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Selective impairment of atrioventricular conduction by 2-(2-pyridyl)-ethylamine and 2-(2-thiazolyl)-ethylamine, two histamine H1-receptor agonists.
Authors:R Levi  C R Ganellin  G Allan  H J Willens
Institution:1. Department of Pharmacology, Cornell University Medical College, New York, N.Y. 10021, U.S.A.;7. The Research Institute, Smith Kline and French Laboratories Ltd., Welwyn Garden City, Hertfordshire, England
Abstract:To further characterize the receptor mediating histamine-induced impairment of atrioventricular conduction, the effects of two selective histamine H1-receptor agonists, 2-(2-pyridyl)-ethylamine (PEA) and 2-(2-thiazolyl)-ethylamine (ThEA), were investigated using the isolated guinea pig heart. These effects were compared with those of histamine and other selective agonists. PEA and ThEA produced a weak stimulation of cardiac rate and contractility; however, they produced a marked prolongation of atrioventricular conduction. The orders of relative potencies observed substantiate the hypothesis that H2-receptors mediate the positive inotropic and chronotropic effects and H1-receptors mediate the negative dromotropic effect of histamine.
Keywords:Cardiac histamine receptors  2-(2-Pyridyl)-ethylamine  2-(2-Thiazolyl)-ethylamine  Atrioventricular conduction
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