TY - JOUR
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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U2 - 10.1016/0014-2999(75)90246-0
DO - 10.1016/0014-2999(75)90246-0
M3 - Article
C2 - 1234767
AN - SCOPUS:0016816845
VL - 34
SP - 237
EP - 240
JO - European Journal of Pharmacology
JF - European Journal of Pharmacology
SN - 0014-2999
IS - 1
ER -