In vitro metabolic studies of novel selective androgen receptor modulators and their use for doping control analysis,Drug Testing and Analysis

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In vitro metabolic studies of novel selective androgen receptor modulators and their use for doping control analysis
Drug Testing and Analysis ( IF 2.6 ) Pub Date : 2021-08-19 , DOI: 10.1002/dta.3151
Katarzyna Kowalczyk _{1,

2} , Julio César Torres-Elguera ₁ , Anna Jarek ₂ , Anna Konopka ₁ , Dorota Kwiatkowska ₂ , Ewa Bulska ₁

Affiliation

Selective androgen receptor modulators were developed as a treatment of choice for diseases that are currently treated or symtomatically treated with steroidal androgens. The present study aimed to explore the metabolic pathways of four structurally unrelated SARMs, namely, PF-06260414, TFM-4AS-1, BMS-564929, and GSK 2881078, in terms of their potential toxicology or doping control analysis. Detected metabolism, mainly resulting from a single or multiple hydroxylations, methoxylation, demethylation, dehydrogenation, and glucuronidation, was considered as potential markers of intake of examined SARMs.

中文翻译：

新型选择性雄激素受体调节剂的体外代谢研究及其在兴奋剂控制分析中的应用

选择性雄激素受体调节剂被开发作为目前使用甾体雄激素治疗或对症治疗的疾病的首选治疗方法。本研究旨在探索四种结构不相关的 SARM 的代谢途径，即 PF-06260414、TFM-4AS-1、BMS-564929 和 GSK 2881078，就其潜在毒理学或兴奋剂控制分析而言。检测到的代谢，主要由单个或多个羟基化、甲氧基化、去甲基化、脱氢和葡萄糖醛酸化引起，被认为是摄入受检 SARM 的潜在标志物。

更新日期：2021-08-19

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