VU0152100 (VU152100) is a potent, selective positive allosteric modulator of M4 mAChR with EC50 of 0.38 uM for rat M4.
VU0152100 potentiates the M4-mediated calcium response calcium response with maximal shifts of 70-fold with 10 uM in vitro assays.
VU0152100 inhibits behavioral and neurochemical effects of cocaine in vivo, also dose-dependently reverses amphetamine-induced hyperlocomotion in rats and wild-type mice, blocks amphetamine-induced disruption of the acquisition of contextual fear conditioning.
