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合成代谢雄激素类固醇的结构特征,有助于其与雄激素受体结合以及产生合成代谢和雄激素活性。甾体结构的应用修饰。

Structural characteristics of anabolic androgenic steroids contributing to binding to the androgen receptor and to their anabolic and androgenic activities. Applied modifications in the steroidal structure.

作者信息

Fragkaki A G, Angelis Y S, Koupparis M, Tsantili-Kakoulidou A, Kokotos G, Georgakopoulos C

机构信息

Doping Control Laboratory of Athens, Olympic Athletic Center of Athens Spyros Louis, Kifisias 37, 15123 Maroussi, Greece.

出版信息

Steroids. 2009 Feb;74(2):172-97. doi: 10.1016/j.steroids.2008.10.016. Epub 2008 Nov 5.

Abstract

Anabolic androgenic steroids (AAS) are synthetic derivatives of testosterone introduced for therapeutic purposes providing enhanced anabolic potency with reduced androgenic effects. Androgens mediate their action through their binding to the androgen receptor (AR) which is mainly expressed in androgen target tissues, such as the prostate, skeletal muscle, liver and central nervous system. This paper reviews some of the wide spectrum of testosterone and synthetic AAS structure modifications related to the intended enhancement in anabolic activity. The structural features of steroids necessary for effective binding to the AR and those which contribute to the stipulation of the androgenic and anabolic activities are also presented.

摘要

合成代谢雄激素类固醇(AAS)是睾酮的合成衍生物,最初用于治疗目的,具有增强的合成代谢效力和降低的雄激素作用。雄激素通过与主要在雄激素靶组织(如前列腺、骨骼肌、肝脏和中枢神经系统)中表达的雄激素受体(AR)结合来介导其作用。本文综述了一些与预期增强合成代谢活性相关的睾酮和合成AAS结构修饰的广泛内容。还介绍了与AR有效结合所必需的类固醇结构特征以及那些有助于规定雄激素和合成代谢活性的特征。

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