EFFECTS OF THE NONPEPTIDE INHIBITOR OPC-21268 ON OXYTOCIN AND VASOPRESSIN STIMULATION OF RAT AND HUMAN MYOMETRIUM

被引:5
|
作者
ATKE, A
VILHARDT, H
HAUZEROVA, L
BARTH, T
ANDERSEN, LF
机构
[1] UNIV COPENHAGEN, DEPT MED PHYSIOL, DIV ENDOCRINOL & METAB, DK-2200 COPENHAGEN N, DENMARK
[2] ACAD SCI CZECH REPUBL, INST ORGAN CHEM & BIOCHEM, PRAGUE, CZECH REPUBLIC
[3] RIGSHOSP, DEPT OBSTET & GYNAECOL, COPENHAGEN, DENMARK
关键词
OXYTOCIN; VASOPRESSIN; MYOMETRIAL RECEPTOR; OPC-21268; VASOPRESSIN RECEPTOR ANTAGONIST;
D O I
10.1016/0014-2999(95)00225-A
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
OPC-21268 (1-[-1-[4-(3-acetylaminopropoxy)benzoyl]-piperidyl]-3,4-dihydro-2(1H)-quinolinone), a non-peptide vasopresssin V-1 receptor antagonist, inhibited oxytocin- and vasopressin-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. When incubated with purified plasma membranes from rat or human myometrial tissue, OPC-21268 inhibited the specific receptor binding of tritiated oxytocin and vasopressin in a dose-dependent and reversible way.
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页码:63 / 68
页数:6
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