[Description]
VU6007477 is a novel M1 PAM. VU6007477 resulted in good rat M1 PAM potency (EC50 = 230 nM, 93% ACh max), minimal M1 agonist activity (agonist EC50 > 10 μM), good CNS penetration (rat braiplasma Kp = 0.28, Kp,uu = 0.32; mouse Kp = 0.16, Kp,uu = 0.18), and no cholinergic adverse events (AEs, e.g., seizures). |