Androgen receptors in the brain: what are we measuring?

Androgen receptors in the brain: what are we measuring?
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大脑中的雄激素受体:我们测量什么?

DOI:
10.1210/edrv-4-2-171
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发表时间:
1983
期刊:
影响因子:
20.3
通讯作者:
P. Sheridan
P. Sheridan
中科院分区:
医学1区
文献类型:
--
作者:
P. Sheridan

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长期以来,人们都知道雄激素作用于大脑,改变行为和其他大脑功能。在过去,两种方法已被用来表征假定的受体介导这些行动。放射自显影已被用于映射和识别雄激素结合神经元。进行了结合研究,以定量和表征系统。由此产生的数据是不一致的,提出了一个新的模型来解决明显的差异。据推测,大脑中存在三类雄激素受体。一个受体优先结合睾酮,第二个优先结合DHT。这两种受体根据隔室的自由水含量在细胞核和细胞质之间处于平衡状态。这两种受体都能被类固醇激活并转化,从而集中在细胞核中。有人提出,第三个受体结合两种类固醇具有相同的相对亲和力。然而,这第三种受体只能被激活而不能被转化(即它不能集中在细胞核中)。建议的系统意味着睾酮作用于大脑中的一些离散的神经元群体,而DHT对中枢神经系统具有非常扩散的作用。
Androgen has long been known to act on the brain to modify behavior and other brain functions. In the past, two methods have been used to characterize the putative receptors which mediate these actions. Autoradiography has been used to map and identify androgen binding neurons. Binding studies have been conducted to quantify and characterize the system(s). The resultant data are discordant and a new model is proposed to resolve the apparent differences. It is proposed that there are three categories of receptors for androgen in the brain. One receptor preferentially binds testosterone and a second one preferentially binds DHT. Both of these receptors are in equilibrium between nucleus and cytoplasm according to the free water content of the compartments. Both of these receptors can be activated and transformed by steroid and thus concentrate in the nucleus. It is proposed that a third receptor binds both steroids with the same relative affinity. However, this third receptor can only be activated but not transformed (i.e. it does not concentrate in the nucleus). The proposed system implies that testosterone acts on a few discrete populations of neurons in the brain while DHT has a very diffuse action on the central nervous system.