{"title":"[Effect of histamine on the isolated aorta of the rabbit. Study of cyproheptadine].","authors":"M Auguet","doi":"","DOIUrl":null,"url":null,"abstract":"<p><p>The vascular effects induced by histamine and their inhibition by cyproheptadine have been studied on rabbit aortic strips. On arteries pre-contracted with phenylephrine, histamine provokes a dose-dependent relaxation only when mepyramine is present in the bath. This effect is independent of the integrity of endothelium. Cyproheptadine (10(-9) M) required the presence of cimetidine to give a parallel antagonism of the histamine curve (Kb: 0.32 nM). At higher concentrations of cyproheptadine (3 X 10(-9) and 10(-8) M) the effect was non-competitive. Cyproheptadine displaced to the right in a parallel manner the dose response curve of noradrenaline (pA2 = 6.6) and of serotonin (pA2 = 8.9) and reduced the contracting effects of KCl (IC50 = 7.3 10(-7) M) and of angiotensin II (IC50 = 4 X 10(5) M).</p>","PeriodicalId":14817,"journal":{"name":"Journal de pharmacologie","volume":"17 3","pages":"260-5"},"PeriodicalIF":0.0000,"publicationDate":"1986-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal de pharmacologie","FirstCategoryId":"1085","ListUrlMain":"","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0
Abstract
The vascular effects induced by histamine and their inhibition by cyproheptadine have been studied on rabbit aortic strips. On arteries pre-contracted with phenylephrine, histamine provokes a dose-dependent relaxation only when mepyramine is present in the bath. This effect is independent of the integrity of endothelium. Cyproheptadine (10(-9) M) required the presence of cimetidine to give a parallel antagonism of the histamine curve (Kb: 0.32 nM). At higher concentrations of cyproheptadine (3 X 10(-9) and 10(-8) M) the effect was non-competitive. Cyproheptadine displaced to the right in a parallel manner the dose response curve of noradrenaline (pA2 = 6.6) and of serotonin (pA2 = 8.9) and reduced the contracting effects of KCl (IC50 = 7.3 10(-7) M) and of angiotensin II (IC50 = 4 X 10(5) M).