M4 mAChR Modulator-2

M4mAChRModulator-2 is an orally active and selective positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (M4mAChR) capable of crossing the blood-brain barrier, with an EC50 of 513 nM. It demonstrates high target selectivity, showing minimal affinity and low inhibition rates for non-target receptors (D1R/D2R/D3R, 5-HT subtypes, κ/δ/μ opioid receptors, H1, M1/M2), while specifically binding to M4mAChR with a Ki of 377 nM and an inhibition rate of 62.8%. Additionally, M4mAChRModulator-2 can reverse the hyperlocomotion induced by Dizocilpine (MK-801) in mice and is applicable for schizophrenia research.