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 › peer-review

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

Keywords

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

ASJC Scopus subject areas

Cellular and Molecular Neuroscience
Pharmacology

Access to Document

10.1016/0014-2999(75)90246-0

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@article{1232a1e3270646738ad361902ce2ed0e,

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

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

author = "Roberto Levi and Ganellin, {C. Robin} and Geoffrey Allan and Willens, {Howard J.}",

note = "Funding Information: * Supported by USPHS Grant 1 RO1 GM 20091, by a grant-in-aid of the New York Heart Association and by the John Polachek Foundation for medical research.",

year = "1975",

month = nov,

doi = "10.1016/0014-2999(75)90246-0",

language = "English (US)",

volume = "34",

pages = "237--240",

journal = "European Journal of Pharmacology",

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T1 - Selective impairment of atrioventricular conduction by 2-(2-pyridyl)-ethylamine and 2-(2-thiazolyl)-ethylamine, two histamine H1-receptor agonists

AU - Levi, Roberto

AU - Ganellin, C. Robin

AU - Allan, Geoffrey

AU - Willens, Howard J.

N1 - Funding Information: * Supported by USPHS Grant 1 RO1 GM 20091, by a grant-in-aid of the New York Heart Association and by the John Polachek Foundation for medical research.

PY - 1975/11

Y1 - 1975/11

N2 - 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.

AB - 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.

KW - 2-(2-Pyridyl)-ethylamine

KW - 2-(2-Thiazolyl)-ethylamine

KW - Atrioventricular conduction

KW - Cardiac histamine receptors

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