Nelivaptan

Nelivaptan (SSR-149415) is a selective and orally active vasopressin V_1b receptor antagonist (K_i: 3.7 and 1.3 nM for native and recombinant rat V_1b receptors, respectively). Nelivaptan inhibits arginine vasopressin (AVP)-induced Ca²⁺ increase and corticotropin secretion. Nelivaptan can be used for research of stress, anxiety and depression^[1][2]. In Vitro:Nelivaptan (0.1-100 nM, 20 min) potently inhibits arginine vasopressin (AVP)-induced Ca² increase in CHO cells transfected with the human V_1b receptor^[1].
Nelivaptan (0.9-15 nM, 45 min) inhibits [³H]AVP binding in a competitive manner in CHO cells transfected with the human V_1b receptor^[1].
In Vivo:Nelivaptan (1-30 mg/kg; 30 min i.p. or 2 h p.o. before an exogenous AVP injection) inhibits exogenous AVP-induced increase in plasma corticotropin in Sprague-Dawley rats^[1].
Nelivaptan (1-10 mg/kg; p.o.; 1, 2, 3, 4, and 6 h before the AVP challenge) produces powerful dose-dependent inhibition of the corticotropin increase in response to exogenous AVP plus corticotropin-releasing factor (CRF) in Sprague-Dawley rats^[1].
Nelivaptan (1-10 mg/kg; i.p. 30 min or 60 min before test; or p.o. for 7 days) displays anxiolytic-like activity after acute and 7-day repeated administrations in male NMRI mice ^[1].
Nelivaptan (30 mg/kg; i.p.; daily for two weeks) retains efficacy in reducing both measured indices of depression-like behavior (learned helplessness and anhedonia), even when neurogenesis is blocked in male Wistar rats with chronic mild stress^[2].