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Journal of Pharmacology And Experimental Therapeutics, Vol. 107, Issue 4, 459-463, 1953
Copyright © 1953 by American Society for Pharmacology and Experimental Therapeutics

PHARMACOLOGY OF VINYL ETHYNYL CARBINOLS—A NEW CLASS OF CENTRAL NERVOUS SYSTEM DEPRESSANTS

S. Y. P'An 1, J. F. Gardocki 1, M. Harfenist 1, and A. Bavley 1

1 The Research Laboratories, Chas. Pfizer & Co., Inc., Brooklyn, New York

1. Two vinyl ethynyl carbinols, 3-methylpent-4-en-1-yn-3-ol (compound II) an intermediate in commercial synthesis of Vitamin A, and its homologue, 3-ethyl-pent-4-en-1-yn-3-ol (compound III) were both found to be effective orally and parenterally as hypnotics in experimental animals.

2. Compounds II and III possess anticonvulsant activity against pentylene-tetrazole seizure in mice, with protective indices of 2.2 and 1.1, respectively.

3. Daily intramuscular injections of as high as 212 mgm. of compound II per kgm. body weight for fourteen days were well tolerated by rats.

4. Daily oral administration of as much as 265 mgm. of compound II for 28 days was tolerated by dogs without deleterious effects on liver and kidney functions or blood pictures.

Submitted on November 11, 1952






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Copyright © 1953 by the American Society for Pharmacology and Experimental Therapeutics.