VU0357017 (hydrochloride)

VU0357017 is an allosteric agonist of M1 muscarinic acetylcholine receptors (mAChRs; Ki = 9.91 µM in CHO cells).{40723} In vitro, it is selective for M1 over M2-M5 mAChRs (Kis = 21.4-50 µM in CHO cells). VU0357017 induces concentration-dependent increases in calcium mobilization and activates the ERK signaling pathway with EC50 values of 1.6 and 37 µM, respectively, in CHO cells expressing human recombinant M1 receptors.{37300} In vivo, VU0357017 crosses the blood-brain barrier and reverses scopolamine-induced deficits in contextual fear conditioning in rats when used at a dose of 10 mg/kg.{40724}