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Journal of Pharmacology And Experimental Therapeutics, Vol. 120, Issue 3, 269-275, 1957
Copyright © 1957 by American Society for Pharmacology and Experimental Therapeutics

RELATION OF PERIPHERAL VASODILATOR ACTIVITY TO CHEMICAL STRUCTURE OF 1,2,3,4-TETRAHYDROISOQUINPLINE DERIVATIVES

Donald L. Cook 1, Coleta A. Lawler 1, and John W. Cusic 1

1 The Divisions of Biological Research and Chemical Research, G. D. Searle & Co., Chicago, Illinois

Peripheral vasodilator activity of a series of 1,2,3,4-tetrahydroisoquinoline (THIQ) derivatives was studied in the dog. The series included four chemical types: aliphatic, heterocydic, ester and ether. Activity was found in all types. The most active compound was a heterocycic derivative, N-beta-hydroxyethyl-THIQ-2-thenyl ether, which was forty-five times as active as the parent compound (THIQ). This compound was also found to possess potent adrenergic blocking activity.

Submitted on January 30, 1957






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