PT  - JOURNAL ARTICLE
AU  - John H. McNeill
AU  - Subhash C. Verma
TI  - BLOCKADE BY BURIMAMIDE OF THE EFFECTS OF HISTAMINE AND HISTAMINE ANALOGS ON CARDIAC CONTRACTILITY, PHOSPHORYLASE ACTIVATION AND CYCLIC ADENOSINE MONOPHOSPHATE
DP  - 1974 Jan 01
TA  - Journal of Pharmacology and Experimental Therapeutics
PG  - 180--188
VI  - 188
IP  - 1
4099  - http://jpet.aspetjournals.org/content/188/1/180.short
4100  - http://jpet.aspetjournals.org/content/188/1/180.full
SO  - J Pharmacol Exp Ther1974 Jan 01; 188
AB  - Histamine and two histamine analogs, betazole and 3-(β-aminoethyl)-1,2,4-triazole (TD), increased cardiac contractility, phosphorylase a levels and cyclic adenosine monophosphate (cyclic AMP) in the isolated perfused guinea-pig heart. The order of potency for the three compounds was histamine > 3-(β-aminoethyl)-1,2,4-triazole > betazole. A similar order of potency was previously noted for the ability of these compounds to increase the activity of cardiac adenylate cyclase. Cyclic AMP was found to increase prior to the increase in contractility or phosphorylase. Classical antihistamine drugs such as diphenhydramine or tripelennamine do not antagonize the cardiac effects of histamine. In the present study the new H2 receptor blocking agent, burimamide (0.5-16 x 10-5 M), was found to be a specific, competitive blocking agent of both the mechanical and biochemical effects of histamine and its analogs on the heart. The results indicate that the cardiac receptors for both the biochemical and mechanical effects of histamine are H2 receptors. The data also indicate that cyclic AMP is involved in the cardiac effects of histamine. © 1974 by The Williams & Wilkins Company