The inhibitory effect of gallamine on muscarinic receptors.

British Journal of Pharmacology
A L Clark, F Mitchelson

Abstract

1 The inhibitory effect of gallamine (1.1 muM-1.1 mM) on negative inotropic responses to acetylcholine (ACh) or carbachol (CCh) was investigated in isolated electrically stimulated atria of the guinea-pig. Gallamine caused parallel rightward shifts of the dose-response curves to the agonists, with no depression of the maximal response. 2 Gallamine (0.11 - 1.1 mM) produced a greater degree of antagnism towards CCh than towards ACh. With either agonist, the degree of antagonism produced by gallamine in high concentrations was less than that expected for a competitive antagonist.. 3 Similar findings were made when either negative inotropic or chronotropic responses were recorded in spontaneously beating guinea-pig atria. The inhibitory effect of gallamine against the negative inotropic response to cholinomimetics in electrically stimulated atria was not altered either in the presence of propranol (17 muM) or in atria obtained from guinea-pigs pretreated with diisopropylphosphorofluoridate (DEP) 12.5 mumol/kg, in divided doses over 3 days). 4 When ACh was used as the agonist, combination of gallamine with atropine (0.05-0.4 muM) produced dose-ratios which were less than expected for combination of two competitive antagonists. The s...Continue Reading

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