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
来源：
EUROPEAN JOURNAL OF PHARMACOLOGY | 1995年 / 281卷 / 01期
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.
引用
收藏
页码：63 / 68
页数：6
相关论文
共 50 条
  • [1] CHARACTERIZATION OF A NOVEL NONPEPTIDE VASOPRESSIN V(1) RECEPTOR ANTAGONIST (OPC-21268) IN THE RAT
    BURRELL, LM
    PHILLIPS, PA
    STEPHENSON, J
    RISVANIS, J
    HUTCHINS, AM
    JOHNSTON, CI
    [J]. JOURNAL OF ENDOCRINOLOGY, 1993, 138 (02) : 259 - 266
  • [2] OPC-21268 - AN ORALLY EFFECTIVE, NONPEPTIDE VASOPRESSIN V-1 ANTAGONIST
    KOHMOTO, O
    SERIZAWA, T
    [J]. CARDIOVASCULAR DRUG REVIEWS, 1993, 11 (03): : 271 - 282
  • [3] OPC-21268, AN ORALLY EFFECTIVE, NONPEPTIDE VASOPRESSIN-VI RECEPTOR ANTAGONIST
    YAMAMURA, Y
    OGAWA, H
    CHIHARA, T
    KONDO, K
    ONOGAWA, T
    NAKAMURA, S
    MORI, T
    TOMINAGA, M
    YABUUCHI, Y
    [J]. SCIENCE, 1991, 252 (5005) : 572 - 574
  • [4] OPC-21268, an orally effective, nonpeptide vasopressin V1 receptor antagonist
    [J]. 1600, (252):
  • [5] OPC-21268 - A NONPEPTIDE ORALLY ACTIVE V1 VASOPRESSIN RECEPTOR ANTAGONIST
    BURRELL, LM
    PHILLIPS, PA
    RISVANIS, J
    STEPHENSON, J
    JOHNSTON, CI
    [J]. JOURNAL OF ENDOCRINOLOGY, 1992, 135 : P60 - P60
  • [6] EFFECTS OF A NONPEPTIDE VASOPRESSIN ANTAGONIST (OPC-21268) ON CYTOSOLIC CA2+ CONCENTRATION IN VASCULAR AND CARDIAC MYOCYTES
    MATSUI, H
    KOHMOTO, O
    HIRATA, Y
    SERIZAWA, T
    [J]. HYPERTENSION, 1992, 19 (06) : 730 - 733
  • [7] EFFECTS OF THE VASOPRESSIN ANTAGONIST OPC-21268 IN RAT AORTIC VASCULAR SMOOTH-MUSCLE CELLS
    LI, XM
    KRIBBEN, A
    WIEDER, ED
    TSAI, P
    SCHRIER, RW
    NEMENOFF, RA
    [J]. CLINICAL RESEARCH, 1993, 41 (01): : A79 - A79
  • [8] Effect of a nonpeptide vasopressin V1 antagonist(OPC-21268) on experimental accelerated focal glomerulosclerosis
    Kurihara, I
    Saito, T
    Obara, K
    Shoji, Y
    Hirai, M
    Imai, Y
    Abe, K
    [J]. NEPHRON, 1996, 73 (04): : 629 - 636
  • [9] Treatment of brain edema with a nonpeptide arginine vasopressin V1 receptor antagonist OPC-21268 in rats
    Bemana, I
    Nagao, S
    [J]. NEUROSURGERY, 1999, 44 (01) : 148 - 154
  • [10] PHARMACOKINETICS, SAFETY, AND PHARMACOLOGICAL EFFECTS OF OPC-21268, A NONPEPTIDE ORALLY ACTIVE VASOPRESSIN-V1 RECEPTOR ANTAGONIST, IN HUMANS
    OHNISHI, A
    KO, Y
    FUJIHARA, H
    MIYAMOTO, G
    OKADA, K
    ODOMI, M
    [J]. JOURNAL OF CLINICAL PHARMACOLOGY, 1993, 33 (03): : 230 - 238
12345