Xanomeline oxalate is a functionally selective mAChR M1 agonist (EC50 values are 0.3, 5, 42, 52 and 92.5 nM at mAChR M1, mAChR M3, mAChR M5, mAChR M4 and mAChR M2 receptors, respectively). It exhibits a reversible and wash-resistant binding resulting in full agonist activity at mAChR M1, delayed wash-resistant partial agonist activity at mAChR M2 and delayed wash-resistant full agonist activity at mAChR M4.
Stanhope et al (2001) The muscarinic receptor agonist xanomeline has an antipsychotic-like profile in the rat. J.Exp.Pharmacol.Ther. 299 782. Jakubik et al (2008) Importance and prospects for design of selective muscarinic agonists. Physiol.Res. 57 S39. Heinrich et al (2009) Pharmacological comparison of muscarinic ligands: historical verus more recent muscarinic M1-preferring receptor agonists. Eur.J.Pharmacol. 605 53.