|Systematic (IUPAC) name|
|Mol. mass||453.498 g/mol|
GW-501,516 (also known as GW1516 or GSK-516) is a drug developed by GlaxoSmithKline, which acts as a PPARδ modulator. It activates AMP-activated protein kinase and stimulates glucose uptake in skeletal muscle tissue, and has been demonstrated to reverse metabolic abnormalities in obese men with pre-diabetic metabolic syndrome, most likely by stimulating fatty acid oxidation. It has been proposed as a potential treatment for obesity and related conditions, especially when used in conjunction with a synergistic compound AICAR, as the combination has been shown to significantly increase exercise endurance in animal studies.
Concerns were raised prior to the 2008 Beijing Olympics that GW-501,516 or the GW-501,516 / AICAR combination could be used by athletes as a performance enhancing drug which was not currently controlled by regulations or detected by standard tests. One of the main researchers from the study on enhanced endurance consequently developed a urine test to detect the drug, and made it available to the International Olympic Committee. The World Anti-Doping Agency has also begun work on a test for the two drugs, and they have been added to the prohibited list from 2009 onwards.
- ↑ Sznaidman ML, Haffner CD, Maloney PR, Fivush A, Chao E, Goreham D, Sierra ML, LeGrumelec C, Xu HE, Montana VG, Lambert MH, Willson TM, Oliver WR Jr, Sternbach DD (May 2003). [Expression error: Missing operand for > "Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity"]. Bioorg. Med. Chem. Lett. 13 (9): 1517–21. doi:10.1016/S0960-894X(03)00207-5. PMID 12699745.
- ↑ Dimopoulos N, Watson M, Green C, Hundal HS (October 2007). [Expression error: Missing operand for > "The PPARdelta agonist, GW501516, promotes fatty acid oxidation but has no direct effect on glucose utilisation or insulin sensitivity in rat L6 skeletal muscle cells"]. FEBS Lett. 581 (24): 4743–8. doi:10.1016/j.febslet.2007.08.072. PMID 17869249.
- ↑ Krämer DK, Al-Khalili L, Guigas B, Leng Y, Garcia-Roves PM, Krook A (July 2007). [Expression error: Missing operand for > "Role of AMP kinase and PPARdelta in the regulation of lipid and glucose metabolism in human skeletal muscle"]. J. Biol. Chem. 282 (27): 19313–20. doi:10.1074/jbc.M702329200. PMID 17500064.
- ↑ Risérus U, Sprecher D, Johnson T, Olson E, Hirschberg S, Liu A, Fang Z, Hegde P, Richards D, Sarov-Blat L, Strum JC, Basu S, Cheeseman J, Fielding BA, Humphreys SM, Danoff T, Moore NR, Murgatroyd P, O'Rahilly S, Sutton P, Willson T, Hassall D, Frayn KN, Karpe F (February 2008). [Expression error: Missing operand for > "Activation of peroxisome proliferator-activated receptor (PPAR)delta promotes reversal of multiple metabolic abnormalities, reduces oxidative stress, and increases fatty acid oxidation in moderately obese men"]. Diabetes 57 (2): 332–9. doi:10.2337/db07-1318. PMID 18024853.
- ↑ Barish GD, Narkar VA, Evans RM (March 2006). [Expression error: Missing operand for > "PPAR delta: a dagger in the heart of the metabolic syndrome"]. J. Clin. Invest. 116 (3): 590–7. doi:10.1172/JCI27955. PMID 16511591.
- ↑ Narkar VA, Downes M, Yu RT, Embler E, Wang Y-X, Banayo E, Mihaylova MM, Nelson MC, Zou Y, Juguilon H, Kang H, Shaw RJ,2 Evans RM (August 2008). "AMPK and PPARδ Agonists Are Exercise Mimetics" (PDF). Cell 134 (3): 1–11. doi:10.1016/j.cell.2008.06.051. PMID 18674809. PMC 2706130. http://download.cell.com/pdfs/0092-8674/PIIS0092867408008386.pdf.
- ↑ "Exercise In A Pill: Researchers Identify Drugs That Enhance Exercise Endurance". Science News. ScienceDaily. 2008-08-01. http://www.sciencedaily.com/releases/2008/07/080731135918.htm. Retrieved 2008-08-01.
- ↑ "AICAR and GW 1516 - The Exercise Pill". http://www.medical-weight-loss-guide.com/AICAR.html. Retrieved 2008-09-18.
- ↑ Laurance J, Rajan A (2008-08-01). "Warning to Beijing Olympics over pills that mimic exercise". Health News, Health & Wellbeing. The Independent. http://www.independent.co.uk/life-style/health-and-wellbeing/health-news/warning-to-beijing-olympics-over-pills-that-mimic-exercise-882608.html. Retrieved 2008-08-01.
- ↑ WADA 2009 Prohibited List
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