M4 mAChR Modulator-2

Description

M4 mAChR Modulator-2 is an orally active, selective, brain-penetrant positive allosteric modulator PAM of the M4 muscarinic acetylcholine receptor M4 mAChR EC50 = 513 nM . M4 mAChR Modulator-2 exhibits high target selectivity, showing negligible affinity and low inhibition rates for non-target receptors D1R/D2R/D3R, 5-HT subtypes, ?/?/? opioid receptors, H1, M1/M2 while specifically binding to M4 mAChR with a Ki of 377 nM and an inhibition rate of 62.8 %. M4 mAChR Modulator-2 reverses Dizocilpine MK-801 HY-15084B -induced hyperlocomotion in mice. M4 mAChR Modulator-2 can be used for the study of schizophrenia