PMID: 40012Oct 1, 1979

Beta adrenoceptor blocking properties of MK-761

The Journal of Pharmacology and Experimental Therapeutics
C S SweetA Scriabine

Abstract

MK-761 is a new class of compound which has beta adrenoceptor antagonist and vasodilating properties in a single molecule. The compound has in vitro beta adrenoceptor blocking activity in the isolated cat heart papillary muscle and isolated rat atria. Unlike propranolol, it did not depress contactile force. Intrinsic sympathomimetic activity was not observed in vitro, (isolated cat papillary muscle, isolated atria) but the compound has some intrinsic sympathomimetric activity because it slightly increased heart rate in reserpinized rats. MK-761 was found to be approximately as potent as timolol and pindolol in blocking cardiac and vascular beta adrenergic receptors in anesthetized dogs. The drug was not, however, cardioselective. Oral beta adrenoceptor blocking activity was observed in rats at doses similar to those which decreased blood pressure.

Related Concepts

Myocardial Contraction
Pyridines
MK 761
Blood Vessel
Antagonist Muscle Action
Adrenergic beta-Agonists
Beta Adrenoceptor Activity
Pindolol
Vascular Diseases
V-Serp

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