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The interaction of pancuronium and vecuronium with cardiac muscarinic receptors
Author(s) -
Sugai Y.,
Sugai K.,
Hirata T.,
Okuda C.,
Miyazaki M.
Publication year - 1987
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.1399-6576.1987.tb02555.x
Subject(s) - muscarinic acetylcholine receptor , medicine , receptor , acetylcholine receptor , pharmacology , muscarinic acetylcholine receptor m2 , inhibitory postsynaptic potential , in vitro , endocrinology , anesthesia , chemistry , biochemistry
The interaction of vecuronium, a monoquaternary analogue of pancuronium, with the cardiac muscarinic receptors in canine hearts was investigated in vitro by [ 3 H] QNB binding assay and compared with that of pancuronium. Both pancuronium and vecuronium, which are nicotinic antagonists of competitive types, inhibited the binding of [ 3 H] QNB to cardiac muscarinic receptors with values of IC 50 of 5.41 × 10 ‐7 mol/l and 3.97 × 10 ‐6 mol/l respectively. According to the Kd and Bmax values on the Scatchard plot, pancuronium, while not influencing the number of receptors, had a 3‐fold greater inhibitory effect than vecuronium on the affinity of the muscarinic receptors. The K 1 values of vecuronium and pancuronium showed that pancuronium had a 7.3‐fold greater affinity with the receptors than vecuronium. We concluded that vecuronium had a direct inhibitory action on the binding of [ 3 H] QNR to the canine heart muscarinic receptors, but this action was much weaker than pancuronium.