Bottari S P, Vokaer A, Kaivez E, Lescrainier J P, Vauquelin G P
J Clin Endocrinol Metab. 1983 Nov;57(5):937-41. doi: 10.1210/jcem-57-5-937.
Adrenergic receptors have been shown to be involved in uterine contractility. alpha-Adrenergic receptors cause uterine contraction, whereas beta-adrenergic receptors induce relaxation. In animals, myometrial alpha-adrenergic receptors are regulated by gonadal steroids. We have identified alpha 1- and alpha 2-adrenergic receptors in myometrial membranes using the newly developed radiolabeled specific antagonists [3H]prazosin and [3H]rauwolscine. This allowed characterization of both receptor subclasses individually and study of them in various physiological and pharmacological conditions in the human, i.e. during different phases of the menstrual cycle, in postmenopausal women, term pregnancy, and during depo-progestin (medroxyprogesterone acetate) therapy. The affinity and number of alpha 1-adrenergic receptors were unchanged in all conditions, whereas the number of alpha 2-adrenergic receptors increased concomitantly with circulating plasma estradiol levels. However, this latter effect was counteracted by progesterone. These results are an example of the heteroregulation of membrane receptors by estrogens and progesterone and throw new light on the regulatory mechanisms involved in uterine contractility in the human.
肾上腺素能受体已被证明与子宫收缩有关。α-肾上腺素能受体引起子宫收缩，而β-肾上腺素能受体则诱导子宫松弛。在动物中，子宫肌层的α-肾上腺素能受体受性腺类固醇调节。我们使用新开发的放射性标记特异性拮抗剂[3H]哌唑嗪和[3H]育亨宾，在子宫肌层膜中鉴定出了α1和α2肾上腺素能受体。这使得能够分别对两种受体亚型进行表征，并在人体的各种生理和药理条件下进行研究，即在月经周期的不同阶段、绝经后妇女、足月妊娠以及醋酸甲羟孕酮（Depo-Provera）治疗期间。在所有条件下，α1肾上腺素能受体的亲和力和数量均未改变，而α2肾上腺素能受体的数量则随着循环血浆雌二醇水平的升高而增加。然而，后一种效应被孕酮抵消。这些结果是雌激素和孕酮对膜受体进行异质性调节的一个例子，并为人类子宫收缩的调节机制提供了新的线索。
