受体的分子调控：β-雌二醇和孕酮与毒蕈碱系统的相互作用
Molecular regulation of receptors: interaction of beta-estradiol and progesterone with the muscarinic system.
作者信息
Sokolovsky M, Egozi Y, Avissar S
出版信息
Proc Natl Acad Sci U S A. 1981 Sep;78(9):5554-8. doi: 10.1073/pnas.78.9.5554.
Abstract
The effects of various substrates on the binding of agonists to muscarinic receptors were studied in the rat hypothalamus and adenohypophysis by competition experiments using the highly specific tritiated muscarinic antagonist N-methyl-4-piperidyl benzilate. It was found that agonist binding properties were affected only by the steroid sex hormones (beta-estradiol and progesterone), both of which resulted in a decrease in the proportion of high-affinity binding sites and a decrease in the dissociation constant. This suggests a link between the muscarinic system and the mechanism by which these steroids exert their gonadotropin-releasing effect on the adenohypophysis. We propose a model to depict the putative relationship between the muscarinic system and other receptor systems, including that which controls the steroid sex hormones.
摘要
利用高特异性的氚标记毒蕈碱拮抗剂N-甲基-4-哌啶基苯甲酸酯，通过竞争实验研究了各种底物对大鼠下丘脑和腺垂体中激动剂与毒蕈碱受体结合的影响。结果发现，激动剂的结合特性仅受甾体性激素（β-雌二醇和孕酮）影响，这两种激素均导致高亲和力结合位点比例降低以及解离常数减小。这表明毒蕈碱系统与这些甾体激素对腺垂体发挥促性腺激素释放作用的机制之间存在联系。我们提出一个模型来描述毒蕈碱系统与其他受体系统之间的假定关系，包括控制甾体性激素的受体系统。
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