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The effects of a 16‐N‐homopiperidino analogue of vecuronium on neuromuscular transmission in anaesthetized cats, pigs, dogs and monkeys, and in isolated preparations
Author(s) -
MUIR A. W.,
ANDERSON K.,
MARSHALL R. J.,
BOOIJ L. H. D. J.,
CRUL J. F.,
PRIOR C.,
BOWMAN W. C.,
MARSHALL I. G.
Publication year - 1991
Publication title -
acta anaesthesiologica scandinavica
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.738
H-Index - 107
eISSN - 1399-6576
pISSN - 0001-5172
DOI - 10.1111/j.1399-6576.1991.tb03247.x
Subject(s) - medicine , neuromuscular transmission , cats , neostigmine , potency , anesthesia , depolarization , neuromuscular blocking agents , vecuronium bromide , pharmacology , chemistry , in vitro , biochemistry
Org 9991, a 16‐N‐homopiperidinium substituted vecuronium analogue, has been tested for neuromuscular blocking activity in anaesthetized cats, pigs, dogs and monkeys, and in isolated nerve‐muscle preparations. Org 9991 exhibited non‐depolarizing neuromuscular blocking activity of the competitive type, being reversible by neostigmine and showing no endplate channel blocking action in isolated preparations. In cats, 50% vagal block was observed at doses of Org 9991 approximately 10 times those producing 50% neuromuscular block; no ganglion block was seen at these doses. Effects on blood pressure or heart rate at 90% twitch blocking doses were either minor or absent. The potency and time course of action of Org 9991 remained similar in all four species: i. e. 90% block at ca 200–300 μg kg ‐1 ; onset time ca 1. 2–1. 9 min; duration 90% ca 4. 5–8. 9 min. This study suggests that 16–N‐homopiperidinium analogues of vecuronium may provide leads in the quest for a potent non‐depolarizing replacement for suxamethonium.