L371,257

L-371,257 is a potent antagonist of oxytocin-induced contractions of the rat uterus in vitro and in vivo and has significant oral bioavailability in rats.

Potent, high affinity human oxytocin (OT) receptor antagonist (K i = 4.6 nM) that displays > 800-fold selectivity over human arginine vasopressin receptors V 1a and V 2 . Antagonizes oxytocin-induced contractions in isolated rat uterine tissue (pA 2 = 8.44) and in anesthetised rats following intravenous and intraduodenal administration. Orally active.

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