18,19-二羟基脱氧皮质酮和18-羟基-19-去甲脱氧皮质酮对醛固酮受体的亲和力及其盐皮质激素活性。

Affinity of 18,19-dihydroxydeoxycorticosterone and 18-hydroxy-19-nor-deoxycorticosterone to aldosterone receptor and their mineralocorticoid activity.

作者信息

Okamoto M, Momoi K, Yamano T, Nakamura M, Odaguchi K, Shimizu T, Okada T, Terasawa T

出版信息

Biochem Int. 1983 Dec;7(6):687-94.

Abstract

Affinity of 18,19-dihydroxydeoxycorticosterone (18,19-diOH-DOC) and 18-hydroxy-19-nor-deoxycorticosterone (18-OH-19-nor-DOC) to aldosterone receptor and their mineralocorticoid activity were evaluated. 18,19-DiOH-DOC (1 X 10(-6) M) did not show appreciable binding to the receptor and its relative potency as a mineralocorticoid was estimated to be less than 1/8,000 of that of deoxycorticosterone (DOC). 18-OH-19-nor-DOC bound to the receptor with an affinity similar to that of 18-hydroxydeoxycorticosterone (18-OH-DOC) or spironolactone. Its sodium retaining activity was 0.04 times as great as that of DOC and similar to that of 18-OH-DOC.

摘要

评估了18,19-二羟基脱氧皮质酮（18,19-diOH-DOC）和18-羟基-19-去甲脱氧皮质酮（18-OH-19-nor-DOC）对醛固酮受体的亲和力及其盐皮质激素活性。18,19-二羟基脱氧皮质酮（1×10⁻⁶ M）与受体未表现出明显结合，其作为盐皮质激素的相对效价估计小于脱氧皮质酮（DOC）的1/8000。18-OH-19-去甲脱氧皮质酮与受体的结合亲和力与18-羟基脱氧皮质酮（18-OH-DOC）或螺内酯相似。其钠潴留活性是DOC的0.04倍，与18-OH-DOC相似。