Lazar G, Agarwal M K
Biochem Biophys Res Commun. 1986 Jan 14;134(1):261-5. doi: 10.1016/0006-291x(86)90556-5.
Kinetics of association--dissociation, competition and chromatography on two different resins, all revealed the presence of a new binding site which: specifically accepts 7-alpha-propyl spirolactone (3H-RU-26752), has little affinity for aldosterone, is present only in the target tissue (rat kidney), and is wanting in a non-target organ (liver). The presence of such sites could explain syndromes of mineralocorticoid excess where even trace amounts of an unusual aldosterone analogue, with little affinity for the classical mineralocorticoid receptor, can nevertheless produce hypertension through the intervention of an entirely new and abundant receptor system. This new molecule thus forms a novel tool to understand the nature and function of the soluble mineralocorticoid receptor in target organs.
结合-解离动力学、竞争以及在两种不同树脂上的色谱分析均显示存在一个新的结合位点，该位点：特异性结合7-α-丙基螺内酯（3H-RU-26752），对醛固酮亲和力低，仅存在于靶组织（大鼠肾脏）中，而非靶器官（肝脏）中则不存在。这些位点的存在可以解释盐皮质激素过多综合征，即即便微量的一种对经典盐皮质激素受体亲和力低的异常醛固酮类似物，仍可通过一个全新且丰富的受体系统的干预而导致高血压。因此，这种新分子构成了一种了解靶器官中可溶性盐皮质激素受体的性质和功能的新型工具。
