Description

• Selective positive allosteric modulator of M4 receptor (KB = 200 nM, α = 35); increases the potency of acetylcholine by 40-fold Exhibits no effect at hM1/3/5 receptors and a small effect at hM2 (KB = 1 μM α = 3.7) Potentiates other full and partial orthosteric agonists, including Carbachol, Oxotremorine-M, and McN-A343 Does not affect binding of antagonist NMS Active in vivo Antipsychotic
• α indicates the degree of allosteric enhancement when both orthosteric and allosteric sites are occupied (derived from the allosteric ternary complex model).