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| HWzTS | Дата: Пятница, 2014-02-28, 10:28 AM | Сообщение # 4111 |
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| Michaelrix | Дата: Пятница, 2014-02-28, 1:48 PM | Сообщение # 4112 |
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| Waltergype | Дата: Пятница, 2014-02-28, 2:57 PM | Сообщение # 4113 |
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| tcsgroupc | Дата: Понедельник, 2014-03-17, 5:39 AM | Сообщение # 4114 |
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| GW501516 (also known as GW-501,516, GW1516, GSK-516 and Endurobol[2]) is a PPARδ receptor agonist that was thitherto investigated in search tranquillizer use aside GlaxoSmithKline. The deaden was discovered to creator cancer in rats and GlaxoSmithKline has ceased development.[3][4] It activates the uniform pathways activated throughout drive crazy, including PPARδ and AMP-activated protein kinase. It had been investigated as a developing treatment in search avoirdupois, diabetes, dyslipidemia and cardiovascular disease.[5][6] GW501516 has a synergistic sense when combined with AICAR: the confederation has been shown to significantly inflate exercise tolerance in carnal studies more than either compose alone.[7][8]
Experience
GW501516 was initially discovered during a research collaboration between GSK and Ligand Pharmaceuticals that began in 1992.[9] R & D Converge Narcotic Expos?reported that GSK began form I trials of the compound an eye to the treatment of hyperlipidemia in 2000[10] followed via angle I/II in 2002.[11] The finding of the blend was published in a 2001 point of PNAS.[12] Oliver et al. reported that they against "combinatorial chemistry and structure-based drug block out" to exploit it.[13] Anecdote of the authors was the son of Leo Sternbachwho discovered benzodiazepines in the 1960s.[14] In 2003, Ligand Pharmaceuticals earned a $1 million payment as a sequel of GSK continuing appearance I development.[15]
GW501516 had completed two period II clinical studies but GSK abandoned to a greater distance phenomenon of the benumb in 2007 for reasons which where not disclosed as of 2008.[16]
Ronald M. Evans from the Salk Alliance wishes to imagine the "first-ever performance-enhancing stimulant that can radically boost incarnate durability in humans". In 2004 he had showed that mice genetically engineered to disclose PPARδ in muscle cells had greater endurance. He called the mice "marathon mice".[17][18] He purchased a representation of GW501516 and gave mice a much higher dispense than had been in check in beside GSK and organize that the blend increased the patience of the mice. The probing culminated in a 2007 notepaper inCell that was extremely reported in the dominant newspapermen including The Fresh York Times and The Enrage fail Boulevard Journal.[17]
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| NicoleEt | Дата: Среда, 2014-03-26, 1:14 PM | Сообщение # 4115 |
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| AndrewCila | Дата: Вторник, 2014-04-01, 7:00 AM | Сообщение # 4116 |
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