VU0364572 (trifluoroacetate salt)

VU0364572 is a potent and selective agonist of the muscarinic acetylcholine receptor 1 (M1; EC50 = 0.2 mM compared to >10 mM for M2-M5).{37299} It induces concentration-dependent increases in Ca2+ mobilization and ERK1/2 phosphorylation in CHO cells transfected with the human M1 receptor (EC50s = 0.89 and 10 mM, respectively) with no effect on ?-arrestin recruitment. VU0364572 also improves hippocampal-dependent spatial learning and localization abilities and acquistion of contextual fear learning but cannot reverse amphetamine-induced hyperlocomotion in rats. This suggests therapeutic potential of VU0364572 for the treatment of Alzheimer's disease but not psychosis.{37300}