甘草次酸的盐皮质激素作用机制。

The mechanism of mineralocorticoid action of carbenoxolone.

作者信息

Armanini D, Karbowiak I, Krozowski Z, Funder J W, Adam W R

出版信息

Endocrinology. 1982 Nov;111(5):1683-6. doi: 10.1210/endo-111-5-1683.

Abstract

The principal side effects of the drug carbenoxolone (Biogastrone; 18 beta-glycyrrhetinic acid sodium hemisuccinate) are sodium retention, hypokalemic alkalosis, suppressed plasma renin, and hypertension. In previous animal studies, carbenoxolone appeared not to have intrinsic mineralocorticoid activity but, rather, to enhance aldosterone action by displacing it from nonspecific binding sites. We here report studies showing that carbenoxolone has demonstrable affinity for rat kidney mineralocorticoid receptors, intrinsic mineralocorticoid activity in the adrenalectomized rat at doses consistent with its receptor affinity, and, in addition, a powerful action of amplifying the electrolyte effects of near-maximal doses of aldosterone.

摘要

甘草次酸（生胃酮；18β-甘草次酸半琥珀酸钠）的主要副作用为钠潴留、低钾性碱中毒、血浆肾素受抑制及高血压。在以往的动物研究中，甘草次酸似乎并无内在的盐皮质激素活性，而是通过将醛固酮从非特异性结合位点置换出来，增强醛固酮的作用。我们在此报告的研究表明，甘草次酸对大鼠肾脏盐皮质激素受体具有可证实的亲和力，在去肾上腺大鼠中，其剂量与受体亲和力相符时具有内在盐皮质激素活性，此外，它还具有强大的作用，可增强接近最大剂量醛固酮的电解质效应。