Christ M, Sippel K, Eisen C, Wehling M
Medizinische Klinik, Klinikum Innenstadt, University of Munich, Germany.
Mol Cell Endocrinol. 1994 Mar;99(2):R31-4. doi: 10.1016/0303-7207(94)90027-2.
Rapid, nongenomic in vitro effects of aldosterone on intracellular electrolytes, cell volume and the sodium-proton antiporter have been found in human mononuclear leukocytes (HML), as have related membrane receptors. In the present study, binding of 125I-labeled aldosterone to plasma membrane preparations from pig kidneys was studied, since nongenomic in vitro effects of aldosterone have also been described in cultured kidney cells. In this preparation, binding of aldosterone shares important features with both functional and binding data in HML. These include a very low apparent Ki of approximately 0.1 nM for aldosterone, a high turnover rate and binding selectivity for aldosterone and fludrocortisone. Desoxycorticosterone acetate and corticosterone show intermediate affinity, with apparent Ki values of approximately 1 and 100 nM, with hydrocortisone even less active. Thus binding of aldosterone to kidney plasma membranes is compatible with the major features of its nongenomic renal effects.
已在人单核白细胞（HML）中发现醛固酮对细胞内电解质、细胞体积和钠-质子反向转运体具有快速的非基因组体外效应，相关膜受体也已被发现。在本研究中，研究了125I标记的醛固酮与猪肾质膜制剂的结合，因为醛固酮的非基因组体外效应在培养的肾细胞中也有描述。在此制剂中，醛固酮的结合与HML中的功能和结合数据具有重要共同特征。这些特征包括醛固酮的表观Ki值极低，约为0.1 nM，周转率高，对醛固酮和氟氢可的松具有结合选择性。醋酸脱氧皮质酮和皮质酮表现出中等亲和力，表观Ki值约为1和100 nM，氢化可的松的活性更低。因此，醛固酮与肾质膜的结合与其非基因组肾效应的主要特征相符。
