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介导豚鼠子宫收缩的毒蕈碱受体亚型的特性分析。

Characterization of the muscarinic receptor subtype mediating contractions of the guinea-pig uterus.

作者信息

Eglen R M, Michel A D, Whiting R L

机构信息

Institute of Pharmacology, Syntex Research, Palo Alto, Ca 94303.

出版信息

Br J Pharmacol. 1989 Mar;96(3):497-9. doi: 10.1111/j.1476-5381.1989.tb11843.x.

Abstract

The muscarinic receptor present on the guinea-pig uterus has been characterized by use of both functional and radioligand binding studies. The contractile responses to carbachol were antagonized by atropine, pirenzepine, methoctramine and hexamethonium with pA2 values consistent with the presence of an M2 receptor (i.e. 9.5, 7.0, 8.0 and 3.7 respectively). In binding studies, pKi values were also observed for pirenzepine, methoctramine and AF-DX 116 which were consistent with the presence of a homogeneous M2 receptor population (i.e. 6.6, 7.9 and 7.1 respectively). The uterus therefore possesses M2 receptors through which a functional contractile response is mediated and in this respect it is clearly different from other smooth muscles. M2 receptors in the uterus mediate excitatory responses, an effect in contrast to their action in other tissues.

摘要

通过功能研究和放射性配体结合研究,对豚鼠子宫上存在的毒蕈碱受体进行了表征。卡巴胆碱引起的收缩反应被阿托品、哌仑西平、甲溴东莨菪碱和六甲铵拮抗,其pA2值与存在M2受体一致(即分别为9.5、7.0、8.0和3.7)。在结合研究中,还观察到哌仑西平、甲溴东莨菪碱和AF-DX 116的pKi值,这与存在同质的M2受体群体一致(即分别为6.6、7.9和7.1)。因此,子宫具有M2受体,通过该受体介导功能性收缩反应,在这方面它明显不同于其他平滑肌。子宫中的M2受体介导兴奋性反应,这一作用与其在其他组织中的作用相反。

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