Xanomeline

Muscarinic receptors are G protein-coupled acetylcholine receptors that play diverse roles. Xanomeline (oxalate) is a potent agonist of muscarinic acetylcholine receptors (EC₅₀ values are 0.3, 92.5, 5, 52, and 42 nM for M₁, M₂, M₃, M₄, and M₅, respectively).¹ It has antipsychotic-like activities in rats and Cebus monkeys.^2,3 M₁ selective agonists, like Xanomeline (oxalate), enhance memory function and has utility in treating Alzheimer’s Disease.⁴

1.Heinrich, J.N., Butera, J.A., Carrick, T., et al.Pharmacological comparison of muscarinic ligands: Historical versus more recent muscarinic M1-preferring receptor agonistsEur. J. Pharmacol.605(1-3)53-56(2009) 2.Stanhope, K.J., Mirza, N.R., Dickerdike, M.J., et al.The muscarinic receptor agonist xanomeline has an antipsychotic-like profile in the ratJ. Pharmacol. Exp. Ther.299(2)782-792() 3.Andersen, M.B., Fink-Jensen, A., Peacock, L., et al.The muscarinic M1/M4 receptor agonist xanomeline exhibits antipsychotic-like activity in Cebus apella monkeysNeuropsychopharmacology28(6)1168-1175(2003) 4.Messer, W.S., Jr.The utility of muscarinic agonists in the treatment of Alzheimer's diseaseJ. Mol. Neurosci.19(1-2)187-193(2002)