CP-601927

CP-601927 is a synthetic small molecule developed by Pfizer as a selective partial agonist of the α4β2 nicotinic acetylcholine receptor. It is orally available and CNS‐penetrant. The compound was investigated for its potential to augment antidepressant therapy in patients with major depressive disorder and demonstrated antidepressant-like activity in animal models. However, clinical development was discontinued after a phase 2 trial due to insufficient efficacy at therapeutic doses[3][7][5]. The drug exhibits high affinity for the α4β2 nAChR subtype (Ki ≈ 21 nM) and much lower affinity for other subtypes such as α3β4[8].

Other names

1,5-Methano-1H-3-benzazepine, 2,3,4,5-tetrahydro-7-(trifluoromethyl)- (1R,5S)CP-601932CP601932CP 601932