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Journal of Pharmacology And Experimental Therapeutics, Vol. 157, Issue 2, 356-362, 1967
Copyright © 1967 by American Society for Pharmacology and Experimental Therapeutics

STERIC ASPECTS OF ADRENERGIC DRUGS. VI. BETA ADRENERGIC EFFECTS OF EPHEDRINE ISOMERS

A. Tye 1, R. Baldesberger 1, J. B. Lapidus 1, and P. N. Patil 1

1 Division of Chemical Pharmacology, College of Pharmacy, The Ohio State University, Columbus, Ohio

The effects of the ephedrine isomers were studied in the isolated guinea-pig tracheal chain preparation (which is believed to contain only beta adrenergic receptors). Cumulative dose-response curves were determined in the presence of methacholine-induced tone. The relaxation produced by the isomers was converted into percentage values with maximal effect as produced by isoproterenol or papaverine considered as 100%. In the normal preparation the isomers showed no striking differences in potency, although L(+)- ephednine was the least potent. In preparations from reserpine-pretreated animals (5 mg/ kg i.p., 16-24 hr) the effects of the D(-) isomers were not reduced but the effects of the L(+) isomers were. In similar preparations propranolol reduced the effects of all isomers. The results indicate that in the guinea-pig trachea D(-)-ephedrine and D(-)-pseudo-ephedrine are essentially directly acting drugs, whereas L(+)-ephedrine and L(+)-pseudo-ephedrine possess an appreciable indirect component in their action and that all four isomers probably act at beta adrenergic receptors.

Submitted on January 5, 1967
Accepted on March 16, 1967




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Copyright © 1967 by the American Society for Pharmacology and Experimental Therapeutics.