多巴胺与妊娠兔子宫肌层中的α受体结合。

Dopamine binding to the alpha receptor in pregnant rabbit myometrium.

作者信息

Phillippe M, Barss V, Jackson K V, Valles L, Giannopoulos G

出版信息

Biochem Biophys Res Commun. 1987 Feb 13;142(3):947-52. doi: 10.1016/0006-291x(87)91505-1.

Abstract

This study evaluated in vitro binding of dopamine ligands to myometrial alpha adrenoceptors. With cell membranes from pregnant rabbits, receptor radioligand binding studies utilizing [3H] dihydroergocryptine +/- dopamine demonstrated receptor affinity (KD) = 0.75 +/- 0.10 nM (+/- SEM) and density (Bmax) = 533.2 +/- 45.2 fM/mg protein. Similar studies utilizing phentolamine or apomorphine gave essentially identical results. Competition binding studies demonstrated steriospecific butaclamol binding, along with significant binding of haloperidol, spiperone, apomorphine, and bromoergocryptine. These observations provide a mechanism for the observed uterotonic effects of dopamine.

摘要

本研究评估了多巴胺配体与子宫肌层α肾上腺素能受体的体外结合情况。利用孕兔的细胞膜，采用[3H]二氢麦角隐亭±多巴胺进行受体放射性配体结合研究，结果显示受体亲和力（KD）= 0.75±0.10 nM（±标准误），密度（Bmax）= 533.2±45.2 fM/mg蛋白。使用酚妥拉明或阿扑吗啡进行的类似研究得出了基本相同的结果。竞争结合研究表明存在立体特异性的布他拉莫结合，同时氟哌啶醇、螺哌隆、阿扑吗啡和溴麦角隐亭也有显著结合。这些观察结果为多巴胺所观察到的子宫收缩作用提供了一种机制。