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Muscarinic agonists and antagonists are used to treat a handful of gastrointestinal (GI) conditions associated with impaired salivary secretion or altered motility of GI smooth muscle. With regard to exocrine secretion, the major muscarinic receptor expressed in salivary, gastric, and pancreatic glands is the M₃ with a small contribution of the M₁ receptor. In GI smooth muscle, the major muscarinic receptors expressed are the M₂ and M₃ with the M₂ outnumbering the M₃ by a ratio of at least four to one. The antagonism of both smooth muscle contraction and exocrine secretion is usually consistent with an M₃ receptor mechanism despite the major presence of the M₂ receptor in smooth muscle. These results are consistent with the conditional role of the M₂ receptor in smooth muscle. That is, the contractile role of the M₂ receptor depends on that of the M₃ so that antagonism of the M₃ receptor eliminates the response of the M₂. The physiological roles of muscarinic receptors in the GI tract are consistent with their known signaling mechanisms. Some so-called tissue-selective M₃ antagonists may owe their selectivity to a highly potent interaction with a nonmuscarinic receptor target.


Frederick J Ehlert, Kirk J Pak, Michael T Griffin. Muscarinic agonists and antagonists: effects on gastrointestinal function. Handbook of experimental pharmacology. 2012(208):343-74

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PMID: 22222706

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