Effects of YM471, a nonpetide AVP V_1A and V_2 receptor antagonist, on human AVP receptor subtype expressed in CHO cells and oxytocin receptors in human uterine smooth muscle cells

摘要

YM471, (Z)-4'-{4,4-difluoro-5-[2-(4-dimethylaminopiperidino)-2-oxoethylidene]-2-oxoethylidene[2,3,4,5-tetrahy- dro-1H-1-benzoazepine-1-carbonyl}-2-phenylbenzanilide monohydrochloride, is a newly synthesized potent vasopressin(AVP)receptor antagonist. Its effects on binding to and signal transduction by cloned human AVP receptors(V_1A, V_1B and V_2)stably expressed in Chinese hamster ovary(CHO) cells, and oxytocin receptors in human uterine smooth muscle cells(USMC)were studied. YM471 potently inhibited specific[~3H]-AVP binding to V_1A and V_2 receptors with K_i values of 0.62 nM and 1.19 nM respectively.