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Journal of Pharmacology And Experimental Therapeutics, Vol. 129, Issue 4, 394-399, 1960
Copyright © 1960 by American Society for Pharmacology and Experimental Therapeutics

REACTIVATION OF NEOSTIGMINE INHIBITED HUMAN PLASMA CHOLINESTERASE

F. F. Foldes 1, E. K. Zsigmond 1, E. G. Erdös 2, and J. A. Zwartz 3

1 Department of Anesthesiology, Mercy Hospital and Section on Anesthesia, Department of Surgery, University of Pittsburgh School of Medicine, Pittsburgh, Pennsylvania
2 Mellon Institute, Pittsburgh 13, Pennsylvania
3 Department of Biochemistry, University of Leiden, The Netherlands

The inhibitory effect of neostigmine on the hydrolysis of procaine and benzoylcholine by human plasma cholinesterase could be prevented and antagonized by tetraethylammonium, dihydrohydroxycodeinone, 14-hydroxydihydromorphinone and by tetraethylammonium, amphetamine and morphine, respectively.

The antagonistic effect was greater when the compounds were incubated with the enzyme before or together with neostigmine than when they were added to the system 20 minutes after neostigmine.

Tetramethylammonium, tetraethylammonium, tetra-n-propylammonium, tetra-n-butylammonium, morphine and 14-hydroxydihydromorphinone in concentrations which inhibited the hydrolysis of acetylcholine by plasma cholinesterase antagonized the inhibitory effect of neostigmine on this process.

The inhibitory effect of neostigmine and the compounds tested on the hydrolysis of acetylcholine by red cell cholinesterase was additive.

Submitted on December 7, 1959






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