L-368,899 (hydrochloride)

非肽催产素受体拮抗剂（在使用离体人类子宫和大鼠子宫的放射性配体结合试验中，IC50s分别为8.9和26nM）；对催产素受体的选择性优于加压素V1a和V2受体（IC50s分别为370和570nM）；可降低催产素引起的离体大鼠子宫收缩（pA2=8.9）和原位大鼠子宫收缩（ED50=0.35mg/kg，iv）。A non-peptide oxytocin receptor antagonist (IC50s = 8.9 and 26 nM in radioligand binding assays using isolated human and rat uterus, respectively); selective for oxytocin receptors over vasopressin V1a and V2 receptors (IC50s = 370 and 570 nM, respectively); reduces oxytocin-induced contraction of isolated rat uterus (pA2 = 8.9) and in situ rat uterus (ED50 = 0.35 mg/kg, i.v.).