ergo-log.com

Definition: "An ergogenic aid is any substance or phenomenon that enhances performance "

19.10.2010

Strong stuff, the new SARM from Radius

Maybe we're barking up the wrong tree, but we think we've found it: the mysterious SARM that the Cambridge-based pharmaceuticals company Radius is doing tests on. The structural formula is shown in the diagram below. We came across it in Tetrahedron Letters, in an article that suggests that this substance has powerful anabolic effects.

SARMs are mostly complex molecules that at first glance bear no resemblance to classical steroids like testosterone, boldenone and trenbolone. But they bind to the androgen receptor and stimulate muscle growth. Chemists are hoping that they can manufacture SARMs with the desired anabolic properties, but without the less desirable androgenic properties. So stronger muscles and bones, but no hair growth, aggression, cardiovascular disease or enlarged prostate.

That's the theory at least. In practice it's all more complicated. The S4 SARM, a compound developed by GTx and already available on the black market, has a very particular side effect. Users developed night blindness, going by the posts on bodybuilding boards. Doctors have occasionally reported the same side effect in users of old-fashioned steroids, but this was only incidental. [Can J Ophthalmol. 1985 Dec; 20 (7): 254-6.] S4 – which also goes by the name of andarine – affects the eyes of some users.

GTx worked together with Merck/Schering-Plough Pharma on the development of SARMs, but at about the time that the side effects of S4 became known in doping circles, the collaboration came to an end. Merck/Schering-Plough Pharma is now concentrating on MK-0773, a new but classical anabolic steroid. GTx is silent on the subject of S4, but a few months ago the company issued press releases on ostarine, an S4-related SARM.

There are other companies working on SARMs too, like Radius. In Tetrahedron Letters Radius researchers describe the synthesis of a compound with the unpronounceable name (2R, 3S) 2-amino 3-(benzyloxy) 4,4,4-trifluorobutanoic acid (4,4,4-trifluoro-OBn-D-allothreonine). In the article the researchers refer to the compound simply as compound 7 [cpd 7], which is the molecule in the diagram above.

The researchers suspect that compound 7 is capable of interacting with the androgen receptor, so they tested it on rats.

LABC = levator ani muscle, a marker for desired anabolic effects; Prostate = the weight of the prostate, a marker for undesired androgenic effects.

Compound 7 works better than testosterone propionate, as you can see. Interestingly though, the researchers gave the rats compound 7 orally, while they injected the testosterone. The dose they gave is modest, for a SARM at least. All things considered, compound 7 seems to resemble another promising SARM, BMS-564929, which is produced by Bristol-Myers Squibb. [Endocrinology. 2007 Jan;148(1):4-12.]

Radius is now doing tests with a SARM that it has labelled RAD140. It is "potentially the first orally administered anabolic drug for treating osteoporosis, sarcopenias, and frailty associated with aging", Radius claims on its website. [Link]

Is this the one we've been waiting for?

Source:
Tetrahedron Letters 51 (2010) 5361-5363.

More:
Merck's new anabolic steroid: MK-0773 02.07.2010
Bottle of S4 costs $170 online 23.11.2009
Anabolic effect of giant Egyptian androgens exceeds that of testosterone 26.04.2009