PF-06764427

PF-06764427 (PF06764427) is a potent, selective M1 muscarinic acetylcholine receptor (mAChR) positive allosteric modulator with EC50 of 55 nM, has no measurable agonist or PAM activity at the M2-M5 receptors at 10 uM; induces a 212-fold shift in the ACh CRC at 10 uM in the PathHunter Arrβ2 assay; demonstrates robust potentiation of acetylcholine across the G-protein and Arrβ2 pathways, adequate brain availability, favorablepharmacokinetic properties and invivo efficacy in a mouse amphetamine-stimulated LMA model.

References 1. Moran SP, et al. Neuropsychopharmacology. 2018 Jul;43(8):1763-1771. 2. Rook JM, et al. ACS Chem Neurosci. 2018 May 8. doi: 10.1021/acschemneuro.8b00131. 3. Davoren JE, et al. Bioorg Med Chem Lett. 2016 Jan 15;26(2):650-655. View Related Products by Target mAChR