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Journal of Pharmacology And Experimental Therapeutics, Vol. 135, Issue 1, 128-133, 1962
Copyright © 1962 by American Society for Pharmacology and Experimental Therapeutics

THE N-DEMETHYLATION OF BUTYNAMINE

Robert E. McMahon 1 and Nelson R. Easton 1

1 Division of Organic Chemistry, Lilly Research Laboratories, Indianapolis, Indiana

Butynamine (3 - methyl - 3 - [N - t - butyl- methylamino]-butyne-1), a hypotensive amine, is N-demethylated by the microsomal enzymes of rat liver. The product of the demethylation reaction is des-N-methyl butynamine which in itself has hypotensive activity of short duration. The implication of the observation that butynamine, a highly hindered aliphatic amine, is a suitable substrate for the microsomal enzyme system is discussed. N-demethylation is the main in vivo metabolic pathway in the rat and in humans.

Submitted on June 28, 1961






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Copyright © 1962 by the American Society for Pharmacology and Experimental Therapeutics.