Inhibition of the plasma cholinesterase variants by pancuronium bromide and some of its analogues

Clinica Chimica Acta; International Journal of Clinical Chemistry
M Whittaker, J J Britten

Abstract

Pancuronium bromide, a 3,17-diacetoxy-5 alpha-androstane, and three of its analogues, the 17-desoxy, the 3,17-dibutyryloxy and the 16-N-monoquaternary ammonium derivatives have been used as inhibitors of the usual and atypical plasma cholinesterase variants. In all cases the usual enzyme is more sensitive to inhibition by the substituted steroids than the dibucaine resistant enzyme. The relative affinities of the bis-quaternary ammonium compounds for either enzyme is in the order dibutyryloxy derivative > 17-desoxy derivative greater than or equal to pancuronium bromide. The monoquaternary compound has the least affinity of all the inhibitors for the usual enzyme but the greater affinity for the atypical enzyme. These observations show that the bis-quaternary compounds are very powerful differentiators of the variants. The monoquaternary derivative shows less differential inhibition, but provides additional evidence that the usual and dibucaine resistant variants differ in structure at or near their esteratic active site.

References

Nov 1, 1976·European Journal of Biochemistry·H MuenschA Yoshida
Sep 1, 1975·British Journal of Anaesthesia·J StovnerJ Holmboe
Feb 1, 1970·Anesthesiology·M Whittaker
Jul 1, 1955·Canadian Journal of Biochemistry and Physiology·W KALOW, H A LINDSAY
Jun 1, 1957·Canadian Journal of Biochemistry and Physiology·W KALOW, K GENEST

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Citations

Jun 29, 2006·Analytical and Bioanalytical Chemistry·Vesna P Stankov-JovanovićVioleta D Mitić
Mar 1, 1986·Anaesthesia·N RobsonM Whittaker
Dec 1, 1983·Acta Anaesthesiologica Scandinavica·R K MirakhurT D Lavery
Jan 1, 1986·Critical Reviews in Clinical Laboratory Sciences·R T Evans
Oct 1, 1996·Anesthesia and Analgesia·D W KimE R Johnson

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