Conivaptan (hydrochloride)

Conivaptan is an antagonist of the arginine vasopressin (AVP) receptors V1A and V2 (Kis = 0.48 and 3.04 nM for rat liver V1A and kidney V2, respectively). It also competitively inhibits oxytocin binding to rat uterine oxytocin receptors (Ki = 44 nM) but has no effect on AVP binding to anterior pituitary V1B receptors at concentrations up to 100 µM in a radioligand binding assay. Conivaptan suppresses AVP-induced increases in intracellular calcium in vascular smooth muscle cells (VSMCs) in vitro and the pressor response in pithed rats. Conivaptan (0.01-0.3 mg/kg, i.v.) increases urine output and decreases urine osmolality in dehydrated conscious rats in a dose-dependent manner. It also reduces brain edema and blood-brain barrier disruption in a mouse experimental stroke model.Formal Name: N-[4-[(4,5-dihydro-2-methylimidazo[4,5-d][1]benzazepin-6(1H)-yl)carbonyl]phenyl]-[1,1'-biphenyl]-2-carboxamide, monohydrochloride. CAS Number: 168626-94-6. Synonyms: YM-087. Molecular Formula: C32H26N4O2 . HCl. Formula Weight: 535.0. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Slightly Soluble, Methanol: Slightly Soluble. SMILES: O=C(NC1=CC=C(C(N2CCC(N=C(C)N3)=C3C4=C2C=CC=C4)=O)C=C1)C(C=CC=C5)=C5C6=CC=CC=C6.Cl. InChi Code: InChI=1S/C32H26N4O2.ClH/c1-21-33-28-19-20-36(29-14-8-7-13-27(29)30(28)34-21)32(38)23-15-17-24(18-16-23)35-31(37)26-12-6-5-11-25(26)22-9-3-2-4-10-22,/h2-18H,19-20H2,1H3,(H,33,34)(H,35,37),1H. InChi Key: BTYHAFSDANBVMJ-UHFFFAOYSA-N.