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Journal of Pharmacology And Experimental Therapeutics, Vol. 104, Issue 2, 122-134, 1952
Copyright © 1952 by American Society for Pharmacology and Experimental Therapeutics

HYDROLYSIS OF LOCAL ANESTHETICS BY HUMAN SERUM CHOLINESTERASE

Werner Kalow 1

1 Department of Pharmacology, University of Toronto, Toronto, Canada

1. The special features of ultraviolet spectrophotometry in its application to the study of esterase actions on local anesthetics and benzoylcholine were described.

2. Evidence for the identity of "procainesterase" and cholinesterase of human serum was presented. Acetylcholine (or benzoylcholine) and procaine (or other local anesthetic esters) can act as competitive inhibitors for the same enzyme. Although the hydrolysis of acetylcholine is about 400 times faster than that of procaine, the affinity of procaine for this esterase is about 220 times greater.

3. Kinetic data of esterase action on procaine were given.

4. Six local anesthetics other than procaine were investigated. Piperocaine was hydrolyzed faster, all other esters more slowly than procaine. The affinities between esterase and all local anesthetics were high, in the case of tetracaine about the same as physostigmine.

Submitted on September 19, 1951




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Copyright © 1952 by the American Society for Pharmacology and Experimental Therapeutics.