OPC 21268

OPC 21268 is a nonpeptide antagonist of vasopressin V1 receptors (IC50 = 0.4 µM in rat liver membranes). It is selective for V1 over V2 receptors (IC50 = >100 µM in kidney membranes). It is also selective for rat over human V1 receptors (Kis = 25 and 8,800 nM, respectively), which can be partially attributed to the alanine residue at position 337 of the rat sequence, instead of a glycine residue in the human sequence, with differences at positions 224, 310, and 324 also contributing. OPC 21268 (0.03-1 mg/kg, i.v.) inhibits pressor responses induced by arginine vasopressin (argipressin, Cay-24154) in pithed rats and arginine vasopressin-induced vasoconstriction in conscious rats (ID50 = 2 mg/kg). It induces hypotension in aged spontaneously hypertensive rats (SHRs) and stroke-prone SHRs when administered at a dose of 3 mg/kg.Formal Name: N-[3-[4-[[4-(3,4-dihydro-2-oxo-1(2H)-quinolinyl)-1-piperidinyl]carbonyl]phenoxy]propyl]-acetamide. CAS Number: 131631-89-5. Molecular Formula: C26H31N3O4. Formula Weight: 449.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 200µg/ml, Ethanol: slightly soluble. lambdamax: 249 nm. SMILES: O=C1CCC2=CC=CC=C2N1C3CCN(C(C4=CC=C(OCCCNC(C)=O)C=C4)=O)CC3. InChi Code: InChI=1S/C26H31N3O4/c1-19(30)27-15-4-18-33-23-10-7-21(8-11-23)26(32)28-16-13-22(14-17-28)29-24-6-3-2-5-20(24)9-12-25(29)31/h2-3,5-8,10-11,22H,4,9,12-18H2,1H3,(H,27,30). InChi Key: KSNUCNRMDYJBKT-UHFFFAOYSA-N.