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Molecular Pharmacology, Vol 2, 593-605, Copyright © 1966 by the American Society for Pharmacology and Experimental Therapeutics

The Reaction of Carbamates with Cholinesterase

R. D. O’BRIEN 1, B. D. HILTON 1, and L. GILMOUR 1

1 Section of Neurobiology and Behavior, Cornell University, Ithaca, New York

It has been shown that both complex formation and carbamylation are of major importance in the reaction between carbamates and cholinesterase. That carbamylation occurs has been shown by demonstration of leaving-group release as the reaction proceeds. Complex formation has been demonstrated by kinetic evidence. Affinity and carbamylation constants have been measured on 11 dimethylcarbamates and 10 methylcarbamates, and correlations with alkaline hydrolyzability have been sought.

Note:
ACKNOWLEDGMENTS This work was supported in part by grant GM 07804 of the Public Health Service. Carbaryl was kindly provided by Union Carbide Corporation; diisopropylphenyl methylcarbamate by Hooker Corporation; Isolan by Geigy Chemical Corporation and o-isopropoxyphenyl methylcarbamate and 4-methylthio-3,5-methylphenyl methylcarbamate by Chemagro Corporation. Miss Karen Johnson performed the pH-profile experiments.

Submitted on June 7, 1966




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Copyright © 1966 by the American Society for Pharmacology and Experimental Therapeutics