A. Atke et al., EFFECTS OF THE NONPEPTIDE INHIBITOR OPC-21268 ON OXYTOCIN AND VASOPRESSIN STIMULATION OF RAT AND HUMAN MYOMETRIUM, European journal of pharmacology, 281(1), 1995, pp. 63-68
OPC-21268 enzoyl]-piperidyl]-3,4-dihydro-2(1H)-quinolinone), a non-pep
tide vasopresssin V-1 receptor antagonist, inhibited oxytocin- and vas
opressin-induced contractions of myometrial strips from rats and from
full-term pregnant women. Administered intravenously in rats the drug
also inhibited uterine contractions caused by infusion of oxytocin. Wh
en incubated with purified plasma membranes from rat or human myometri
al tissue, OPC-21268 inhibited the specific receptor binding of tritia
ted oxytocin and vasopressin in a dose-dependent and reversible way.