X-Pertise Consulting, Mittelhausbergen, France.
Institut de medecine légale, Strasbourg, France.
Drug Test Anal. 2020 Jul;12(7):980-986. doi: 10.1002/dta.2802. Epub 2020 Apr 25.
GW501516, also known as GW-1516 or cardarine and endurobol, is a peroxisome proliferator-activated receptor delta (PPAR-δ) agonist. Activation of the receptor will increase fat-burning capacity and muscle production, as it changes the body's fuel preference from glucose to lipids. GW501516 has no therapeutic use, but can be abused for performance-enhancing purposes using the oral route, at dosages of 10 to 20 mg per day, for 6 to 8 weeks. Both athletes and amateurs can abuse GW501516 as the drug can be easily obtained via the Internet. Since January 2009, the list of prohibited substances and methods of doping as established by the World Anti-Doping Agency includes GW-501516, first as a gene doping substance and now in the S4.5 Metabolic modulators class. It is prohibited at all times. Using LC/MS-MS and confirmation by LC/HRM, after methanol incubation of 20 mg with ultrasound for 1 hour, GW501516 was identified in the hair of a male abuser at 32 and 22 pg/mg in 2 × 2 cm segments. The result is the first evidence that this compound with a carboxylic acid function is incorporated in human hair.
GW501516，也被称为 GW-1516 或卡达林和恩多布罗，是一种过氧化物酶体增殖物激活受体 δ（PPAR-δ）激动剂。激活该受体将增加脂肪燃烧能力和肌肉生成，因为它改变了身体从葡萄糖到脂质的燃料偏好。GW501516 没有治疗用途，但可以通过口服途径滥用，剂量为每天 10 至 20 毫克，持续 6 至 8 周，以提高运动表现。运动员和业余爱好者都可以滥用 GW501516，因为这种药物可以很容易地通过互联网获得。自 2009 年 1 月以来，世界反兴奋剂机构（World Anti-Doping Agency）确定的禁用物质和兴奋剂方法清单中包括 GW-501516，最初作为基因兴奋剂物质，现在属于 S4.5 代谢调节剂类。它一直被禁止使用。通过 LC/MS-MS 并通过 LC/HRM 确认，在对 20 毫克进行甲醇孵育 1 小时后，在一名男性滥用者的头发中用超声处理 2 × 2 厘米片段，GW501516 的含量为 32 和 22 pg/mg。这是第一个证据表明，这种具有羧酸功能的化合物已被纳入人类毛发中。
