Iperoxo (iodide)

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. Croy, C.H., Schober, D.A., Xiao, H., et al. Characterization of the novel positive allosteric modulator, LY2119620, at the muscarinic M2 and M₄ receptors. Mol. Pharmacol. 86(1), 106-115 (2014).

2. Dallanoce, C., Conti, P., De Amici, M., et al. Synthesis and functional characterization of novel derivatives related to oxotremorine and oxotremorine-M. Bioorg. Med. Chem. 7(8), 1539-1547 (1999).

3. Barocelli, E., Ballabeni, V., Bertoni, S., et al. Evidence for specific analgesic activity of a muscarinic agonist selected among a new series of acetylenic derivatives. Life Sci. 68(15), 1775-1785 (2001).