Corticoid receptors in rat brain: evidence for an aldosterone receptor.
Corticoid receptors in rat brain: evidence for an aldosterone receptor.
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大鼠大脑中的皮质激素受体：醛固酮受体的证据。
DOI：
10.1210/endo-98-3-676
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发表时间：
1976
期刊：
影响因子：
4.8
通讯作者：
Darrell D. Fanestil
中科院分区：
文献类型：
--
作者：
Norman S. Anderson;Darrell D. Fanestil
通过与[~3H]-醛固酮(~3H-A)的特异性结合，在去肾上腺大鼠脑胞浆中存在高亲和力和低亲和力的盐皮质激素结合大分子(受体)。根据对螺内酯SC-9420或非放射性A、DM和B的选择性，可将高亲和力的醛固酮部位与对[~3H]地塞米松(~3H-DM)或[~H]皮质酮(~H-B)有较高亲和力的部位区分开来。当放射性配体在20℃或37℃下孵育时，~3H-A与受体没有明显的结合，表明受体是耐热的。对~3H-A在200倍浓度范围内的结合数据的Scatchard分析表明，醛固酮有两个结合部位，高亲和力成分(A1)和低亲和力成分(A2)，其Kd约为1.5×10(-9)M和低亲和力成分(A2)，其Kd约为6.3×10(-8)M。以~3H-DM为放射性配基的类似研究表明，~3H-DM只有一个结合部位，Kd=6.2×10(-9)M。对醛固酮的选择性提示，这种激素在中枢神经内或通过中枢神经系统发挥作用的可能是肾外机制。
The existence of high and low affinity mineralocorticoid-binding macromolecules (receptors) has been demonstrated in vitro in cytosols derived from the adrenalectomized rat brain by the specific binding of [3H]aldosterone (3H-A). The high-affinity aldosterone sites can be distinguished from those sites which have a higher affinity for either [3H]dexamethasone (3H-DM) or [3H]corticosterone (3H-B) on the basis of selectivity for spirolactone SC-9420 or non-radioactive A, DM, and B. The binding of 3H-A to the receptors was maximal after 2 hours of incubation of 0-4C. No significant binding of 3H-A to the receptors could be demonstrated when incubations of the radioactive ligand were performed at either 20 or 37 C, indicating that the receptor is heat-liabile. Scatchard analysis of the 3H-A binding data over a 200-fold concentration range of 3H-A indicated that there are two binding sites for aldosterone, a high affinity component (a1) with a Kd approximately equal to 1.5 X 10(-9)M and a low-affinity component (a2) with a Kd approximately equal to 6.3 X 10(-8)M. A similar study using 3H-DM as the radioactive ligand demonstrated only one site for the 3H-DM binding with a Kd = 6.2 X 10(-9)M. The presence of specific aldosterone receptors in the brain with high affinity, limited capacity, and selectivity for aldosterone suggests a possible extra-renal mechanism of action of the hormone in or mediated through the CNS.