COMPARATIVE CENTRAL DEPRESSANT ACTIONS OF SOME 5-PHENYL-5-ALKYL BARBITURIC ACIDS

¹ Division of Pharmacology and Experimental Therapeutics, University of California Medical School, San Francisco; Laboratories of Gordon A. Alles, Ph. D., Pasadena

1. Additional evidence, from studies of the comparative central actions of dialkyl, phenyl-alkyl and diphenyl barbituric acids, is presented to show that the mechanism which raises the convulsant threshold is different from the mechanism producing hypnosis as evidenced by ataxia and drowsiness.

2. Anticonvulsant activity of barbituric acid derivatives is intensified by the presence of one 5-phenyl group, diminished by the presence of a second 5-phenyl group, and maximal with the phenyl-butyl compound in the series of phenylalkyl barbituric acids.

3. Among the 5-phenyl-5-alkyl barbituric acids the widest range between anticonvulsant and hypnotic activities was found to be with 5-phenyl-5-butyl barbituric acid.

4. Of the ten dialkyl and phenyl-alkyl barbituric acids studied, 5-phenyl -5-butyl barbituric acid showed the most marked anticonvulsant activity at dose levels below the hypnotic dose range.

5. The hypnotic activities of the phenyl-alkyl barbituric acids are greatest with the compounds containing the smallest alkyl groups, and this type of central depressant activity decreases with increasing size of the alkyl group.

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