催产素和加压素拮抗剂受体结合,抑制对孤立的子宫肌层的影响孕妇早产和术语。

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Akerlund M, Bossmar T, Brouard R, Kostrzewska, Laudanski T, Lemancewicz, Serradeil-Le加C, Steinwall M

催产素和加压素拮抗剂受体结合,抑制对孤立的子宫肌层的影响孕妇早产和术语。

Br。Gynaecol。1999年10月,106(10):1047 - 53年。

PubMed ID

10519430 (在PubMed

]

文摘

目的:测试绑定亲和力和抑制性影响,子宫肌层的催产素和加压素拮抗剂对他们的治疗潜力。设计:受体结合研究转染细胞系。体外人类子宫肌层的收缩性的研究。设置:赛诺菲异国风味的研究实验必威国际app室,中心de图卢兹,法国和妇产科的部门,隆德大学医院,瑞典和比亚韦斯托克大学医院,波兰。参与者:九名女性早产和37通过剖腹产手术生在常规产科指征。干预措施:催产素的结合亲和力,精氨酸加压素,atosiban (1-deamino-2-D-Tyr(诗人)4-thr-8-om-oxytocin), SR 49059和SR 121463人类催产素和抗利尿激素受体测定的不同亚型。量效曲线与催产素和精氨酸加压素是从早产,记录在子宫肌层term-delivered妇女在控制实验和在2.5和10的SR 49059 nmol / L。此外,使用术语子宫肌层,SR 49059和SR 121463浓度的影响3、10、30和100 nmol / L反应EC50催产素和抗利尿激素的浓度进行比较。主要结果测量:受体结合亲和力。体外收缩效应及其抑制。 RESULTS: Oxytocin had a high affinity for the oxytocin receptor (K(i) in mean = 6.8 nmol/L) and bound, to some extent, to the vasopressin V1a receptor (K(i) = 34.9 nmol/L). Vasopressin displayed higher affinities for vasopressin V1a, V1b and V2 receptors (K(i) = 1.4, 0.8 and 4.2 nmol/L, respectively) than for the oxytocin receptor (K(i) = 48 nmol/L). Atosiban and SR 49059 both had a high affinity for the vasopressin V1a receptor (K(i) = 4.7 and 7.2 nmol/L, respectively, and a moderate one for the oxytocin receptor (K(i) = 397 and 340 nmol/L, respectively). SR 121463 exerted a predominant binding to the V2 receptor (K(i) = 3.0 nmol/L). In the concentration-response experiments levels of up to 10 nmol/L of SR 49059 had no influence on the effect of oxytocin on myometrium from women preterm and at term pregnancy. However, a concentration-dependent inhibition of the responses of both these type of tissues to vasopressin was seen. The effects of EC50 concentrations of oxytocin and vasopressin on term pregnant myometrium were markedly inhibited by 10 nmol/L and higher concentrations of SR 49059, the inhibition of the response to vasopressin being more pronounced than that of the oxytocin response. SR 121463 at maximal concentration only caused slight inhibitions of the oxytocin and vasopressin responses. CONCLUSIONS: Atosiban and SR 49059 both have moderate binding affinities for the human oxytocin receptor and high binding affinities for the vasopressin V1a one. We demonstrated that SR 49059 inhibits the response of term myometrium to oxytocin and that of both preterm and term myometrium to vasopressin. These observations suggest a therapeutic potential of SR 49059 in preterm labour. The vasopressin V2 receptor is apparently not involved to any significant degree in the activation of the pregnant human uterus.

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药物靶点

药物	目标	类	生物	药理作用	行动
Atosiban	催产素受体	蛋白质	人类	是的	拮抗剂	细节
Atosiban	后叶加压素V1a受体	蛋白质	人类	未知的	拮抗剂	细节
Atosiban	后叶加压素受体V1b	蛋白质	人类	未知的	拮抗剂	细节
Atosiban	后叶加压素V2受体	蛋白质	人类	未知的	拮抗剂	细节
Relcovaptan	催产素受体	蛋白质	人类	未知的	拮抗剂	细节
Relcovaptan	后叶加压素V1a受体	蛋白质	人类	未知的	拮抗剂	细节