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Iperoxo is an agonist of muscarinic acetylcholine receptors.1,2 It stimulates [35S]GTPγS binding to CHO cell membranes expressing human M2 muscarinic receptors and cell membranes expressing M4 muscarinic receptors (EC50s = 2.12 and 8.47 nM, respectively).1 Iperoxo induces M1-dependent inhibition of the twitch response in electrically-stimulated isolated rabbit vas deferens (pD2 = 9.87) and M3-mediated contraction of isolated guinea pig ileum (pD2 = 9.78).2 In vivo, iperoxo reduces formalin-induced paw licking and acetic acid-induced writhing in mice (ED50s = 0.004 and 0.001 mg/kg, respectively).3
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1. Characterization of the novel positive allosteric modulator, LY2119620, at the muscarinic M2 and M4 receptors. Mol. Pharmacol. 86(1), 106-115 (2014).
2. Synthesis and functional characterization of novel derivatives related to oxotremorine and oxotremorine-
3. Evidence for specific analgesic activity of a muscarinic agonist selected among a new series of acetylenic derivatives. Life Sci. 68(15), 1775-1785 (2001).