L-371,257

A nonpeptide oxytocin receptor antagonist (Ki = 19 and 4.6 nM for the rat uterine and human uterine receptors, respectively), selective for oxytocin receptors over human AVP receptors V1A and -V2 (Kis = 3,200 and >10,000 nM for the human platelet and kidney receptors, respectively) and rat AVP receptor V2 (Ki = >10,000 nM for the rat kidney receptor) but also inhibits rat AVP receptor V1A (Ki = 3.7 nM for the rat liver receptor), inhibits spontaneous contractions in isolated human myometrial strips (IC50 = 71 pM), inhibits oxytocin-induced uterine contractions in rats (ED50 = 0.55 mg/kg). Formulation: A solid. InChI: InChI=1S/C28H33N3O6/c1-19(32)29-15-11-22(12-16-29)37-23-7-8-24(26(17-23)35-2)27(33)30-13-9-21(10-14-30)31-25-6-4-3-5-20(25)18-36-28(31)34/h3-8,17,21-22H,9-16,18H2,1-2H3. InChIKey: WDERJSQJYIJOPD-UHFFFAOYSA-N. SMILES: O=C1OCC2=C(N1C3CCN(CC3)C(C4=C(OC)C=C(C=C4)OC5CCN(CC5)C(C)=O)=O)C=CC=C2