ISSN:
1573-3904
Keywords:
agonist
;
bradykinin
;
cyclic kinins
;
smooth muscle contraction
Source:
Springer Online Journal Archives 1860-2000
Topics:
Chemistry and Pharmacology
Notes:
Summary Three linear bradykinin (BK) analogues, Lys-Lys-BK, Nle-Lys-BK and Lys-Nle-BK and their head-to-tail cyclic analogues, along with cyclo-Nle-Nle-BK and cyclo-Lys-Lys-[Trp5]BK, were synthesized and tested on an isolated rat duodenum preparation. All kinins, except the [Trp5]-analogue, cause relaxation with EC50 values in the picomolar range. The most potent linear analogue (Lys-Nle-BK) is about 40 times more active than BK and the most potent cyclic kinin (cyclo-Nle-Lys-BK) is about 6 times more active. Present results suggest that the significant potency of cyclo-Lys-Lys-BK, the earlier most potent cyclic kinin which is only a little less potent than linear BK, depends on the ring size rather than on the presence of the extra basic residues.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF02443585
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