23/06/2014   What is GW1516 (or GW501516)






WADA had issued a warning regarding the improper use of a medicinal product by GlaxoSmithKline and withdrew from the trial because despite could cure obesity and muscle of guinea-pigs doubling their strength they were dying of cancer

 
WADA, the World Anti-Doping Agency in March 21, 2013 had issued a warning regarding a new drug doping that can exponentially increase the performance of the athlete who hired him, however, putting at serious risk his life.
 
It all started with a fairly terse statement posted on its website.
 
According to Wada in the black market would be possible to buy a drug called by his name of experimentation, GW501516. This would have been used by some of the athletes probably unaware of the fact that the chemical composition thereof may potentially put in jeopardy the life of the person who hired it.
This product is so dangerous that the same manufacturer has decided to abandon the project after the experimental results of pre-clinical testing. For this reason, its clinical use will never be accepted. Not only that, already some of the athletes has been tweaked to use that substance. To this have been put on alert for anti-doping agencies around the world.
 
 

(edn)

 

GW1516 is also known with following names and codes: GW501516 (the original project), GW501,516GSK 516,and Endurobol

 
 
 
(from wikipedia)

 

Mode of action

 

GW501516 is a selective agonist (activator) of the PPARδ receptor. It displays high affinity (Ki = 1 nM) and potency (EC50 = 1 nM) for PPARδ with > 1000 fold selectivity over PPARα and PPARγ.

In rats, binding of GW501516 to PPARδ recruits the coactivator PGC-1α. The PPARδ/coactivator complex in turn upregulates the expression of proteins involved in energy expenditure. 

Furthermore in rats treated with GW501516, increased fatty acid metabolism in skeletal muscle and protection against diet-induced obesity and type II diabetes was observed. In obese rhesus monkeys, GW501516 increased high-density lipoprotein (HDL) and lowered very-low-density lipoprotein (VLDL). The mechanism by which PPARδ agonists increase HDL appears to be a result of increased expression of the cholesterol transporter ABCA1.

 

Use in doping in sports

 

In a 2004 article in New Scientist Ronald M. Evans stated "I suspect that animals training with the drug will increase endurance more rapidly," and that "the potential for this to be abused by athletes is real." A spokeswoman for WADA said it would not be surprising if athletes were to take the substance if it was available. GSK told New Scientist that it had not investigated whether the compound had any effect on endurance.

Concerns were raised prior to the 2008 Beijing Olympics  that GW501516 could be used by athletes as an ergonenic performance enhancing drug that 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 Commitee. The WADA has also begun work on a test for GW501516 and other related PPARδ modulators, and they have been added to the prohibited list from 2009 onwards. GW501516 has been promoted on bodybuilding and athletics websites and has been available for some time on the grey market.  In 2011 it was reported to cost $1000 for 10 g.  WADA claim to have already detected its use. In 2012, WADA recategorised GW501516 from a gene doping compound to a "hormone and metabolic modulator".

In April 2013, Russian cyclicst Valery Kaykov was suspended by cycling's governing body UCI after having tested positive for GW501516. Kaykov's team Rusvelo sacked him immediately and in May 2013, Venezuelan Miguel Ubeto was provisionally suspended by the Lampre team.

 

 

 

 

 

 

GW1516 in Internet