Selective impairment of atrioventricular conduction by 2-(2-pyridyl)-ethylamine and 2-(2-thiazolyl)-ethylamine, two histamine H1-receptor agonists

Roberto Levi; C. Robin Ganellin; Geoffrey Allan; Howard J. Willens

doi:10.1016/0014-2999(75)90246-0

Selective impairment of atrioventricular conduction by 2-(2-pyridyl)-ethylamine and 2-(2-thiazolyl)-ethylamine, two histamine H₁-receptor agonists

Roberto Levi, C. Robin Ganellin, Geoffrey Allan, Howard J. Willens

Medicine

Research output: Contribution to journal › Article

25 Scopus citations

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.

Original language	English (US)
Pages (from-to)	237-240
Number of pages	4
Journal	European Journal of Pharmacology
Volume	34
Issue number	1
DOIs	https://doi.org/10.1016/0014-2999(75)90246-0
State	Published - Nov 1975

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Keywords

2-(2-Pyridyl)-ethylamine
2-(2-Thiazolyl)-ethylamine
Atrioventricular conduction
Cardiac histamine receptors

ASJC Scopus subject areas

Cellular and Molecular Neuroscience
Pharmacology

Cite this

Levi, R., Ganellin, C. R., Allan, G., & Willens, H. J. (1975). Selective impairment of atrioventricular conduction by 2-(2-pyridyl)-ethylamine and 2-(2-thiazolyl)-ethylamine, two histamine H₁-receptor agonists. European Journal of Pharmacology, 34(1), 237-240. https://doi.org/10.1016/0014-2999(75)90246-0

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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.",

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10.1016/0014-2999(75)90246-0