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Journal of Pharmacology And Experimental Therapeutics, Vol. 121, Issue 1, 113-118, 1957
Copyright © 1957 by American Society for Pharmacology and Experimental Therapeutics


SOME PHARMACOLOGIC PROPERTIES OF A NEW SERIES OF CHOLINESTERASE INHIBITORS

W. J. Fleming 1, J. P. Long 1, R. J. Wulf 1, and R. M. Featherstone 1

1 Department of Pharmacology, College of Medicine, State University of Iowa, Iowa City

The anticholinesterase activity of four bis agr, agr'-disubstituted-4 , 4'biacetanilids has been evaluated. The experimental procedures included intravenous toxicity, duration of action, in vitro cholinesterase inhibition, effects on dog blood pressure, d-tubocurarine antagonism, and acetylcholine potentiation on the isolated rabbit heart. The 2-methylpyridyl and 3-methylpyridyl disubstitution derivatives were found to be more active than neostigmine on a molar basis. Correlations of position isomerism on the heterocyclic quaternary cationic head of the molecule with anticholinesterase activity have been discussed.

Submitted on May 2, 1957







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Copyright © 1957 by the American Society for Pharmacology and Experimental Therapeutics.