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20.07.2011


Lab uncovers underdosed Aicar, GW1516 and MK-2866 on black market

Doping users don't confine their purchases to steroids, growth hormone, insulin and EPO. More and more athletes are using experimental substances which go by the name of 'research chemicals'. Biochemists at the German Sport University Cologne bought three preparations in this increasingly popular category from webshops. All three were heavily underdosed.

The researchers do not reveal the research chemicals webshop where they bought the substances and we don't know which one it was either. And no, we have no indication that the Aicar shown here was the one they used.
We reproduce the data that the researchers published on the website of Drug Testing and Analysis. We hope you find this useful.

Officially, research chemicals webshops sell to researchers wanting to do experiments on cells or mice, and not to chemical athletes wanting to break records. Nevertheless you can't get around the fact that the substances you can buy in these webshops are pretty interesting for athletes; some are even more than just pretty interesting. The researchers wanted to know whether the compounds in the vials actually contain the amounts listed on the labels.


They bought three substances: Aicar, GW1516 and MK-2866. The contents of the bottles that they studied in the lab did contain the right ingredients. Their structural formulas are shown below.



Aicar is a new endurance drug. It's an AMPK booster. If you give the stuff to inactive mice, their endurance increases by 44 percent. [Cell. 2008 Aug 8;134(3):405-15.] It's pretty much an open secret that athletes use Aicar. The French police first discovered it in 2009 in the lockers of cyclists in the Tour de France. [BMJ. 2009 Oct 13; 339:b4201.]

GW1516 comes from the same set-up as Aicar: the molecular researcher Ron Evans. GW1516 is a PPAR-delta-agonist. If you give Aicar to mice their muscle cells burn radically more fat. If you give mice Aicar and GW1516, they reinforce each other's effect and the lab animals turn into ultra-marathon mice. And an interesting detail: some research chemicals shops give a reduction if you buy GW1516 together with Aicar.

The GW1516 contained a warning, the researchers write. "GW501516 is a very potent chemical. This form is for research/laboratory use only. Not intended for human use. Accidental ingestion could cause increased body temperature, heart palpitations, vomiting, shaking, or even death. Keep out of the reach of children. Protect from light. Store at room temperature."

Finally, MK-2866 is a SARM. You might be familiar with it under the name of ostarine, the little brother of andarine, alias S4. The researchers had previously tested a vial of S4 that they had bought online, and discovered an overdose of S4 with a number of metabolites that had been created during the biosynthesis process, but which the manufacturer had forgotten to remove. The ostarine that the researchers tested on this occasion was clean, however.

The researchers don't know whether MK-2866 is already being used. They have their suspicions, as S4 has already shown up in doping tests. Last year doping hunters found S4 in a urine sample from the Jamaican Bobby-Gaye Wilkins. [Jamaica Observer 14 July 2010] S4 is unlikely to be launched officially. The company behind S4 stopped tests on the substance a couple of years ago.






Of the three substances tested, Aicar is probably the most interesting for athletes. The body produces the substance itself in fair quantities during physical exertion. Devising a test that can distinguish between synthetic Aicar and the endogenous variety is not so simple.

Source:
Drug Test Anal. 2011 May;3(5):331-6.

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