Key result
Methoctramine and himbacine potently antagonize cardiac muscarinic receptors, though methoctramine exhibits direct inotropic actions.
Population
Guinea-pig isolated trachea, oesophageal muscularis mucosae, paced left atria, and rat aortic preparations
Design
Preclinical
Authors
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May support preclinical tool selection; leaves open clinical translation of cardiac muscarinic antagonism.
Methoctramine and himbacine act as potent and selective antagonists for cardiac muscarinic receptors, though methoctramine also shows allosteric inhibitory and direct inotropic effects.
Eglen et al. (1988) studied this question. Methoctramine and himbacine was evaluated on Muscarinic receptor antagonism (pA2 / pKB values). Methoctramine and himbacine are potent and selective antagonists for cardiac muscarinic receptors, though methoctramine exhibits inhibitory allosteric properties and direct inotropic actions.
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