曲洛司坦，一种甾体生物合成的口服活性抑制剂。

Trilostane, an orally active inhibitor of steroid biosynthesis.

作者信息

Potts G O, Creange J E, Hardomg H R, Schane H P

出版信息

Steroids. 1978 Sep;32(2):257-67. doi: 10.1016/0039-128x(78)90010-7.

Abstract

Trilostane is a competitive inhibitor of 3beta-hydroxysteroid dehydrogenase. In vitro, the drug inhibits conversion of pregnenolone to progesterone but does not alter conversion of cholesterol to pregnenolone nor progesterone to corticoid hormones. When given orally to rats, trilostane inhibits corticosterone and aldosterone production and elevates circulating levels of pregnenolone at doses lower than those that produce adrenal hypertrophy or inhibit gonadal steroidogenesis.

摘要

曲洛司坦是3β-羟基类固醇脱氢酶的竞争性抑制剂。在体外，该药物可抑制孕烯醇酮向孕酮的转化，但不会改变胆固醇向孕烯醇酮的转化，也不会改变孕酮向皮质激素的转化。给大鼠口服曲洛司坦时，在低于产生肾上腺肥大或抑制性腺类固醇生成的剂量下，它会抑制皮质酮和醛固酮的产生，并提高循环中的孕烯醇酮水平。