Why the study?
Does vecuronium have a weaker inhibitory action on cardiac muscarinic receptors compared to pancuronium in canine hearts?
Does vecuronium have a weaker inhibitory action on cardiac muscarinic receptors compared to pancuronium in canine hearts?
Vecuronium has a direct but much weaker inhibitory action on cardiac muscarinic receptors compared to pancuronium in canine hearts.
Vecuronium's weaker affinity may limit vagolytic effects in canine models; leaves open translation to human anesthesia.
The interaction of vecuronium, a monoquaternary analogue of pancuronium, with the cardiac muscarinic receptors in canine hearts was investigated in vitro by [3H] QNB binding assay and compared with that of pancuronium. Both pancuronium and vecuronium, which are nicotinic antagonists of competitive types, inhibited the binding of [3H] QNB to cardiac muscarinic receptors with values of IC50 of 5.41 X 10(-7) mol/l and 3.97 X 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 KI 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 [3H] QNB to the canine heart muscarinic receptors, but this action was much weaker than pancuronium.
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Sugai et al. (1987) studied this question.
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