in evolving from one sex determining mechanism to another: straightforward transitions between different mechanisms exist under various conditions.
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    Cellular and molecular life sciences 44 (1988), S. 297-303 
    ISSN: 1420-9071
    Keywords: Biology ; creation science ; creationism ; evolution ; hundredth monkey phenomenon ; paranormal ; pseudoscience
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Summary Public suspicion of science stems from science's challenging of perceptions and myths about reality, and a public fear of new technology. The result is a susceptibility to pseudoscience. In claiming that creation ‘science’ is as valid as evolution the creationists misquote scientists and seek to spread their own ‘scientific’ myths concerning a young age for the earth, an act of creation based on a particular literalist interpretation of the Christian Bible and a single worldwide flood. They use methods of debate and politics, rather than scientific research. A selection of their arguments is examined and the nature of the evidence for evolution is discussed. Problems with the creation ‘science’ model are noted. In the myth of the hundredth monkey phenomenon, original research is misquoted to denigrate scientific research and support sentimental ideas of paranormal events. The misuse of science is seen as damaging to society because it reduces the effective gathering and application of scientific information. However, pseudoscience provides a valuable guide to gaps in public scientific education.
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    Cellular and molecular life sciences 44 (1988), S. 735-738 
    ISSN: 1420-9071
    Keywords: Insect ; flight ; evolution
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    Notes: Summary The activity patterns of interneurones in the flight systems of dragonflies and mayflies were investigated using standard intracellular recording and staining techniques, and were compared with those of crickets and locusts. The results show several basic similarities in the operation of a central motor pattern generator for flight in all four groups of insects. These similarities can be explained as resulting from conservative evolution of flight pattern generating circuitry within the central nervous system.
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    Cellular and molecular life sciences 44 (1988), S. 697-700 
    ISSN: 1420-9071
    Keywords: Lizard ; Chamaeleontidae ; Agamidae ; tongue ; feeding ; evolution
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    Notes: Summary An incipient form of tongue projection occurs inPhrynocephalus helioscopus, a generalized agamid lizard. We argue that this condition represents a functional intermediate between typical lingual prehension and chamaeleontid tongue projection, and that tongue projection evolved in chameleons by augmentation of ancestral mechanisms still operating in related, generalized lizards.
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  • 49
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    Cellular and molecular life sciences 45 (1989), S. 248-262 
    ISSN: 1420-9071
    Keywords: Sex pheromone ; biosynthesis ; neurobiology ; sensory biology ; orientation behavior ; flight control ; anemotaxis ; genetics ; communication ; olfaction ; evolution
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    Notes: Summary Significant progress has been made recently in research on lepidopterous sex pheromones. Advances in understanding the biochemical, neurobiological, and behavioral events that results in both successful and unsuccessful pheromone communication have allowed researchers to gain new insights into the genetic control and evolution of phermone systems.
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  • 50
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    Cellular and molecular life sciences 45 (1989), S. 284-295 
    ISSN: 1420-9071
    Keywords: Annual cycle ; Asclepias ; cardenolide ; Danaidae ; Danaus plexippus ; defense ; ecological chemistry ; evolution ; herbivory ; host plant ; life history ; migration ; milkweed ; monarch butterfly ; overwintering ; predation ; repellent allomone ; sequestration ; storage
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    Notes: Summary Monarch butterflies sequester cardenolides from their larval host plants in the milkweed genusAsclepias for use in defense against predation. Of 108Asclepias species in North America, monarchs are known to feed as larvae on 27. Research on 11 of these has shown that monarchs sequester cardenolides most effectively, to an asymptote of approximately 350 μg/0.1 g dry butterfly, from plants with intermediate cardenolide contents rather than from those with very high or very low cardenolide contents. SinceAsclepias host plant species are distributed widely in space and time across the continent, monarchs exploit them by migration between breeding and overwintering areas. After overwintering in central Mexico, spring migrants east of the Rocky Mountains exploit three predominantAsclepias species in the southern USA that have moderately high cardenolide contents. Monarchs sequester cardenolides very effectively from these species. First generation butterflies are thus well protected against predators and continue the migration north. Across the northern USA and southern Canada most summer breeding occurs on a fourthAsclepias species and in autumn most of these monarchs migrate back to Mexican overwintering sites. The ecological implications of this cycle of cardenolide sequestration for the evolution of monarch migration are discussed.
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  • 51
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    Cellular and molecular life sciences 44 (1988), S. 919-930 
    ISSN: 1420-9071
    Keywords: Heart ; circulation ; blood ; lower vertebrate ; embryology ; evolution
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    Topics: Biology , Medicine
    Notes: Summary In very few instances can the cardiovascular systems of adult ‘lower’ vertebrates serve asdirect models for development in ‘higher’ vertebrates, primarily because numerous evolutionary specializations for preferential distribution of cardiac output between systemic tissues and gas exchange, organs occur in the highly derived circulation of most extant lower vertebrates. Yet, the extensive literature on the cardiovascular anatomy and physiology of aquatic and air breathing fishes, amphibians and reptiles offers important conceptual insights into both patterns and mechanisms of development in birds and mammals. The primary contribution of such studies to the student of developing bird and mammal circulations is the clear demonstration that surprisingly complex hemodynamic function can develop from supposedly ‘simple’ cardiovascular systems typified by incompletely divided heart chambers. Thus, the hemodynamics of embryonic bird and mammal circulations should be determined by measurement, rather than inferred from structure.
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  • 52
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    Cellular and molecular life sciences 46 (1990), S. 1117-1126 
    ISSN: 1420-9071
    Keywords: Genetic code ; mitochondria ; evolution ; organelles
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    Notes: Summary The universal genetic code is used without changes in chloroplasts and in mitochondria of green plants. Non-plant mitochondria use codes that include changes from the universal code. Chloroplasts use 31 anticodons in translating the code; a number smaller than that used by bacteria, because chloroplasts have eliminated 10 CNN anticodons that are found in bacteria. Green plant mitochondria (mt) obtain some tRNAs from the cytosol, and genes for some other tRNAs have been acquired from chloroplast DNA. The code in non-plant mt differs from the universal code in the following usages found in various organisms: UGA for Trp, AUA for Met, AGR for Ser and stop, AAA for Asn, CUN for Thr, and possibly UAA for Tyr. CGN codons are not used byTorulopsis yeast mt. Non-plant mt, e.g. in vertebrates, may use a minimum of 22 anticodons for complete translation of mRNA sequences. The following possible causes are regarded as contributing to changes in the non-plant mt: directional mutation pressure, genomic economization, changes in charging specificity of tRNAs, loss of release factor RF2, changes in RF1, changes in anticodons, loss of lysidine-forming enzyme system, and disappearance of codons from coding sequences.
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  • 53
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    Cellular and molecular life sciences 49 (1993), S. 110-117 
    ISSN: 1420-9071
    Keywords: Polymerization ; sickle hemoglobin ; sickle cell disease ; kinetics ; thermodynamics ; polymer domains ; nucleation
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    Notes: Abstract The polymerization of sickle hemoglobin occurs by the same mechanisms in solutions and in cells, and involves the formation of 14 stranded fibers from hemoglobin molecules which have assumed a deoxy quaternary structure. The fibers form via two types of highly concentration-dependent nucleation processes: homogeneous nucleation in solutions with hemoglobin activity above a critical activity, and heterogeneous nucleation in similarly supersaturated solutions which also contain hemoglobin polymers. The latter pathway is dominant, and creates polymer arrays called domains. The individual polymers bend, but also cross-link, and the resulting mass behaves as a solid. The concentration of polymerized hemoglobin increases exponentially unless clamped by rate limiting effects such as oxygen delivery.
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  • 54
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    Keywords: Molluscan insulin-related peptides ; schistosomin ; neuropeptide gene family ; generation of neuropeptide diversity ; stimulus-dependent expression ; information-handling capacity ; evolution
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    Notes: Abstract We review recent experiments showing that the cerebral neuroendocrine Light Green Cells (LGCs) of the freshwater snail,Lymnaea stagnalis, express a family of distinct though related molluscan insulin-related peptide (MIP) genes. The LGCs are involved in the regulation of a wide range of interrelated life processes associated with growth, (energy) metabolism and reproduction. We consider the mechanism of generation of diversity among MIPs, and present evidence that conditions with distinct effects on growth, metabolism and reproduction also can induce distinct patterns of expression of the MIP and schistosomin genes. The stimulus-dependent expression of multiple neuropeptide genes enormously increases the adaptive potential of a peptidergic neuron. We suggest that this contributes significantly to the information-handling capacity of the brain.
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    Cellular and molecular life sciences 49 (1993), S. 317-319 
    ISSN: 1420-9071
    Keywords: Chitin ; cuticle ; evolution ; vertebrates ; bony fish ; Blenniidae ; Paralipophrys trigoides
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    Notes: Abstract Lectin binding, endo-chitinase binding and enzymatic degradation studies show that the epidermal cuticle of the bony fishParalipophrys trigloides (Blenniidae) is chitinous. This is the first evidence that a vertebrate species possesses a chitinous tissue. Recently aXenopus gene has been identified which has significant sequence similarity to the catalytic domain of yeast chitin synthase III, a chitin producing enzyme1,2. Taken together these two findings imply that chitin synthesis capability may be a basic vertebrate feature.
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  • 56
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    Cellular and molecular life sciences 50 (1994), S. 429-437 
    ISSN: 1420-9071
    Keywords: Genetics ; ecology ; DNA-transfer ; conjugation ; transformation ; transduction ; transposons ; dormant cells ; epilithon ; microbial colonisation ; symbiosis ; virus resistance ; biosafety ; release of genes ; insults to humanity ; evolution ; biodiversity
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    Notes: Abstract Genetic ecology is the extension of our modern knowledge in molecular genetics to studies of viability, gene expression and gene movements in natural environments like soils, aquifers and digestive tracts. In such milieux, the horizontal transfer of plasmid-borne genes between phylogenetically distant species has already been found to be much more frequent than had been expected from laboratory experience. For the study of exchanges involving chromosomally-located genes, more has to be learned about the behaviour of transposons in such environments. The results expected from studies in genetic ecology are relevant for considerations of evolution, biodiversity and biosafety. The role of this new field of research in restoring popular confidence in science and in its biotechnological applications is stressed.
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    Cellular and molecular life sciences 52 (1996), S. 14-24 
    ISSN: 1420-9071
    Keywords: Lycaenidae ; Formicidae ; symbiosis ; mutualism ; parasitism ; communication ; ecology ; evolution
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    Notes: Abstract Associations with ants, termed myrmecophily, are widespread in the butterfly family Lycaenidae and range from mere co-existence to more or less specific mutualistic or even parasitic interactions. Secretions of specialized epidermal glands are crucial for mediating the interactions. Transfer of nutrients (carbohydrates, amino acids) from butterfly larvae to ants plays a major role, but manipulative communication with the help of odour signals is also involved. By means of myrmecophily, lycaenid butterflies largely escape ant predation, and certain species gain protection through attendant ants or achieve developmental benefits from ant-attendance. Benefits to the ants range from minimal to substantial food rewards. While most lycaenid species maintain facultative relationships with a variety of ant genera, highly specific and obligatory associations have convergently evolved in a number of butterfly lineages. As a corollary, communication systems are largely unspecific in the former, but may be highly specialized in the latter. The sophisticated communication between obligate myrmecophiles and their host ants is tightly connected with the evolutionary rise of specialized life-cycles and thus is a source of augmenting diversity within the butterflies.
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    Cellular and molecular life sciences 52 (1996), S. 503-510 
    ISSN: 1420-9071
    Keywords: Drosophila ; accessory gland ; reproduction ; sexual behavior ; sperm displacement ; evolution
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    Notes: Abstract Recent results from biochemical and molecular genetic studies of the accessory gland proteins in maleDrosophila are reviewed. The most prominent feature is the species-specific variability. However, the analysis of the sex peptide inD. melanogaster shows that there is a strong homology in the molecular structure to the closely related sibling species, and that divergence increases with increasing phylogenetic distance. For this reason the sex peptide, after being transferred to the female genital tract during copulation, reduces receptivity and increases oviposition only in virgin females belonging to the same species group and subgroup. Even though studies were hitherto limited to a small number of the secretory components, it is evident that the accessory gland proteins play a key role in reproductive success of the fruit fly by changing female sexual behavior, supporting sperm transfer, storage and displacement. Thus, genes encoding the accessory gland proteins are apparently under strong evolutionary selection.
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    Insectes sociaux 40 (1993), S. 325-335 
    ISSN: 1420-9098
    Keywords: Formicidae ; social parasitism ; PCR ; 18 S ribosomal RNA ; evolution
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    Topics: Biology
    Notes: Summary The evolutionary relationship between socially parasitic ants and their hosts is still an unsolved problem. We have compared a 1.2 kb sequence of the 18 S ribosomal RNA genes of the parasitic antsDoronomyrmex kutteri, Harpagoxenus sublaevis andChalepoxenus muellerianus to the sequence of the host speciesLeptothorax acervorum andL. recedens (all subfamily Myrmicinae, tribe Leptothoracini) and to an out-group antCamponotus ligniperda (Formicinae). We found that parasitic species and the host species and alsoCamponotus ligniperda differ at less than 1% of the base positions of the 1.2 kb segment of the 18S rRNA gene. The sequences showed 80.3% identity to the 18 S ribosomal RNA genes of the beetleTenebrio molitor and only 66.5% to that of the dipteranDrosophila melanogaster.
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  • 60
    ISSN: 1423-0445
    Keywords: defensive secretion ; hot secretion ; elytral flanges ; evolution ; benzoquinones ; hydrocarbons ; bombardier beetle ; Coleoptera ; Carabidae ; Paussinae
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    Topics: Biology
    Notes: Summary The Australian bombardier beetle,Mystropomus regularis, sprays a mixture of quinones (1,4-benzoquinone, 2-methyl-1,4-benzoquinone, 2-ethyl-1,4-benzoquinone) and hydrocarbons (principallyn-pentadecane). The defensive fluid ist generated explosively in two-chambered glands, and is ejected audibly and hot (maximal recorded temperature = 59°C).Mystropomus is a member of the paussoid lineage of bombardiers. In common with other members of the group, it has a pair of elytral flanges (flanges of Coanda), associated with the gland openings, that serve as launching guides for anteriorly-aimed ejections of spray. It is argued thatMystropomus may be the least derived of flanged paussoids, and the closest living relative of the most primitive of extant bombardiers (Metriini).
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  • 61
    ISSN: 1423-0445
    Keywords: sex pheromone ; synergist ; antagonist ; mate recognition ; reproductive isolation ; chemotaxonomoy ; phylogeny ; evolution ; Lepidoptera ; Tortricidae
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    Topics: Biology
    Notes: Summary The geometric isomers (E,E)-, (E,Z)-, (Z,E)-, and (Z,Z)-8,10-dodecadien-1-yl acetate were identified as sex pheromone components or sex attractants in the tribes Eucosmini and Grapholitini of the tortricid subfamily Olethreutinae. Species belonging to the more ancestral Tortricinae were not attracted. Each one isomer was behaviourally active in males ofCydia andGrapholita (Grapholitini), either as main pheromone compound, attraction synergist or attraction inhibitor. Their reciprocal attractive/antagonistic activity in a number of species enables specific communication with these four compounds.Pammene, as well as otherGrapholita andCydia responded to the monoenic 8- or 10-dodecen-1-yl acetates. Of the tribes Olethreutini and Eucosmini,Hedya, Epiblema, Eucosma, andNotocelia trimaculana were also attracted to 8,10-dodecadien-1-yl acetates, but several otherNotocelia to 10,12-tetradecadien-1-yl acetates. The female sex pheromones ofC. fagiglandana, C. pyrivora, C. splendana, Epiblema foenella andNotocelia roborana were identified. (E,E)- and (E,Z)-8,10-dodecadien-1-yl acetate are producedvia a commonE9 desaturation pathway inC. splendana. CallingC. nigricana andC. fagiglandana females are attracted to wingfanning males.
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    Insectes sociaux 39 (1992), S. 425-438 
    ISSN: 1420-9098
    Keywords: Formicidae ; Nothomyrmecia ; evolution ; sociogram ; ethogram ; recognition
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    Topics: Biology
    Notes: Summary Results of laboratory-based ethological studies on twoNothomyrmecia macrops colonies with individually marked workers are reported. Interactive behavioural acts constituted less than 1% of all those recorded, revealing a strong tendency by the ants not to engage in social contact. Very few workers performed queen-directed acts. They stayed near the queen, though seldom in direct contact. Division of labour was otherwise barely apparent, except that some individuals showed a propensity to guard the nest entrance. No exchange of food was observed between workers, workers and queen, or adults and larvae (apart from worker placement of prey items with larvae). A queen fed from aDrosophila carcass retrieved from the nest floor, without assistance from workers. Systematic scanned observations confirmed levels of inactivity higher than previously observed in ants (comprising almost 2/3 of recorded behavioural acts). The time budget for activities directed toward the immature stages was the same in both colonies, and fluctuated during the circadian period. Non-nestmate larvae added to worker groups were more frequently licked than nestmate larvae, but this might not involve the particular recognition of nestmateversus non-nestmate brood. These observations support the hypothesis thatNothomyrmecia is primitively eusocial, and of special significance in myrmecology.
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    Insectes sociaux 43 (1996), S. 375-389 
    ISSN: 1420-9098
    Keywords: Nasutitermitinae ; Subulitermes ; Coatitermes ; Velocitermes ; evolution ; phylogeny
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    Topics: Biology
    Notes: Summary The developmental pathways of the neuter castes were studied in three species of Nasutitermitinae from central Panama. The humivorousSubulitermes denisae andCoatitermes clevelandi display several primitive traits: absence of sex dimorphism, representation of both sexes among workers and soldiers, and occurrence of successive worker instars. The litter-dwellingVelocitermes barrocoloradensis has a more complex caste system: female larvae are larger than males and give rise to the large workers, which constitute the bulk of the work force; male larvae proceed to soldiers through a small worker or a special larval instar. The resulting soldier caste is polymorphic. These results support previously formulated hypotheses regarding a link between humivorous diet and reduced polymorphism on the one hand, and between forest-floor foraging and large continuous size variation among soldiers on the other. Whereas the caste systems ofSubulitermes andCoatitermes probably represent a primitive condition,Velocitermes shares derived traits withNasutitermes and the other fully nasute genera previously studied. I therefore hypothesize that ancestors with these advanced features may have spread from the neotropics and be at the origin of most nasute genera, including humivorous taxa, present in other regions.
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  • 64
    ISSN: 1420-9098
    Keywords: Formicidae ; Leptothoracini ; Tetramoriini ; internal transcribed spacer ; social parasitism ; evolution ; phylogenetics
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    Notes: Summary A fragment of the internal transcribed spacer (ITS-1) adjacent to the 5.8S rRNA gene of 20 myrmicine ant species was sequenced. Sequence comparisons were carried out between 11 species of the tribe Leptothoracini, five species of the tribe Tetramoriini, three species of the tribe Solenopsidini and one species of the tribe Myrmicini. Additionally, the formicine antCamponotus ligniperda (tribe Camponotini) was analyzed as an outgroup species. Among all investigated species, the fragment had a variable length of ≈ 230–380 bp with only a few conserved sequence elements. The sequences of this fragment were perfectly identical within four palearctic populations ofLeptothorax acervorum indicating that intraspecific variation is rather low. Within the species of Tetramoriini (includingAnergates atratulus) 94.1% of sequence positions were identical, 95.6% within the species of theLeptothorax s.str.-group and 64.6% within the species of theMyrafant-group. Phylogenetic analysis reveals that the social parasitesHarpagoxenus sublaevis, Doronomyrmex goesswaldi, D. kutteri andD. pacis, Chalepoxenus muellerianus as well asStrongylognathus alpinus andTeleutomyrmex schneideri are most closely related to the groups of their respective host species, which generally confirms the taxonomical classifications of the subfamily Myrmicinae based on morphological criteria. The taxonomical positions of the speciesA. atratulus has as yet been uncertain, however, sequence comparison of the ITS-1 fragment leads to the conclusion thatA. atratulus rather belongs to the tribe Tetramoriini than to the Solenopsidini.
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    Development genes and evolution 191 (1982), S. 1-4 
    ISSN: 1432-041X
    Keywords: Embryo ; RNA ; evolution
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    Topics: Biology
    Notes: Summary Frog embryo nuclear and cytoplasmic RNA populations, labeled in vivo and in vitro, were hybridized to, filterbound homologous and heterologous DNA. The transcription of homologous (frog) repetitive DNA into nuclear RNA decreases qualitatively during development while the transcription of heterologous (minnow, human) repetitive DNA into nuclear RNA remains relatively constant qualitatively. The diversity of homologous repetitive mRNA increases during development, but there is only a slight change in the diversity of heterologous repetitive mRNA transcripts. There is a marked restriction of transport of the heterologous RNA sequences to the cytoplasm at a later stage of development.
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    Development genes and evolution 204 (1994), S. 62-69 
    ISSN: 1432-041X
    Keywords: Cell determination ; direct development dorsoventral axis ; echinoids ; evolution
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    Topics: Biology
    Notes: Abstract In the direct-developing sea urchin Heliocidaris erythrogramma the first cleavage division bisects the dorsoventral axis of the developing embryo along a frontal plane. In the two-celled embryo one of the blastomeres, the ventral cell (V), gives rise to all pigmented mesenchyme, as well as to the vestibule of the echinus rudiment. Upon isolation, however, the dorsal blastomere (D) displays some regulation, and is able to form a small number of pigmented mesenchyme cells and even a vestibule. We have examined the spatial and temporal determination of cell fates along the dorsoventral axis during subsequent development. We demonstrate that the dorsoventral axis is resident within both cells of the two-celled embryo, but only the ventral pole of this axis has a rigidly fixed identity this early in development. The polarity of this axis remains the same in half-embryos developing from isolated ventral (V) blastomeres, but it can flip 180° in half-embryos developing from isolated dorsal (D) blastomeres. We find that cell fates are progressively determined along the dorsoventral axis up to the time of gastrulation. The ability of dorsal half-embryos to differentiate ventral cell fates diminishes as they are isolated at progressively later stages of development. These results suggest that the determination of cell fates along the dorsoventral axis in H. erythrogramma is regulated via inductive interactions organized by cells within the ventral half of the embryo.
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    Insectes sociaux 38 (1991), S. 263-272 
    ISSN: 1420-9098
    Keywords: Isoptera ; Kalotermitidae ; Neotermes papua ; termites ; caste differentiation ; division of labour ; evolution
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    Topics: Biology
    Notes: Summary The direct development ofNeotermes papua (Isoptera: Kalotermitidae) comprises four larval and three nymphal instars before the alate. The first five instars can be easily characterized. The second stage nymphs come morphologically close to the pseudergates, characterized by reduced wing buds. These nymphs can moult stationarily, i.e. with little morphological change, or to presoldiers, or proceed to the alate via the third nymphal stage. Pseudergates originate through a late and reversible deviation from the straight development to the alate. Presoldiers may derive from several stages, up to the last nymphal one; their production is subject to an inhibition by extant soldiers. This developmental schema is congruent with those described in other Kalotermitidae and the Termopsidae. By pinpointing the existence of a large pool of pluripotent individuals, in which the penultimate nymphal stage mingles with pseudergates, the present study also reveals a great similarity betweenNeotermes andProrhinotermes, and suggests that this developmental schema might be generally applicable to termites devoid of a permanent worker caste.
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  • 68
    ISSN: 1420-9098
    Keywords: Isoptera ; Termitidae ; Nasutitermitinae ; caste differentiation ; phylogeny ; evolution
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    Notes: Summary The developmental pattern of the neuter castes was studied in the mandibulate nasute generaCornitermes, Embiratermes andRhynchotermes. InCornitermes walkeri, all the workers and soldiers are male. There are two larval and a single worker instar. Workers can molt into presoldiers. InEmbiratermes chagresi andRhynchotermes perarmatus, both sexes are present among the neuters. A slight sexual dimorphism (males 〉 females) is discernible among both larval instars and among workers ofE. chagresi; female workers can molt into presoldiers. InR. perarmatus, the sexual dimorphism is conspicuous from the first larval instar on. Male larvae go through two instars, then give rise to workers, which do not molt. InR. perarmatus, there is no worker stage in females, but a third larval instar, preceding the presoldier. Hypotheses are proposed as to the evolution of these caste patterns, attempting to conciliate present knowledge of Nasutitermitinae phylogeny and known evolutionary trends affecting termite caste patterns, according to the species' ecology.
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    Insectes sociaux 42 (1995), S. 57-69 
    ISSN: 1420-9098
    Keywords: Hindgut ; alkalinity ; evolution ; symbionts ; gut morphology
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    Topics: Biology
    Notes: Summary The pH of the gut contents was measured in 52 species of higher termites (Termitidae), representing 36 genera in all four subfamilies. A statistically significant trend was shown from lower termites with low mean gut pH through to the Termitinae with higher mean gut pHs. Elevation of the pH occurred principally in the first and third proctodaeal segments, reaching values as high as 10.5 in 8 soil-feeding genera and 1 wood-feeding genus of Termitinae. Elevation of gut pH within the Termitidae appears to be independent of the general nature of the feeding substrate.
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  • 70
    ISSN: 1432-072X
    Keywords: Key words Auxostat ; Batch culture ; Chemostat ; Continuous culture ; Fermentation control ; Inhibition ; kinetics ; Nutristat ; On-line measurement ; Pentachlorophenol ; Pollutant ; Sphingomonas ; Steady-state conditions ; Toxicity
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract A bacterium degrading pentachlorophenol (PCP) as the only source of carbon and energy was grown in a “nutristat”, i.e., a continuous culture with on-line measurement and control of the substrate concentration. We improved the PCP nutristat by incorporation of a personal computer with a proportional integral derivative (PID) algorithm for controlling the medium feed pump. The controlled value deviated from the average (set-point) value by 1% maximally. In the PCP nutristat (30°C), the steady-state dilution rate, and hence, specific growth rate, showed a maximum value of 0.142 ± 0.004 h–1 at set-point PCP concentrations between 37 and 168 μM. At PCP concentrations above 168 μM, the steady-state growth rate decreased because of inhibition. The growth yield coefficient was not seriously affected by the PCP concentration, suggesting that uncoupling was not the inhibitory mechanism. It was concluded that the PCP nutristat is very useful for establishing steady-state conditions that maintain growth-inhibitory PCP concentrations and high cell concentrations, conditions for which the chemostat is not suitable.
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    European biophysics journal 13 (1986), S. 343-353 
    ISSN: 1432-1017
    Keywords: Lipid/cholesterol ; phase transition ; kinetics ; second order transition ; pressure jump relaxation
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    Topics: Biology , Physics
    Notes: Abstract Lipid bilayers and monolayers composed of dimyristoylphosphatidic acid (DMPA) and cholesterol were characterized by differential scanning calorimetry and film balance measurements. Increasing cholesterol content decreases the bilayer phase transition temperature and enthalpy in a manner similar to that observed before for other lipid/cholesterol systems. In monomolecular films at the air-water interface cholesterol exhibits the well known condensing effect in the liquid-expanded phase, while the liquid-condensed phase is less affected. As with the bilayer phase transition, the transition temperature and change in area at the liquid-condensed to liquid-expanded phase transition, as measured from isobars at 25 dynes/cm, decreases with increasing cholesterol content. The kinetics of the phase transition of DMPA/cholesterol bilayers were measured using the pressure jump relaxation technique with optical detection. Three relaxation times were observed. The relaxation times and amplitudes pass through maximum values at the transition midpoint. With increasing cholesterol content the maximum values of the relaxation times decrease but not in a linear fashion. The time constants display an intermediate maximum at ca. 10% to 12 mol% cholesterol. This observation is discussed in terms of a possible change in the nature of the phase transition from first-order with phase separation to a continuous second-order transition. The dependence of the relaxation amplitudes on cholesterol content gave evidence for nucleation being the rate limiting step for the transition in this particular system.
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  • 72
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    European journal of clinical pharmacology 17 (1980), S. 285-293 
    ISSN: 1432-1041
    Keywords: tolbutamide ; chlorpropamide ; kinetics ; food ; age ; blood glucose ; plasma insulin
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The influence of food intake (standardized breakfast) on the oral single-dose kinetics and effects of tolbutamide (0.5 g) and chlorpropamide (250 mg) was investigated in young, healthy volunteers. The single-dose kinetics of the two drugs was also studied in elderly healthy subjects. There was great interindividual variation in the elimination rate of both drugs, but food intake influenced neither their AUCs nor their rates of absorption and elimination. The peak concentration of chlorpropamide, but not that of tolbutamide, was reduced by food intake. The peak concentrations of serum tolbutamide were approximately doubled by an increase in dose from 0.5 to 1.0 g, and from 1.0 to 2.0 g. At no time did tolbutamide 0.5 g affect the plasma insulin level, neither in the fasting nor in the non-fasting state. However, this dose did reduce the blood glucose level during fasting and the increase in blood glucose in response to the meal. The latter effect was recorded within 30 min, when the serum level of tolbutamide still was close to zero. Plasma insulin concentrations did increase within 30 min after a higher dose of tolbutamide (1.0 g), when the serum concentration of tolbutamide was about 50 µmol/l. Between 2.5 and 8 h after administration of chlorpropamide 250 mg, serum drug concentrations were lower than those following tolbutamide 0.5 g. The blood glucose response was smaller and occurred later, being significant at 2 h, when the serum concentration of the drug was about 70 µmol/l. There was no significant change in plasma insulin. There was no significant pharmacokinetic difference between young and elderly subjects, except that the peak concentration of tolbutamide was higher in the latter. It appears that both for tolbutamide and chlorpropamide there is great interindividual variation in drug disposition, but food intake does not influence the bioavailability of either drug. The effect of any particular drug concentration seems dependent upon the blood glucose level and hence upon the elapsed time since the last meal. Both drugs can reduce blood glucose without an alteration in the peripheral blood concentration of insulin. This may reflect an extrapancreatic effect of the drugs, but it could also be an expression of increased insulin secretion, which is not detected because of enhanced hepatic degradation of the hormone released into the portal circulation. The observations made in young individuals are also probably relevant for elderly subjects.
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  • 73
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    European journal of clinical pharmacology 22 (1982), S. 309-314 
    ISSN: 1432-1041
    Keywords: acetylsalicylic acid ; salicylic acid ; dipyridamol ; bioavailability ; kinetics ; rapid- and slow-release formulations
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Acetylsalicylic acid (ASA) is a strong, irreversible inhibitor of platelet aggregation, but loses this activity following first-pass deacetylation to salicylic acid (SA). In order to compare the bioavailability of unchanged ASA from rapid- and slow-release formulations, the single-dose concentration profiles of ASA and SA were studied in healthy volunteers following intake of two different rapid-release (conventional and effervescent tablets) and three different slow-release (microencapsulated ASA in tablets and in capsules, and enteric-coated tablets) formulations of ASA, and of one slow-release formulation of sodium salicylate. Since anti-platelet therapy with ASA is often combined with dipyridamol, the influence of this drug was also examined. The concentrations of ASA and SA were measured by high-pressure liquid chromatography. While the bioavailability of SA from the 5 ASA formulations was essentially equal and similar to that of the salicylate formulation, the bioavailability and peak concentrations of ASA appeared to be the much greater after rapid-release than after slow-release formulations. Indeed, ASA was only rarely detected in systemic blood following intake of slow-release ASA. Co-administered dipyridamol did not significantly influence the kinetics of ASA or SA. It appears that rapid-release formulations of ASA should be prefered in anti-platelet therapy, either alone or in combination with dipyridamol.
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  • 74
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    European journal of clinical pharmacology 23 (1982), S. 529-533 
    ISSN: 1432-1041
    Keywords: beta-blocker ; bufuralol ; enantiomers ; kinetics ; metabolism ; man
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Single oral doses of (+)-, (−)- and (±)-bufuralol were administered to a healthy volunteer to compare the disposition and metabolism of the individual isomers and the racemate. Plasma levels and area under plasma curve (AUC) of the active isomer, (−)-bufuralol, were higher than those of the (+)-isomer; plasma clearance was correspondingly lower. Intermediate values were found for the racemate. The elimination half-life of (−)-bufuralol was shorter than that of (+)-bufuralol, but similar to the racemate. Both isomers were cleared almost entirely by metabolism. The main metabolic pathway for (−)-bufuralol was aromatic hydroxylation, whereas the principal route for (+)-bufuralol was conjugation. Phenol metabolites in the systemic circulation were present mainly as conjugates. Both isomers also underwent aliphatic hydroxylation. This pathway was more favoured by the (+)-isomer, although plasma levels and AUC of the principal product, 2′-hydroxy-bufuralol, were almost identical for the two forms. Major differences in metabolic fate thus had relatively little effect on the disposition of pharmacologically active metabolites.
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  • 75
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    European journal of clinical pharmacology 24 (1983), S. 217-220 
    ISSN: 1432-1041
    Keywords: metoprolol ; pregnancy ; hypertension ; kinetics ; pre-eclampsia
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The disposition of oral metoprolol was studied in 5 women during the last trimester of pregnancy and 3 to 5 months after delivery. After a single oral dose of 100 mg the individual peak plasma concentration in the pregnant state was only 20–40% of that after pregnancy. The plasma half-lives of metoprolol were about the same during (average 1.3 h) and after pregnancy (average 1.7 h). By contrast, the area under the plasma concentration versus time curve was much smallerduring (mean 262 nmol/l×h) thanafter (mean 1298 nmol/l×h) pregnancy, resulting in an average apparent oral clearance (Clo) of metoprolol that was 4.4times higher during (362 ml×kg−1 body-weight×min−1) than after pregnancy. The increased Clo in pregnancy is assumed to be due to enhanced hepatic metabolism of the drug. The possible clinical consequence of the difference in the disposition of metoprolol is discussed.
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  • 76
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    Keywords: prizidilol ; antihypertensive effect ; acute and long-term blood pressure control ; plasma renin activity ; acetylator phenotype ; antinuclear antibodies ; side effects ; kinetics
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary After an initial placebo period of four weeks 24 patients with primary hypertension were treated with prizidilol, a hydrazinopyridazine derivative with combined vasodilator and non-selective beta-adrenoceptor blocking actions, for a dose titration period of 14 weeks. Prizidilol 200 to 800 mg was given once daily to achieve a target supine diastolic blood pressure (BP)〈90 mmHg. Supine and standing BP recorded 24–27 h after drug intake decreased from 172±17/106±6 mmHg (mean±SD) and 167±18/111±8 mmHg, respectively, after placebo to 159±16/99±8 and 154±18/101±9 mmHg after active treatment for six weeks (mean dose 447 mg), and to 154±16/97±7 and 148±14/97±7 mmHg after treatment for 14 weeks (mean dose 687 mg/day). A slight reduction in HR was seen after treatment for six weeks and in plasma renin activity and urinary methoxycatecholamine excretion after treatment for 14 weeks. A sustained decrease in BP was observed for 10 h after prizidilol 800 mg (n=9), with a maximum antihypertensive effect (mean reduction in supine BP 33/18 mmHg) 2.5 h after dosing, which coincided with the mean peak plasma concentration. The plasma elimination half-life of the drug was 3.9 h (range 2.0–8.9 h). Changing to a twice daily regimen in 17 patients (mean daily dose 748 mg at six months) did not produce any further reduction in the BP (recorded 12–15 h after dosing) as compared to the once daily regimen at 14 weeks. During treatment for up to 24 months, 16 patients did not achieve satisfactory BP control. Eight of them were withdrawn and eight received additional treatment with bendroflumethiazide (2.5–5 mg/day). In 7 of the latter satisfactory BP control was achieved. Side effects were few. Dizziness and tiredness occurred in four patients 2–5 h after prizidilol 600–800 mg once daily. These symptoms partly subsided when the subjects changed to a twice daily regimen. No ocular side-effects were found. Before treatment 13 out of 24 patients had a low titre of IgM antinuclear antibodies (ANA) and one patient also a low titre of IgG ANA. During treatment the frequency of patients with positive ANA-titres became higher, and after treatment for 12 months (n=17) 15 patients had positive IgM and seven patients positive IgG ANA-titres. However, the titres were low and no patient showed a clinical lupus erythematosus syndrome. There was no relation between acetylator phenotype of the patient and acute or longterm effecton BP, pharmacokinetics of the drug or the development of a raised ANA-titre.
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  • 77
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    European journal of clinical pharmacology 24 (1983), S. 801-806 
    ISSN: 1432-1041
    Keywords: acebutolol ; hydrochlorothiazide ; kinetics ; drug combination ; interaction ; diacetolol ; healthy subjects ; renal clearance
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of acebutolol and hydrochlorothiazide (HCT) alone or in combination were studied in 12 healthy subjects in a cross over study. Acebutolol and diacetolol (the main metabolite) in plasma and urine were determined by HPLC and hydrochlorothiazide by GLC. The main pharmacokinetic parameters of acebutolol did not differ significantly: AUC 4492±272 µg l−1 h given alone versus 4118±354 µg l−1 h with HCT, half-life (7,69±0,32 h vs 8,10±0,72 h) and renal clearance (13,1±0,5 lh−1 vs 13,8±0,9 lh−1), respectively. There was no difference in diacetolol pharmacokinetics. HCT values were not significantly different: AUC 784±48 µg l−1 h given alone and 720±42 µg l−1 h with acebutolol, t1/2 (4,79±0,37 h vs 4,73±0,43 h). The renal clearance was slightly higher when HCT was given with acebutolol (26,2±2,6 vs 20,3±2,11 h−1,p〈0,05). This increase, observed during the first four hours, was probably due to competition between the drugs for binding to red blood cells.
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  • 78
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    European journal of clinical pharmacology 22 (1982), S. 27-32 
    ISSN: 1432-1041
    Keywords: sulfonylureas ; diabetes ; chlorpropamide ; glipizide ; C-peptide ; insulin ; blood glucose ; kinetics
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The influence of sulfonylurea on the secretion, disposal and effect of insulin was studied in 9 Type 2 diabetics during 3 one-month courses of treatment with a) chlorpropamide (t1/2〉24 h) once daily, b) glipizide (t1/2=2–4 h) once daily, and c) glipizide in divided doses. Food intake by each patient was identical during each period. Blood concentrations of immunoreactive insulin (IRI) and C-peptide (radioimmunoassays), and of glucose (enzymatic assay), chlorpropamide (gas chromatography) and glipizide (high-pressure liquid chromatography) were determined before and after breakfast and lunch on the 4th day of each examination period. All comparisons were intraindividual. Despite the lunch-time dose of glipizide given during the divided dose treatment, once-daily administration of this drug led to higher drug concentrations not only after breakfast but also for the first few hours after lunch. Divided dosage, on the other hand, led to higher concentrations later. In contrast to once-daily dosage, continuous exposure to glipizide was found in most patients. Chlorpropamide gave the most continuous sulfonylurea exposure. The blood glucose levels were inversely related to the concurrent sulfonylurea concentrations; glucose levels after breakfast and lunch were lowest during once-daily glipizide, whereas the fasting level was lowest during chlorpropamide treatment. The IRI response to breakfast was 60%–70% higher during once-daily glipizide than during the other two treatments, but the C-peptide responses to breakfast were almost identical. Thus, the greater after-breakfast availability of peripheral insulin appeared to be due to an effect of glipizide on the extrapancreatic disposal of the hormone.
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  • 79
    ISSN: 1432-1041
    Keywords: digoxin ; verapamil ; digoxin-verapamil interaction ; kinetics ; plasma level ; renal clearance ; extra-renal clearance
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Single-dose investigations in healthy subjects have demonstrated substantial impairment of renal and extrarenal clearance of digoxin during coadministration of verapamil. A longitudinal study has been performed to assess the changes in digoxin disposition during long-term verapamil therapy. After one week of verapamil 240 mg/d mean plasma digoxin had risen from 0.21±0.01 ng/ml (SE) to 0.34±0.01 ng/ml (p〈0.01), and renal digoxin clearance had fallen from 197.57±17.37 ml/min to 128.20±10.33 ml/min (p〈0.001). These changes gradually subsided, and after six weeks, renal digoxin clearance had normalized and plasma digoxin had declined to 0.27±0.02 ng/ml (NS). The 24-h urinary recovery of digoxin increased from 46.46±3.23% before to 69.78±3.69% (p〈0.001) after six weeks of verapamil co-administration, and this elevation persisted throughout the study. The verapamil-induced suppression of renal digoxin elimination disappears over a few weeks of drug exposure, whereas the inhibition of the extrarenal clearance of digoxin seems to persist.
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  • 80
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    European journal of clinical pharmacology 24 (1983), S. 273-276 
    ISSN: 1432-1041
    Keywords: undernourished ; chlorquine ; kinetics ; plasma levels ; red cell uptake
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The plasma and whole blood kinetics of chloroquine was studied in 7 normal and 8 undernourished subjects following a single oral dose of 600 mg. The terminal half-lives were similar in both groups. The AUC was also similar in the 2 groups, even though a higher dose per kg body weight was administered to the undernourished. This was probably because of faster clearance in this group. Chloroquine uptake by erythrocytes, its main site of action in malaria, was also comparable in the two groups. The plasma concentration of chloroquine over a period of time was found to be similar in 4 normal and 4 undernourished subjects following administration of 1.5 g of the drug in divided doses. The undernourished appear, therefore, to handle chloroquine in such a way that they do not suffer a greater risk of toxicity than normals.
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  • 81
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    European journal of clinical pharmacology 24 (1983), S. 525-527 
    ISSN: 1432-1041
    Keywords: theophylline ; airway obstruction ; biotransformation ; kinetics ; oral dosage
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Oral theophylline was given to 6 adults with airways obstruction. The initial dose was 125 mg daily and this was increased by 125 mg each week. The final total daily dose reached was determined by side effects and ranged from 500 mg to 1125 mg. At the end of each week and before the next dosage increment steady state, trough plasma theophylline concentrations were measured. For each individual and for the group as a whole there was a highly significant linear correlation between theophylline dose and trough plasma concentration. This indicates that for oral theophylline, in adults, dose-dependent kinetics do not play a significant role and dose may be adjusted without fear of a disproportionate rise in plasma concentration.
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  • 82
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    European journal of clinical pharmacology 27 (1984), S. 491-494 
    ISSN: 1432-1041
    Keywords: amiodarone ; kinetics ; volunteers
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary We studied three healthy volunteers after a single i.v. bolus of amiodarone, during 1 month of chronic oral dosing and after the discontinuation of the drug. Blood concentrations of amiodarone declined rapidly in a bi-exponential fashion after i.v. bolus. The terminal half-life ranged from 10 to 17 h; after discontinuation of chronic treatment the terminal half-lives were 8–21 days. The i.v. data, the trough levels during multiple dosing and the washout phase could be simultaneously fitted using a tri-exponential equation. The subjects were carefully monitored for cardiac and thyroid function. One subject had to stop taking amiodarone because of profound bradycardia. A reduction of serum TT3 and FT3 concentrations and an increase of serum rT3 and FT4 was found.
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  • 83
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    European journal of clinical pharmacology 26 (1984), S. 521-530 
    ISSN: 1432-1041
    Keywords: chloroquine ; malaria ; rheumatoid disease ; kinetics ; major metabolite ; optimal dosage ; therapeutic regime ; monodesethylchloroquine ; bidesethylchloroquine
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The kinetics and disposition of chloroquine (CQ) and its metabolite monodesethylchloroquine (CQM) were investigated in 5 healthy volunteers after incremental (150–300–600 mg CQ base) single oral doses of CQ. The analytical method used (HPLC and fluorescence detection) is the most sensitive known method for CQ and CQM. Plasma and whole blood concentrations of CQ, CQM and a third metabolite, bidesethylchloroquine (CQMM), were determined. The kinetics of CQ was found to be unique. The best fit was obtained by a multicompartmental model. The biological half-life appeared to be between 30–60 days; the volume of distribution (Vd) was ∼ 800l/kg, and the clearance ∼ 11/h/kg when calculated from plasma data. The whole blood concentrations were ∼ 8–10 times higher than in plasma, and consequently the Vd and whole blood clearance were ∼ 10 times lower. The kinetics changed as the dose was increased. An indication of capacity-limited steps in CQ disposition was found, as the rate constants decreased even though the clearance remained the same. The intrinsic half-life of CQM was 1/4 of that of CQ, but was prolonged after the highest dose of CQ. The present knowledge of CQ kinetics could provide a basis for revision of current dosage regimens in malaria suppression and rheumatoid disease to ensure efficacious and safe therapy.
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  • 84
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    European journal of clinical pharmacology 27 (1984), S. 367-369 
    ISSN: 1432-1041
    Keywords: flurbiprofen ; syrup ; suppository ; kinetics ; children ; bioavailability
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Eight subjects, aged 6–12 years and weighing 18.8–36.7 kg, received single doses of flurbiprofen 50 or 75 mg (corresponding to 1.4–2.7 mg/kg) as syrup and suppository in a Latin square design. Half-life (2.7–3.2 h), elimination constant (0.22–0.26 h−1), area under the plasma level curve (72.4–77.3 µg·h·ml−1) and time to reach the concentration peak (1–0.75 h) were similar after the syrup and suppository. Flurbiprofen showed equivalent bioavailability after oral and rectal administration and the same pharmacokinetic profile was confirmed in children as observed in adults.
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  • 85
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    European journal of clinical pharmacology 29 (1985), S. 251-253 
    ISSN: 1432-1041
    Keywords: paracetamol ; antacids ; acetaminophen ; bioavailability ; kinetics
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effect of two antacids on the bioavailability of paracetamol has been investigated in 12 young healthy volunteers. Following a random cross over design, each subject swallowed, on three separate occasions, one weak apart, 500 mg paracetamol alone, or together with two different aluminium hydroxide, magnesium hydroxide preparations (Dimalan and Maalox). Plasma paracetamol levels were measured by HPLC. The bioavailability of paracetamol was not altered by either antacid, but they both delayed the time to peak plasma concentration (0.85 h; 1.43 h; 1.25 h, without antacid, with Dimalan and with Maalox respectively). The peak plasma concentration was not affected by concurrent antacid administration.
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  • 86
    ISSN: 1432-1041
    Keywords: Theophylline ; kinetics ; apnea ; premature newborns ; developmental pharmacology
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Aminophylline (theophylline-ethylenediamine) was administered to 27 premature newborns to prevent apneic spells. Of the 22 patients monitored for theophylline concentration, a therapeutic blood level was reached in 19 in 1–2 days, and 3 stayed below it. ‘Toxic’ blood levels (≥20 µg/ml) were reached in 3 cases, one of whom showed signs of toxicity. Theophylline treatment was not efficient in the prevention of apnea when a serious underlying disease was present. Theophylline blood half-life (mean : 27.0 h) and clearance (mean 12.9 ml/h/kg) confirmed the slow elimination pattern of the drug in the premature infant.
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  • 87
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    European journal of clinical pharmacology 21 (1982), S. 403-408 
    ISSN: 1432-1041
    Keywords: glibenclamide ; diabetes ; insulin ; kinetics ; blood glucose ; relationship to meals ; absorption
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In an attempt to assess whether intake of glibenclamide before meals would improve its therapeutic capacity, the present investigation compared the effect of glibenclamide 2.5mg t.i.d. given before and together with meals. In addition, these effects were compared with that of glibenclamide given as a single morning dose of 7.5mg. The subjects studied were six Type 2 diabetics not previously exposed to sulphonylurea drugs. Irrespective of dosage and mode of administration, addition of glibenclamide to a standardized breakfast, lunch and dinner enhanced plasma IRI concentrations and reduced blood glucose concentrations as compared to administration of meals without the drug. The different modes of glibenclamide administration did not differ significantly with respect to IRI responses. However, the blood glucose reduction after breakfast was significantly greater when glibenclaimde 2.5mg had been given before the meal than when 2.5 or 7.5mg were given with the meal; a similar, but non-significant tendency was observed after lunch; no consistent difference was seen after dinner. Food intake did not affect glibenclamide kinetics. It appears that administration of glibenclamide 2.5mg before breakfast improved glucose utilization following the breakfast load, due to earlier attainment of an effective concentration of glibenclamide.
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  • 88
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    European journal of clinical pharmacology 22 (1982), S. 225-228 
    ISSN: 1432-1041
    Keywords: pinazepam ; N-desmethyldiazepam ; kinetics ; metabolism ; human
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The plasma profile of a single oral dose of pinazepam 10 mg was studied in 6 healthy male volunteers, aged 26 to 31 years. The concentrations of the parent compound and of its metabolite in plasma were measured by gas-chromatography. The peak plasma levels of pinazepam was 36.8±5.1 ng/ml and of N-desmethyldiazepam 150±13.3 ng/ml. The plasma concentration of the metabolite become higher than that of the parent compound shortly after administration, suggesting that pinazepam acts as a prodrug.
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  • 89
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    European journal of clinical pharmacology 22 (1982), S. 435-439 
    ISSN: 1432-1041
    Keywords: azlocillin ; kinetics ; biliary excretion ; liver dysfunction
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    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetic of azlocillin was followed in five elderly patients after biliary surgery. Total clearance was 138.6±17.7 ml/min when 2.0 g was given as an i.v. bolus injection. The half-life of the β-phase averaged 110 min. The total clearance and the half-life of azlocillin were influenced by slight impairment of renal function (creatinine clearance 59.4±13.6 ml/min). In patients with normal liver function biliary excretion of the drug amounted to 5.3±2.8% of the dose (n=3) and the kinetics of biliary excretion were linear. In contrast, in two patients with impaired liver function biliary excretion was 0.2% and 0.5% of the dose, and kinetic analysis of biliary excretion rates revealed at least one zero order step in the excretion process. Renal excretion of the drug amounted to 45.0±17.7% of the dose, which means that 50% of the total clearance of azlocillin has to be accounted for by metabolic clearance.
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  • 90
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    European journal of clinical pharmacology 29 (1986), S. 529-534 
    ISSN: 1432-1041
    Keywords: pethidine ; epidural injections ; pain scores ; kinetics ; spinal cord
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Twenty-one patients who had undergone total hip replacement were randomly assigned to one of three groups in order to compare a single dose of 1 mg/kg of pethidine im (I) and 20 mg (II) or 60 mg of extradural pethidine (III) in a double-blind design. The degree of analgesia, the adverse effects, and the kinetics were studied for 18 h. Pain was monitored using a visual analogue scale (VAS). Supplementary doses of oxycodone if required were given no earlier than 0.75 h after pethidine. Plasma concentrations of pethidine were measured with gas chromatography mass spectrometry (GCMS). Hypoalgesia to pin prick test was evaluated. Low pain scores were observed in the extradural groups between 0.25 and 1.5 h after the dose. A significant difference in pain score compared with the im group was found after the higher extradural dose only between 0.5 and 1 h (p〈0.05). The area under the curve (AUC) of pain score versus time (0–18 h) was not significantly different between groups. The recorded adverse effects were minor in all three groups. The terminal half-lives and plasma clearances of pethidine, and the time to peak concentration were not different between the groups. Single patients in the extradural groups showed hypoalgesia to pin prick in parallel to the effect. The present study shows that extradural pethidine produces shortlived analgesia, in contrast to the long-lasting effect of morphine found in other studies.
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  • 91
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    European biophysics journal 16 (1989), S. 321-325 
    ISSN: 1432-1017
    Keywords: Sodium currents ; inactivation ; kinetics ; channel gating
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    Topics: Biology , Physics
    Notes: Abstract The time constant of the process producing the delay in Na inactivation development as determined by the two pulse method (τdelay) was extracted and compared to that of the slowest Na activation process τ3 for the I Na during the conditioning pulse of that same determination. τdelay and two pulse inactivation τc values were computer generated using a nonlinear least squares algorithm. τh and single pulse inactivation τh values were independently generated for each determination also with the aid of the computer using the same non-linear least squares algorithm. In one determination at 2 mV, τc was 4.68 and τdelay 0.494 ms while τh was 4.70 and τ3 0.491 ms for a τc/τh of 0.996 and a τdelay/τ3 of 1.006. Mean τdelay/τ3 from five determinations in four axons, both Cs and K perfused, and spanning a potential range of-27 to 2mV was 1.068. The precursor process to inactivation is channel opening. Some fraction of channels presumably inactivate via another route where prior channel opening is not required.
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  • 92
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    European journal of clinical pharmacology 28 (1985), S. 163-169 
    ISSN: 1432-1041
    Keywords: indomethacin ; platelet aggregation ; prostanoids ; plasma concentration ; arachidonic acid ; thromboxane B2 ; 6-keto-prostaglandin F1α ; kinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A single oral dose of indomethacin 1 mg/kg was given to 6 male and 6 female volunteers. The formation of thromboxane B2 (TXB2) and 6-ketoprostaglandin F1α (6-keto-PGF1α) in clotting whole blood was measured by radioimmunoassay, and platelet aggregation induced by archidonic acid (AA) was measured with a plasma aggregometer. The results were related to the concomitant plasma concentration of indomethacin. The maximum plasma concentration ranged between 3.24 and 8.11 µg/ml and the elimination half-life between 4 and 11 h. Formation of the prostanoids was reversibly inhibited, with maximum suppression when the drug concentration in plasma exceeded 0.5–1.0 µg/ml; the IC50 was approximately 0.1 µg/ml. Platelet aggregation was also reversibly inhibited. The correlation between the formation of prostanoids and the different phases of the aggregatory response to exogenous AA is discussed.
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  • 93
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    European journal of clinical pharmacology 21 (1981), S. 215-220 
    ISSN: 1432-1041
    Keywords: phenytoin ; cimetidine ; antipyrine test ; drug interaction ; drug metabolism ; kinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In a prospective study in nine patients the effects of phenytoin and of cimetidine (1000mg/day) + phenytoin on the antipyrine test and serum phenytoin concentrations were studied. Serum phenytoin increased from the steady state level of 5.7±1.3 mg/l to 9.1±1.4mg/l after three weeks on cimetidine (p〈0.01), and fell to 5.8±1.2 mg/l within two weeks after withdrawal of cimetidine. The protein binding of phenytoin was not changed by cimetidine. After use of phenytoin for 2–4 months, antipyrine clearance increased from 0.67±0.06ml/min/kg to 1.61±0.22 ml/ min/kg, and antipyrine half-live fell from 10.9±1.3h to 4.5±0.6h as compared to the values before phenytoin treatment (p〈0.01). After three weeks combined use of cimetidine and phenytoin, antipyrine clearance was decreased to 1.01±0.07 ml/min/kg and antipyrine half-life was prolonged to 6.1±0.5h, (p〈0.01) compared to the values on phenytoin alone. The distribution volume of antipyrine was not affected by phenytoin nor by cimetidine + phenytoin. The half-life of cimetidine was 2.8±0.3h in the patients on longterm phenytoin treatment. There was a significant positive correlation (p〈0.001) between the increase in serum phenytoin concentration and the prolongation of antipyrine half-life caused by cimetidine. Thus, cimetidine increases serum phenytoin concentration, very probably by inhibiting its metabolism. Care should be taken in the concomitant use of cimetidine and phenytoin, and the dose of phenytoin should be modified according to the clinical symptoms and serum phenytoin concentrations.
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  • 94
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    European journal of clinical pharmacology 22 (1982), S. 545-551 
    ISSN: 1432-1041
    Keywords: oxcarbazepine ; kinetics ; disposition ; metabolites ; renal excretion ; volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Oxcarbazepine (oxcarb) 600 and 900 mg (2360 and 3540 µmol) was taken by 3 volunteers (2 ♀, 1 ♂; 45–67 kg; age 22–34 years) after an overnight fast. Blood, saliva and urine were collected for the next 72 h for assay of oxcarb, 10,11-dihydro-10-hydroxy-carbamazepine (OHcarb), and 10,11-dihydrotrans-10,11-dihydroxy-carbamazepine (diol). Oxcarb reached a maximum level of about 1 µg/ml (3.93 µmol/l) within 1 h and dropped below the detection limit (0.1 µg/ml=0.39 µmol/l) within 3 h. The active metabolite OHcarb appeared in the blood before oxcarb and reached the higher maximum level of 7.4 µg/ml (29 µmol/l) after 7 h. Thereafter serum levels decreased with a t1/2 of about 25 h, and after 40 h with a t1/2 of 9 h, the latter agreeing with the renal excretory t1/2 calculated from the urine data (10 h). The ratio of OHcarb concentration in saliva to that in plasma varied considerably (0.3–1.7; median 1; r〉0.9), whereas that of blood to plasma was 1.25 with only small variation (r〉0.98); OHcarb concentrations in erythrocytes were 50% higher than in plasma. Diol was detected in blood (maximum level 0.5 µg/ml=1.84 µmol/l) in 2 volunteers. 45% of the dose could be recovered in urine (Oxcarb 5%, OH-carb 36%, Diol 4%). Whereas Oxcarb was completely conjugated, only 25% of OHcarb was conjugated and diol was unconjugated.
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  • 95
    ISSN: 1432-1041
    Keywords: metoprolol ; age ; disposition ; elderly subjects ; kinetics ; metabolism ; alpha-OH-metoprolol
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The absorption and disposition of metoprolol have been evaluated in 10 healthy, non-smoking, elderly individuals (mean age 73.1 years) by simultaneous determination of [3H]-metoprolol and unlabelled metoprolol. The labelled drug was given as an intravenous tracer dose, immediately followed by oral metoprolol 25 mg. The experiment was preceded by administration of metoprolol 25 mg b.i.d. for 3 days. The volume of distribution, elimination half-life and total body clearance were almost the same as previously observed in healthy, young subjects. The mean systemic availability was about 39% in the elderly, which is lower than the mean of 55% observed in a control group of young volunteers who received 50 mg b.i.d. In the elderly, the mean plasma concentration of α-OH-metoprolol was about twice as high as that of the parent drug, whereas the opposite was true of the control group. The results indicate that age-related physiological changes have a negligible effect on the pharmacokinetics of metoprolol.
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  • 96
    ISSN: 1432-1041
    Keywords: hyperthyroidism ; propranolol ; methimazole ; metoprolol ; atenolol ; kinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The kinetic profiles of oral methimazole 40mg, propranolol 80mg, metoprolol 100mg and atenolol 100mg were compared in hyperthyroid patients both during the hyper-and euthyroid states. For methimazole, neither the peak concentration (Cmax), the time to reach peak concentration (tmax), the elimination half-life (t1/2) nor the area under the curve (AUC) value was affected by the hyperthyroid state. For propranolol and metoprolol, which undergo extensive presystemic clearance, the AUC values were lower (p〈0.02) when the patients were hyperthyroid than when they had become euthyroid, but the t1/2's were not significantly altered. For atenolol, there were no significant kinetic differences between the hyperthyroid and euthyroid states. The findings are compatible with the assumption that hyperthyroidism does not affect the kinetics of methimazole or atenolol, but that it may enhance presystemic clearance of propranolol and metoprolol.
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  • 97
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    European journal of clinical pharmacology 23 (1982), S. 261-266 
    ISSN: 1432-1041
    Keywords: mexiletine ; rifampicin ; kinetics ; enzyme induction ; excretion ; antipyrine clearance ; dosage adjustment
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary To study the effects of enzyme induction on its pharmacokinetics, a single oral dose of the new antiarrhythmic agent mexiletine hydrochloride 400 mg was administered to 8 healthy volunteers before and after treatment with rifampicin 300 mg b.i.d. for ten days. The absorption and distribution of mexiletine were not changed after rifampicin, but its elimination half-life fell from 8.5±0.8 h (mean±SE) to 5.0±0.4 h (p〈0.01), and its nonrenal clearance increased from 435±68 ml/min to 711±101 ml/min (p〈0.01). The mean renal clearance of mexiletine did not change, but it showed an exponential correlation with urinary pH. The amount of unchanged mexiletine excreted in urine over two days decreased from 32±7 to 18±3 mg (p〈0.01). The half-life of antipyrine fell from 11.8±0.4 to 5.5±0.3 h and its clearance increased from 40±3 ml to 74±3 ml/min (p〈0.01). There was a significant (p〈0.05) positive linear correlation between both the half-lives and the clearances of antipyrine and mexiletine. The clearances were positively correlated with serum γ-glutamyl transpeptidase. The results suggest that the dosage of mexiletine should be adjusted when enzyme inducing drugs are started or stopped during therapy with it.
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  • 98
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    European journal of clinical pharmacology 27 (1984), S. 233-236 
    ISSN: 1432-1041
    Keywords: glibenclamide ; acarbose ; kinetics ; alpha-glucosidase inhibitor ; blood glucose control ; plasma insulin ; Type 2 diabetes
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A single dose of glibenclamide 5 mg was administered to six Type 2 diabetics, randomly treated for 7 days either with acarbose (3×100 mg daily) or with placebo. The serum concentration of the drug was measured for 10 h. Peak concentrations, times-to-peak concentration, elimination half-lives and the extent of bioavailability of the drug were not significantly modified by acarbose. The combined administration of glibenclamide and acarbose resulted in a modest improvement in the blood glucose profile after breakfast and lunch, together with a significant diminution in plasma insulin. Thus, acarbose appears a useful additional treatment for Type 2 diabetics already receiving sulphonylurea derivatives.
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  • 99
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    European journal of clinical pharmacology 10 (1976), S. 43-48 
    ISSN: 1432-1041
    Keywords: Spironolactone ; acetylsalicylic acid ; fludrocortisone ; kinetics ; pharmacology ; interaction
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The influence of 600 mg acetylsalicylic acid (ASA) on the renal excretion and clearance of canrenone, the principal unconjugated metabolite of spironolactone, was examined in a double-blind crossover study in six healthy subjects. ASA significantly reduced the urinary excretion, and the fractional excretion, of canrenone between 4 — 6 hours after administration of 50 mg spironolactone. The pharmacological activity of spironolactone, assessed simultaneously by alterations in fludrocortisone-induced urinary electrolyte changes, was slightly but not significantly reduced. The reductions in urinary canrenone excretion correlated with changes in the urinary log 10 Na/K ratio. The results suggest that canrenone may be actively secreted at the proximal renal tubule, and that secretion is blocked by ASA or its conjugates. This is a possible mechanism for the pharmacological interaction between ASA and spironolactone which has been described previously.
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  • 100
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    European journal of clinical pharmacology 22 (1982), S. 39-45 
    ISSN: 1432-1041
    Keywords: furosemide ; neonates ; kinetics ; placental transfer ; intravenous therapy
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of furosemide was evaluated in 12 newborns who received the drug transplacentally, and in 21 neonates who received it directly for therapeutic reasons. In the first group, the apparent plasma half-lives ranged from 96 to 6.8 h with a significant inverse relationship (p〈0.01) between the gestational age and the elimination rate. In two cases a clear effect on diuresis was also observed. In the neonates receiving the drug i.v. for therapeutic reasons, the elimination kinetics appeared to follow a two-compartment open model, with a significant difference in the therminal plasma half-life between premature (26.8±12.2 h) and full-term newborns (13.4±8.6 h). In this group no relationship was observed between elimination rate and either gestational or conceptional age. In the case of repeated administration, an increase in plasma clearance and reduction in t1/2 β was noticed.
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