In Vitro Cardiac Pharmacology of the New Histamine H2-receptor Agonist Amthamine: Comparisons with Histamine and Dimaprit

Overview

Journal Agents Actions

Specialty Pharmacology

Date 1993 Sep 1

PMID 8147269

Citations 3

Authors

E Poli

C Pozzoli

G Coruzzi

G Bertaccini

H Timmerman

Affiliations

Soon will be listed here.

Abstract

The cardiac activity of the novel histamine H2-receptor agonist amthamine was investigated in a variety of isolated heart preparations from guinea pigs and humans and in the isolated rabbit aorta. Amthamine caused an increase in the sinus rate of spontaneously beating guinea-pig atria (pD2 = 6.72) and in the contractility of the electrically driven guinea-pig papillary muscle (pD2 = 6.17) and of the human atrium (pD2 = 5.38). In all these systems, amthamine behaved as a full agonist with a potency comparable to or slightly higher than that of histamine and 10 times higher than that of dimaprit. The positive effects of amthamine were competitively antagonized by ranitidine which had pA2 values (6.46 and 6.25 in the guinea-pig atria and papillary muscle, respectively) comparable with those calculated against histamine and dimaprit. In the isolated rabbit aorta amthamine was devoid of H1-mediated activities up to 3 x 10(-4) M. These results indicate that amthamine is a potent and selective histamine H2-receptor agonist which can be considered a valuable tool for investigating H2-receptor mediated effects in cardiac tissues.

Citing Articles

The Roles of Cardiovascular H-Histamine Receptors Under Normal and Pathophysiological Conditions.

Neumann J, Kirchhefer U, Dhein S, Hofmann B, Gergs U Front Pharmacol. 2022; 12:732842.

PMID: 34987383 PMC: 8720924. DOI: 10.3389/fphar.2021.732842.

Cardiovascular effects of the novel histamine H2 receptor agonist amthamine: interaction with the adrenergic system.

Coruzzi G, Gambarelli E, Bertaccini G, Timmerman H Naunyn Schmiedebergs Arch Pharmacol. 1996; 353(4):417-22.

PMID: 8935708 DOI: 10.1007/BF00261438.

Presynaptic histamine H2 receptors modulate the sympathetic nerve transmission in the isolated rat vas deferens; no role for H3-receptors.

Poli E, Todorov S, Pozzoli C, Bertaccini G Agents Actions. 1994; 42(3-4):95-100.

PMID: 7879708 DOI: 10.1007/BF01983472.

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