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GW-501,516 (also known as GW1516 or GSK-516) is a drug developed by GlaxoSmithKline
GlaxoSmithKline

GlaxoSmithKline plc is a United Kingdom-based pharmaceutical industry, biological, and healthcare company. GSK is the world's second largest pharmaceutical company and a research-based company with a wide portfolio of pharmaceutical products covering anti-infectives, central nervous system, respiratory, gastro-intestinal/metabolic,...
, which acts as a PPARd
Peroxisome proliferator-activated receptor delta

Peroxisome proliferator-activated receptor delta , also known as NR1C2 is a nuclear receptor encoded by the gene.This gene encodes a member of the peroxisome proliferator-activated receptor family....
 modulator. It activates AMP-activated protein kinase
AMP-activated protein kinase

5' AMP-activated protein kinase or AMPK or 5' adenosine monophosphate-activated protein kinase consists of three proteins that together make a functional enzyme, conserved from yeast to humans, that plays a role in cellular energy homeostasis....
 and stimulates glucose uptake
Glucose uptake

Method of glucose uptake differs throughout tissues depending on two factors; the metabolic needs of the tissue and availability of glucose. The two ways in which glucose uptake can take place are facilitated diffusion and secondary active transport ....
 in skeletal muscle
Skeletal muscle

They generally contract voluntarily , although they can contract involuntarily through Reflex action. The whole muscle is wrapped in a special type of connective tissue, epimysium....
 tissue, and has been demonstrated to reverse metabolic abnormalities in obese men with pre-diabetic metabolic syndrome
Metabolic syndrome

Metabolic syndrome is a combination of medicine disorders that increase the risk of developing cardiovascular disease and Diabetes mellitus. It affects one in five people, and prevalence increases with age....
, 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
AICA ribonucleotide

AICA ribonucleotide or AICAR is an intermediate in the generation of inosine monophosphate, which acts as an AMP-activated protein kinase agonist....
, 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.






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GW-501,516 (also known as GW1516 or GSK-516) is a drug developed by GlaxoSmithKline
GlaxoSmithKline

GlaxoSmithKline plc is a United Kingdom-based pharmaceutical industry, biological, and healthcare company. GSK is the world's second largest pharmaceutical company and a research-based company with a wide portfolio of pharmaceutical products covering anti-infectives, central nervous system, respiratory, gastro-intestinal/metabolic,...
, which acts as a PPARd
Peroxisome proliferator-activated receptor delta

Peroxisome proliferator-activated receptor delta , also known as NR1C2 is a nuclear receptor encoded by the gene.This gene encodes a member of the peroxisome proliferator-activated receptor family....
 modulator. It activates AMP-activated protein kinase
AMP-activated protein kinase

5' AMP-activated protein kinase or AMPK or 5' adenosine monophosphate-activated protein kinase consists of three proteins that together make a functional enzyme, conserved from yeast to humans, that plays a role in cellular energy homeostasis....
 and stimulates glucose uptake
Glucose uptake

Method of glucose uptake differs throughout tissues depending on two factors; the metabolic needs of the tissue and availability of glucose. The two ways in which glucose uptake can take place are facilitated diffusion and secondary active transport ....
 in skeletal muscle
Skeletal muscle

They generally contract voluntarily , although they can contract involuntarily through Reflex action. The whole muscle is wrapped in a special type of connective tissue, epimysium....
 tissue, and has been demonstrated to reverse metabolic abnormalities in obese men with pre-diabetic metabolic syndrome
Metabolic syndrome

Metabolic syndrome is a combination of medicine disorders that increase the risk of developing cardiovascular disease and Diabetes mellitus. It affects one in five people, and prevalence increases with age....
, 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
AICA ribonucleotide

AICA ribonucleotide or AICAR is an intermediate in the generation of inosine monophosphate, which acts as an AMP-activated protein kinase agonist....
, 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
International Olympic Committee

The International Olympic Committee is an organization based in Lausanne, Switzerland, created by Pierre de Coubertin and Demetrios Vikelas on June 23, 1894....
. The World Anti-Doping Agency
World Anti-Doping Agency

The World Anti-Doping Agency , , is an independent foundation created through a collective initiative led by the International Olympic Committee ....
 has also begun work on a test for the two drugs, and they have been added to the prohibited list from 2009 onwards.

See also

  • AICA ribonucleotide
    AICA ribonucleotide

    AICA ribonucleotide or AICAR is an intermediate in the generation of inosine monophosphate, which acts as an AMP-activated protein kinase agonist....
  • Peroxisome proliferator-activated receptor
    Peroxisome proliferator-activated receptor

    In the field of molecular biology, the peroxisome proliferator-activated receptors are a group of nuclear receptor proteins that function as transcription factors regulating the expression of genes....