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孕酮拮抗剂奥那司酮可提高催产素诱导分娩的有效性,而不改变子宫肌层催产素受体的浓度。

The progesterone antagonist onapristone increases the effectiveness of oxytocin to produce delivery without changing the myometrial oxytocin receptor concentrations.

作者信息

Chwalisz K, Fahrenholz F, Hackenberg M, Garfield R, Elger W

机构信息

Research Laboratories of Schering AG, Berlin, Germany.

出版信息

Am J Obstet Gynecol. 1991 Dec;165(6 Pt 1):1760-70. doi: 10.1016/0002-9378(91)90030-u.

DOI:10.1016/0002-9378(91)90030-u
PMID:1661070
Abstract

The progesterone antagonist onapristone was used in guinea pigs during late pregnancy (43 +/- 2 days after coitus) and before term (day 61 after coitus) to investigate the role of progesterone on uterine reactivity to exogenous oxytocin, concentration of oxytocin receptors, and gap junctions in the myometrium. Onapristone priming increased the ability of oxytocin to induce delivery during late pregnancy and before term by factors of greater than or equal to 30 and approximately 10, respectively. The intrauterine pressure recording on day 43 after coitus revealed phasic, laborlike contractions in response to oxytocin in onapristone-treated animals, in contrast to tonic reactions in controls. The increase in the oxytocin response in onapristone-treated animals was not associated with an increase in myometrial oxytocin receptor concentrations either during late pregnancy or before term. By contrast, treatment with onapristone significantly decreased the input resistance of myometrial cells in guinea pigs in late pregnancy (43 +/- 1 day after coitus) to the level of animals at term. This was associated with a marked increase in myometrial gap junctions stained with antibodies against connexin 43. These results indicate that progesterone may control myometrial reactivity to oxytocin in pregnant guinea pigs by effects on postreceptor events mainly by suppressing the gap junctions.

摘要

在豚鼠妊娠晚期(交配后43±2天)和足月前(交配后第61天)使用孕酮拮抗剂奥那司酮,以研究孕酮对子宫对外源性催产素的反应性、催产素受体浓度及子宫肌层缝隙连接的作用。奥那司酮预处理分别使妊娠晚期和足月前催产素诱导分娩的能力提高了大于或等于30倍和约10倍。交配后第43天的子宫内压力记录显示,与对照组的强直性反应相反,奥那司酮处理的动物对催产素产生了阶段性的、类似分娩的收缩。奥那司酮处理的动物对催产素反应的增加在妊娠晚期或足月前均与子宫肌层催产素受体浓度的增加无关。相比之下,奥那司酮处理显著降低了妊娠晚期(交配后43±1天)豚鼠子宫肌层细胞的输入电阻,使其降至足月动物的水平。这与用抗连接蛋白43抗体染色的子宫肌层缝隙连接显著增加有关。这些结果表明,孕酮可能主要通过抑制缝隙连接,对受体后事件产生影响,从而控制妊娠豚鼠子宫肌层对催产素的反应性。

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1
The progesterone antagonist onapristone increases the effectiveness of oxytocin to produce delivery without changing the myometrial oxytocin receptor concentrations.孕酮拮抗剂奥那司酮可提高催产素诱导分娩的有效性,而不改变子宫肌层催产素受体的浓度。
Am J Obstet Gynecol. 1991 Dec;165(6 Pt 1):1760-70. doi: 10.1016/0002-9378(91)90030-u.
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The use of progesterone antagonists for cervical ripening and as an adjunct to labour and delivery.孕激素拮抗剂在宫颈成熟以及引产和分娩辅助中的应用。
Hum Reprod. 1994 Jun;9 Suppl 1:131-61. doi: 10.1093/humrep/9.suppl_1.131.
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Endometrial and myometrial effects of progesterone antagonists in pregnant guinea pigs.孕酮拮抗剂对妊娠豚鼠子宫内膜和肌层的影响。
Am J Obstet Gynecol. 1987 Oct;157(4 Pt 2):1065-74. doi: 10.1016/s0002-9378(87)80134-5.
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Rabbit myometrial oxytocin and alpha 2-adrenergic receptors are increased by estrogen but are differentially regulated by progesterone.雌激素可增加兔子宫肌层的催产素和α2-肾上腺素能受体,但它们受孕酮的调节存在差异。
Endocrinology. 1987 Mar;120(3):1184-9. doi: 10.1210/endo-120-3-1184.
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Myometrial oxytocin receptors levels in the pregnant rat are higher in distal than in proximal portions of the horn and correlate with disparate oxytocin responsive myometrial contractility in these segments.妊娠大鼠子宫肌层中催产素受体水平在子宫角远端高于近端,且与这些节段中子宫肌层对催产素反应性的不同收缩力相关。
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Effects of inactivation of oxytocin receptor and inhibition of prostaglandin synthesis on uterine oxytocin receptor and gap junction formation and labor in the rat.
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Inhibition of the estradiol-mediated endometrial gland formation by the antigestagen onapristone in rabbits: relationship to uterine estrogen receptors.抗孕激素奥那司酮对兔体内雌二醇介导的子宫内膜腺体形成的抑制作用:与子宫雌激素受体的关系
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Progesterone and mifepristone modify principally the responses of circular myometrium to oxytocin in preparturient rats: comparison with responses to acetylcholine and to calcium.孕酮和米非司酮主要改变分娩前大鼠子宫环形肌层对催产素的反应:与对乙酰胆碱和钙的反应比较。
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[The importance of oxytocin and prostaglandins to the mechanism of labor in humans].[催产素和前列腺素对人类分娩机制的重要性]
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Myometrial steroid concentration and oxytocin receptor density in parturient women at term.足月产妇子宫肌层类固醇浓度及催产素受体密度
Steroids. 1996 Jun;61(6):338-44. doi: 10.1016/0039-128x(96)00035-9.

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J Endocrinol Invest. 1994 Oct;17(9):739-56. doi: 10.1007/BF03347771.