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Journal of Pharmacology And Experimental Therapeutics, Vol. 125, Issue 1, 23-27, 1959
Copyright © 1959 by American Society for Pharmacology and Experimental Therapeutics

PHARMACOLOGY OF STEREOISOMERS OF 1-METHYL-5-(1-METHYL-2-PENTYNYL)-5-ALLYL-BARBITURIC ACID

William R. Gibson 1, Wilbur J. Doran 1, Wallace C. Wood 1, and Edward E. Swanson 1

1 The Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana

Pharmacological investigation of the 4 optically active forms and 2 racemic mixtures of 1-methyl-5-(1-methyl-2-pentynyl)-5-allyl barbitunric acid revealed important qualitative and quantitative differences. Rats, dogs and monkeys were used, and quantitative data collected from the 3 species correlated well. Twofold to threefold differences in anesthetic potency were found between enantiomorphs. Dogs and rats exhibited qualitative differences when different stereoisomers were administered, but monkeys did not. Desirable anesthesia with a satisfactory therapeutic index and low incidence of sideeffects was consistently produced by the agr-dl isomer (25398, methohexital, Lilly).

Submitted on July 21, 1958






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