Estra‐4,9‐diene‐3,17‐dione (dienedione) is an anabolic‐androgenic steroid (AAS) available on the market as a dietary supplement for bodybuilding. It is prohibited in both human and equine sports due to its potential performance‐enhancing effect. With the rare presence of the 4,9‐diene configuration in endogenous steroids, dienedione has been considered as a synthetic AAS. Nevertheless, the reoccurring detection of dienedione in entire male horse urine samples led to the investigation of its possible endogenous nature in horses, and its endogenous nature in entire male horses has been recently confirmed and reported by the authors' laboratory. While dienedione is not detected in castrated horses (geldings), it is essential to study its elimination and identify its metabolites for its effective control. To study the elimination and biotransformation of dienedione, administration experiments were performed by giving three castrated horses (geldings) each single oral dose of 1500 mg of dienedione powder for seven consecutive days. The postulated in vivo metabolites included 17‐hydroxyestra‐4,9‐dien‐3‐one (M1a and M1b), hydroxylated dienedione (M2a, M2b, M3a, M3b, M4, M5) and hydroxylated M1 (M6a, M6b, M7a, M7b, M8a and M8b), formed from hydroxylation and reduction of dienedione. To control the misuse of dienedione in geldings, M3a and M3b are the potential targets that gave the longest detection time, which could be detected for up to 2–5 days in urine and 0.4–4 days in plasma.

中文翻译：

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马中雌激素-4,9-二烯-3,17-二酮的兴奋剂控制


Estra-4,9-二烯-3,17-二酮（二烯二酮）是一种合成代谢雄激素类固醇 (AAS)，在市场上可作为健美膳食补充剂。由于其潜在的提高成绩的作用，它在人类和马术运动中都是被禁止的。由于内源性类固醇中很少存在 4,9-二烯构型，二烯二酮被认为是一种合成 AAS。然而，在整个雄性马尿液样本中重复检测到二烯二酮导致了对其在马中可能的内源性的研究，并且其在整个雄性马中的内源性最近已被作者的实验室证实和报告。虽然在阉割的马（骟马）中未检测到二烯二酮，但有必要研究其消除并鉴定其代谢物以有效控制其。为了研究二烯二酮的消除和生物转化，通过连续7天给三匹阉割的马（骟马）每次口服1500毫克二烯二酮粉末进行给药实验。假定的体内代谢物包括 17-羟基雌激素-4,9-二烯-3-酮（M1a 和 M1b）、羟基化二烯二酮（M2a、M2b、M3a、M3b、M4、M5）和羟基化 M1（M6a、M6b、M7a、 M7b、M8a 和 M8b)，由二烯二酮的羟基化和还原形成。为了控制二烯二酮在骟马中​​的滥用，M3a和M3b是检测时间最长的潜在目标，在尿液中可检测到长达2-5天，在血浆中可检测到0.4-4天。