GW501516 is a PPARδ receptor. It activates the same pathways activated through exercise, including PPARδ and AMP-activated protein kinase. It had been investigated as a potential treatment for obesity, diabetes, dyslipidemia and cardiovascular disease. GW501516 has a synergistic effect when combined with AICAR: the combination has been shown to significantly increase exercise endurance in animal studies more than either compound alone.
GW501516 could be used by athletes as an ergogenic 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 Committee.
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