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  • pharmacokinetics  (599)
  • Coleoptera
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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    European journal of nutrition 22 (1983), S. 14-26 
    ISSN: 1436-6215
    Keywords: branched chain α-keto acids ; 4-methyl-2-oxopentanoate, 3-methyl-2-oxopentanoate ; 3-methyl-2-oxobutyrate ; dehydrogenation ; transamination ; pharmacokinetics ; absorption
    Source: Springer Online Journal Archives 1860-2000
    Topics: Agriculture, Forestry, Horticulture, Fishery, Domestic Science, Nutrition , Medicine
    Description / Table of Contents: Zusammenfassung Michaelis-Konstanten und Aktivitäten von Dehydrogenasen und Transaminasen der drei verzweigten α-Ketosäuren Keto-Valin, Keto-Leucin und Keto-Isoleucin in Leber, Niere, Skeletmuskel und Gehirn von Ratten werden mitgeteilt. Nach oraler Zufuhr passieren nur 11–22% der Ketosäuren unverändert die Leber. Aus pharmakokinetischen und Resorptions-Untersuchungen erhaltene Blutspiegel an Ketosäuren werden zu den Michaelis-Konstanten in Beziehung gesetzt. Bei den geringen Konzentrationen an Ketosäuren nach oraler Zufuhr kann angenommen werden, daß die oxidativen Prozesse in den nichthepatischen Geweben über die Transaminierung überwiegen. Daten über die Wachstumseffizienz von verzweigtkettigen α-Ketosäuren im Vergleich zu den entsprechenden Aminosäuren stimmen mit dieser Vorstellung überein. Bei intravenöser Verabreichung müßten die Voraussetzungen für Transaminierung besser sein als nach oraler Zufuhr. Auf der Basis von Daten aus der Literatur werden die Übertragbarkeit unserer Befunde auf den Menschen und die verschiedenen Faktoren, welche die Effizienz der verzweigten α-Ketosäuren durch Einwirkung auf ihren Stoffwechsel beeinflussen können, diskutiert.
    Notes: Summary Miehaelis-constants and enzyme activities for dehydrogenation and transamination of the three branched chainα-keto acids in liver, kidney, skeletal muscle, and brain of rats are reported. After oral load only 11–22 % of the keto acids pass the liver unchanged. Blood levels in pharmacokinetic and absorption studies are related to the Michaelis-constants. At the low keto-acid concentrations after oral application, dehydrogenation in the non-hepatic tissues is supposed to prevail over transamination. Data on feed efficiency of branched chain α-keto acids reported in the literature support this view. The chance for transamination is better after intravenous administration. The transferability of our data to humans, and various factors influencing the efficiency of branched chain α-keto acids are discussed in connection with data reported in the literature.
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  • 2
    ISSN: 1570-7458
    Keywords: Pterostichus melanarius ; Coleoptera ; Carabidae ; pitfall traps ; insecticides ; prey ; hunger ; activity ; Rhopalosiphum padi ; Fenitrothion ; Sumicidin (Fenvalerate) ; spring barley
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Description / Table of Contents: Résumé Au cours d'essais à grande échelle, effectués en 1981 et 1982, sur orge de printemps, pour évaleur l'effet des insecticides Fenitrothion et Sumicidine (fenvalerate) sur les arthropodes utiles, un accroissement significatif des captures, dans des trappes pièges de Barber, de Pterostichus melanarius (Illiger) a été observé plusierus semaines après le traitement dans les lots traités par rapport aux lots témoins. Significativement plus de femelles de P. melanarius ont été capturées dans les parcelles traitées pendant cette période d'accroissement après traitement. Une diminution correspondante dans les populations de proies a été observée à la suite des traitements. Chaque femelle de P. melanarius des parcelles traitées avait une fraction significativement moins importance de son intestin remplie d'aliments solides (arthropodes) que celles des parcelles non traitées. Des auteurs précédents avaient observé des taux de capture plus rapides dans les trappes et ne plus grande mobilité des carabes affamés. La réduction des populations proies par l'application d'insecticides affamerait les carabes dont l'activité serait par suite plus élevée. Comme le taux de captures dans les trappes est dû à la fois à la taille de la population et à son activité, on en déduit que la capture par trappes seule ne peut donner une image exacte de l'effet des insecticides sur les populations de carabes dans les champs.
    Notes: Abstract During large-scale field experiments in 1981 and 1982, designed to assess the effects of the insecticides Fenitrothion and Sumicidin (Fenvalerate) on beneficial arthropods in spring barley, significant increases in pitfall-trap catches of Pterostichus melanarius (Illiger) were observed in treated plots compared to untreated controls, several weeks after treatment. Significantly more female P. melanarius were caught in treated plots during these post-treatment increases. Corresponding decreases were observed in prey populations following treatments. Individual female P. melanarius from treated plots had significantly fewer of their gut areas full of solid (arthropod) food when compared to those from untreated control plots. Earlier workers observed both faster recapture rates in pitfalls and higher mobility in hungry carabid beetles. The following hypothesis is suggested: reducing prey populations by the application of insecticides results in hungrier carabid beetles with consequently higher activity. Since pitfall-trap catch is determined not only by population size but also activity, it is argued that pitfall-trap catches alone cannot give a true measure of the effects of insecticides on carabid populations in the field.
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    Entomologia experimentalis et applicata 30 (1981), S. 151-156 
    ISSN: 1570-7458
    Keywords: Xyleborus ferrugineus ; pupae ; ecdysteroids ; pharate adult ; radioimmunoassay ; Coleoptera ; Scolytidae
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Description / Table of Contents: Zusammenfassung Der Ecdysteroidtiter weiblicher Puppen von Xyleborus ferrugineus (Fabr.) wurde geschätzt, indem ganze Tiere homogenisiert und radioimmunologisch untersucht wurden. Ein ausgeprägtes Maximum an Ecdysteroiden wurde bei 36 Stunden Puppenent-wicklung beobachtet (743 pg/mg Körpergewicht). Der Titer nahm ab auf 299 pg/mg im Pharatstadium und auf 193 pg/mg unmittelbar vor Schlüpfen der Adulten. Qualitative Studien mit HPLC ergaben in frischen Puppen ein Verhältnis von 3:1 Ecdyson zu 20-Hydrooxyecdyson. Pharatstadien enthielten vor allem 20-Hydrooxyecdyson. Das beobachtete einzige Maximum im Titer stimmt überein mit den Resultaten bei andern untersuchten Coleopteren.
    Notes: Abstract Ecdysteroid titers were estimated on the whole body homogenates of Xyleborus ferrugineus (Fabr.) female pupae during development by radioimmunoassay. A distinct peak of ecdysteroids was observed at 36-hr pupal development (743 pg/mg body wt). Titer declined to 299 pg/mg by the pharate adult stage and to 193 pg/mg body wt just before adult emergence. Qualitative studies by HPLC revealed a ratio of 3:1 ecdysone to 20-hydroxyecdysone in the initial pupal stage. Pharate adults had mainly 20-hydroxyecdysone. The observed single peak in ecdysteroid titer agrees with findings in other studied coleopteran species.
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    Entomologia experimentalis et applicata 34 (1983), S. 291-296 
    ISSN: 1570-7458
    Keywords: Coleoptera ; Curculionidae ; Cyrtobagous ; Salvinia weevil ; Feeding characteristics of larvae ; Development of larvae ; Plant nutrition ; Temperature effects on development
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Description / Table of Contents: Résumé Après leur naissance, les larves de Cyrtobagous sp. passent de 1 à 4 jours à brouter les racines, et de 0 à 9 jours dans les bourgeons de la plante hôte, Salvinia molesta, avant d'y creuser une galerie dans le rhizome. Bien que les larves aient été capables de survivre jusqu'à 38 jours en broutant les racines, quant elles furent privées de rhizome, elle ne purent achever leur développement. Quand les galeries furent commencées, le développement larvaire, entre 21° et 31°, dépendit de la température et de la teneur en azote de l'hôte. Les larves ne se développèrent pas à 17°. Une haute valeur nutritive de l'aliment consommé par les larves réduisit la durée du développement, mais n'influença pas la durée ultérieure de leur développement nymphal. Les lieux de prise de nourriture et les dégâts produits par des larves isolées furent précisés.
    Notes: Abstract Newly-emerged larvae of a salvinia weevil, Cyrtobagous sp. spent from 1–4 days browsing on the roots and from 0–9 days in the buds of the host plant, Salvinia molesta, prior to tunnelling into the rhizome of this aquatic weed. Although larvae were able to survive up to 38 days browsing on roots when rhizomes were withheld, they were unable to complete development. After tunnelling began, larval development between 21° and 31° was dependent on temperature and nitrogen levels in the host. Larvae failed to develop at 17°. High nutritional intake by the larvae reduced larval development time but did not influence duration of their subsequent pupal development. The feeding sites and plant damage produced by individual larvae were assessed.
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  • 5
    ISSN: 1570-7458
    Keywords: Coleoptera ; Curculionidae ; Cylas formicarius elegantulus ; sweetpotato weevil ; sweet potato ; digestion ; enzyme distribution ; trypsin-inhibitors ; resistance
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Description / Table of Contents: Résumé L'activité endoprotéinase était limitée au liquide de la lumière des régions ventriculaires antérieure et postérieure de l'intestin moyen des larves deCylas formicarius elegantulus Summers. Les aminopeptidases ont été trouvées dans le liquide de la lumière (18%), mais étaient principalement associées avec les fractions insolubles des cellules du ventricule postérieur (82%). Suivant le substrat, l'activité carboxypeptidase était à peu près également répartie entre le liquide de la lumière et les fractions insolubles des cellules du ventricule postérieur. L'amylase, enzyme secrétée, a été observée à la fois dans la lumière antérieure et postérieure. Cinq bandes d'activité amylase ont été révélées sur zymogrammes d'amidon après électrophorèse d'intestins moyens entiers. Trois des bandes d'amylase pouvaient provenir de la plante. Il y avait au moins 2 α-glucosidases, une secrétée et une liée aux cellules du ventricule antérieur. L'activite β-glucosidase était liée aux cellules du ventricule antérieur, fandis que l'activité α-galactosidase était limitée au fluide de la lumière. Les activités β-galactosidase et cellulase ont été trouvées à la fois dans le liquide de la lumière et dans la fraction cellulaire insoluble. Ainsi, la digestion initiale des grosses protéines et des polymères de carbohydrates se produit dans le liquide de la lumière dans les régions ventriculaires antérieure et postérieure. Cependant, l'achèvement de la digestion des oligopeptides se produit principalement dans le ventricule postérieur, tandis que la fin de la digestion des oligosaccharides se produit dans le ventricule antérieur. Les concentrations en inhibiteurs de trypsine de 5 cultivars d'I. batatas L. diffèrent de 1 à 20. Les endoprotéinases deC. formicarius elegantulus ont été inhibées par des extraits de cultivars, mais les cultivars avec des concentrations relativement élevées d'inhibiteur avainent antérieurement montré être susceptibles d'être attaqués par le coléoptère dans des essais en champs.
    Notes: Abstract Endoproteinase activity was confined to luminal fluid from anterior and posterior ventricular regions of midguts of larvae of the sweetpotato weevil,Cylas formicarius elegantulus (Summers). Aminopeptidase was found in luminal fluid (18%) but was primarily associated with insoluble fractions from cells of the posterior ventriculus (82%). Depending on substrate, carboxypeptidase activity was about equally distributed between luminal fluid and insoluble fractions from posterior ventriculus cells. Amylase was found in luminal fluid in both the anterior and posterior ventriculus. Five bands of amylase activity were detected on starch zymograms following electrophoresis of whole midgut samples. Three of the amylase bands may be plant-derived. At least two α-glucosidases were present, one secreted and one bound to anterior ventriculus cells. β-Glucosidase activity was bound to anterior ventriculus cells whereas α-galactosidase activity was confined to luminal fluid. β-Galactosidase and cellulase activities were found in both luminal fluid and the insoluble cell fraction. Thus, initial digestion of large protein and carbohydrate polymers occurs in luminal fluid in both anterior and posterior ventriculus regions. However, terminal digestion of oligopeptides occurs primarily in the posterior ventriculus while terminal digestion of oligosaccharides occurs in the anterior ventriculus. A 20-fold difference in trypsin-inhibitor concentration was found among five sweetpotato cultivars. Endoproteinases from sweetpotato weevil larvae were inhibited by extracts from the cultivars but cultivars with relatively high concentrations of inhibitor were previously shown to be susceptible to weevil attack in field trials.
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  • 6
    Electronic Resource
    Electronic Resource
    Springer
    Entomologia experimentalis et applicata 34 (1983), S. 124-126 
    ISSN: 1570-7458
    Keywords: Negret ; Melanic mutant ; X-linked mutation ; Flour Beetle ; Tribolium confusum ; Coleoptera
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
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  • 7
    ISSN: 1570-7458
    Keywords: Storage pests ; Coleoptera ; Bostrichidae ; Prostephanus truncatus ; (±)-1-methylbutyl (E)-2-methyl-2-pentenoate ; Rhyzopertha dominica ; (±)-1-methyl-butyl (E)-2,4-dimethyl-2-pentenoate ; Dominicalure ; Aggregation pheromone ; Monitoring
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Description / Table of Contents: Résumé Les réponses de Prostephanus truncatus Horn (Coleoptera: Bostrichidae) à deux constituants de la phéromone d'agrégation de Rhyzopertha dominica Fabricius (Coleoptera: Bostrichidae), le (±)-1-méthylbutyl (E)-2-méthyl-2-penténoate et le (±)-1-méthylbutyl (E)-2,4-diméthyl-2-pentéoate, connus comme “Dominicalure 1” et “Dominicalure 2”, ont été étudiées au laboratoire et au champ. Auslaboratoire ces composés ont été essayés individuellement et en mélange 1:2. Une membrane de caoutchouc imprégnée de phéromone a été utilisée comme émetteur lent, et une courbe de réponse en fonction de la dose a été établie. P. truncatus répondait plus vigoureusement à la Dominicalure 2 seule. Tous ces traitements ont été comparés dans un essai aux champs en Tanzanie, dans lesquels des pièges en carton ondulé contenant des diffuseurs de phéromone étaient placés dans des entrepôts de maïs dans les fermes. La Dominicalure 1 et le mélange de 1 et 2 étaient tous deux efficaces pour piéger R. dominica. La Dominicalure 2 a piégé plus de P. truncatus que les autres traitements et était à peu près aussi efficace que le contrôle visuel pour détecter la présence de cet insecte dans les stocks. On peut envisager que la Dominicalure 2 pourrait servir de base à un programme pour lutter contre P. truncatus en Afrique de l'Est.
    Notes: Abstract Laboratory and field studies have been made of the responses of Prostephanus truncatus (Horn) to two components of the aggregation pheromone of Rhyzopertha dominica (Fabricius) — (±)-1-methylbutyl (E)-2-methyl-2-pentenoate and (±)-1-methylbutyl (E)-2,4-dimethyl-2-pentenoate, known as “Dominicalure 1” and “Dominicalure 2” respectively. In the laboratory, these compounds were tested individually and as a 1:2 mixture; P. truncatus responded most strongly to Dominicalure 2 alone. All three treatments were compared in a field trial in Tanzania to monitor both R. dominica and P. truncatus in farm stores. Dominicalure 1 or a mixture of 1 and 2 were both highly effective for trapping R. dominica. In contrast, Dominicalure 2 trapped more P. truncatus than the other treatments and was about as effective as visual inspection at demonstrating the presence of the beetle in stores. Dominicalure 2 could form the basis of a monitoring programme for P. truncatus in East Africa.
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  • 8
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 8 (1975), S. 97-105 
    ISSN: 1432-1041
    Keywords: Di-n-propylacetate ; 2-propyl-valeric acid sodium salt ; pharmacokinetics ; anti-epileptic ; drug monitoring ; man
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of the anti-epileptic drug di-n-propylacetate (DepakineR) have been studied in 7 patients, in whom plasma concentrations were determined during and following subchronic treatment. Elimination of the drug appeared to follow a monophasic exponential course; biological half lives were 8 to 15 hours. The data supported the assumption that an open one-compartment model can be used to describe the kinetics of dipropylacetate in man. The drug appeared to have a relatively restricted distribution: calculated relative distribution volumes ranged from 0.15 to 0.40 1/kg. There were large interindividual differences in clearance rate. The therapeutic range was considered to be between 50 and 100 mg/1 plasma. Plasma levels of phenobarbital were markedly raised during treatment with dipropylacetate for an unknown reason. Determination of the plasma concentrations of drugs at accurately fixed times appears to be a reliable method for pharmacotherapeutic monitoring of epileptic patients.
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  • 9
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 8 (1975), S. 157-160 
    ISSN: 1432-1041
    Keywords: Isosorbide dinitrate ; pharmacokinetics ; metabolism ; pharmacological action ; nitrates
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary An oral dose of 5 mg of14C-isosorbide dinitrate was rapidly absorbed, biotransformed and excreted by human subjects. Peak whole blood concentrations of radioactivity were reached after 1.5 to 2 hours and declined relatively slowly. The radioactivity in whole blood mainly represented metabolites, isosorbide mononitrates. The peak concentrations found were 4.5, 11.7 and 34.3 ng/ml of isosorbide dinitrate, isosorbide 2-mononitrate and isosorbide 5-mononitrate, respectively, in the blood of one subject and 5.9, 15 and 61.3 ng/ml, respectively, in the blood of another subject. However, concentrations of the metabolites declined relatively slowly during 6 h after the oral dose. Up to 99% of an oral dose of isosorbide dinitrate was excreted during 5 days, mainly in the urine of the first day (ca. 78%). The results showed that isosorbide mononitrates were available to contribute to the pharmacological action.
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  • 10
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 8 (1975), S. 241-248 
    ISSN: 1432-1041
    Keywords: pharmacokinetics ; experimental design
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary It is apparent from studying recent articles on pharmacokinetics that a number of misunder-standings exist, both about the design of experiments and the analysis of results. The purpose of this paper is to outline many of the common pitfalls associated with the design of experiments and also the limitations upon the analysis of results. The paper describes mathematical, laboratory and clinical aspects which must be examined in designing a protocol for pharmacokinetic experiments. Simulated data is presented to demonstrate the dangers of using standard computer programs for parameter estimation. Even when convergence is obtained the answers may be dependent on the method employed. A mathematical model is of little use unless a reasonable amount of good, accurate data is obtained.
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