The antagonizing activity of a novel peptide analogs, iQWcF,on the function of endothelin receptors
- VernacularTitle:新型类肽化合物iQWcF对内皮素受体功能的拮抗作用
- Author:
Gaishun FEI
;
Wensheng YU
;
Keliang LIU
;
Hai WANG
;
- Publication Type:Journal Article
- Keywords:
endothelin;
endothelin receptor;
antagonist
- From:
Chinese Pharmacological Bulletin
1987;0(03):-
- CountryChina
- Language:Chinese
-
Abstract:
AIM To evaluate the antagonizing activity of iQWcF, a modified tripeptide, to endothelin receptors. METHORDS ①Vasoconstriction experiments with aorta strips of rats. ② In vivo experiments:male normotensive Wistar rats were anesthetized with pentobarbital Na (50 mg?kg -1 ),and catheterized into the carotic artery for measurement of blood pressure, and into the femoral vein for administration of iQWcF (30 mg?kg -1 ) and ET 1(0 9 nmol?kg -1 ). The test compound was given intravenously 5 min before the bolus injection of ET 1. Control animals received saline on the same time schedule.The blood pressure was recorded at different time interval after injecting ET 1. RESULTS ①iQWcF prohibited the vascontriction of aorta induced by ET 1 in a concentration dependent fashion.②The compound(30 mg?kg -1 .iv) markedly antagonized ET 1 induced the long lasting pressor phase mediated by ET A without affecting early transient depressor phase by ET B. CONCLUSION iQWcF is one of ET A selective antagonists.
