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Journal of Pharmacology And Experimental Therapeutics, Vol. 124, Issue 4, 347-349, 1958
Copyright © 1958 by American Society for Pharmacology and Experimental Therapeutics

COMPARATIVE PHARMACOLOGY OF CHLORPHENIRAMINE (CHLOR-TRIMETON) AND ITS OPTICAL ISOMERS

Franklin E. Roth 1 and William M. Govier 1

1 Department of Pharmacology, Scientific Research Division, Schering Corporation, Bloomfield, New Jersey

In vitro antihistamine studies on guinea pig gut have demonstrated that d-chlorpheniramine was approximately twice as potent as the racemic compound. The l-isomer had only about one-one hundredth the potency of dl-chlorpheniramine.

The oral protective action of the d-isomer against death induced by intravenous or aerosolized histamine in guinea pigs revealed an average potency of 1.8-2.4 times that observed for the racemic compound.

The general pharmacodynamics of the d-isomer in the anesthetized dog were similar to those of the dl-compound.

The central nervous system effect of all 3 drugs in mice and cats was manifested as general stimulation of approximately the same degree.

The acute toxicity of the d-isomer in guinea pigs, rats and mice was no greater than that of the dl-compound.

Oral subacute studies in the rat and monkey did not reveal any abnormalities which could be attributed to administration of either d-or dl-chlorpheniramine.

Submitted on July 28, 1958






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Copyright © 1958 by the American Society for Pharmacology and Experimental Therapeutics.