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介导卵巢卵泡壁收缩和舒张的组胺受体的特性研究

Characterization of histamine receptors mediating contraction and relaxation of the ovarian follicle wall.

作者信息

Schmidt G, Kannisto P, Owman C, Walles B

机构信息

Department of Histology, University of Lund, Sweden.

出版信息

Int J Fertil. 1987 Sep-Oct;32(5):399-406.

PMID:2889689
Abstract

Histamine is known to be present in ovarian tissue and may play a role in the ovulation process. The effect of histamine on the follicular smooth musculature was investigated using strips from the protruding part of mature bovine follicles, mounted in vitro for registration of isometric motor activity. Histamine contracted the preparation in a concentration-dependent manner. The response was inhibited competitively by the specific H1 receptor antagonist pyrilamine while the adrenergic alpha-receptor antagonist phentolamine had no clear-cut effect. A Schild plot revealed a pA2 value of 8.81, corresponding to a mean KB value (dissociation constant for receptor-antagonist complex) of (7.5 +/- 3.2) X 10(-9) M. After potassium depolarization and blockade of the contractile H1-receptors with pyrilamine, histamine induced a concentration-dependent relaxation of the follicle wall preparation. This response could be inhibited by the H2-receptor antagonist cimetidine (which also potentiated the contractile effect in the absence of pyrilamine). The pA2 value for the cimetidine-induced inhibition was 6.25, and KB was found to be (6.5 +/- 3.0) X 10(-7) M. The beta-receptor antagonist propranolol was effective only in very high concentrations. It is suggested that a possible role for histamine during follicle rupture is mediated via specific receptors in the follicular smooth musculature.

摘要

已知组胺存在于卵巢组织中,并且可能在排卵过程中发挥作用。使用来自成熟牛卵泡突出部分的条带研究了组胺对卵泡平滑肌组织的影响,将其体外安装以记录等长运动活性。组胺以浓度依赖性方式使制剂收缩。该反应被特异性H1受体拮抗剂吡苄明竞争性抑制,而肾上腺素能α受体拮抗剂酚妥拉明没有明显作用。Schild图显示pA2值为8.81,对应于平均KB值(受体 - 拮抗剂复合物的解离常数)为(7.5 +/- 3.2)×10(-9) M。在用吡苄明进行钾去极化和阻断收缩性H1受体后,组胺诱导卵泡壁制剂浓度依赖性松弛。该反应可被H2受体拮抗剂西咪替丁抑制(在没有吡苄明的情况下,西咪替丁也增强收缩作用)。西咪替丁诱导抑制的pA2值为6.25,发现KB为(6.5 +/- 3.0)×10(-7) M。β受体拮抗剂普萘洛尔仅在非常高的浓度下有效。提示组胺在卵泡破裂过程中的可能作用是通过卵泡平滑肌组织中的特异性受体介导的。

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