GW501516
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GW501516
GW501516, also known as GW1516, GSK-516, and Endurobol, is a peroxisome proliferator-activated receptor delta (PPAR_) agonist that was initially developed in the 1990s as a potential treatment for metabolic diseases and cardiovascular diseases. It is known for its ability to enhance endurance and fat burning in animal studies, which has led to its use as a performance-enhancing drug in sports.
Mechanism of Action
GW501516 works by activating the PPAR_ receptor, which is a type of nuclear receptor that regulates the expression of genes involved in energy metabolism. When activated, PPAR_ increases the oxidation of fatty acids in muscle tissue, leading to improved endurance and reduced fat mass. This makes it an attractive compound for athletes looking to enhance their performance.
Development and Research
GW501516 was developed by GlaxoSmithKline in collaboration with Ligand Pharmaceuticals. Initial studies showed promising results in improving lipid profiles and increasing high-density lipoprotein (HDL) levels, which are beneficial for cardiovascular health. However, further research revealed that long-term use of GW501516 in animal models led to the development of cancer in several organs, which halted its development for therapeutic use.
Use in Sports
Despite its potential risks, GW501516 has been used by athletes as a performance-enhancing drug. It is banned by the World Anti-Doping Agency (WADA) and is classified as a prohibited substance under the category of hormone and metabolic modulators. Athletes caught using GW501516 face penalties, including suspension from competition.
Safety and Side Effects
The use of GW501516 is associated with significant health risks, primarily due to its potential to cause cancer. Other side effects may include liver damage, gastrointestinal issues, and muscle pain. Due to these risks, it is not approved for human use by any regulatory agency.
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