Selective modulators of androgenic receptors - SARMs

SARMs (Selective androgen receptor modulator) — selective modulators of androgenic receptors. By the same principle, as SERMs — selective modulators of estrogenic receptors to which well-known clomifene and tamoxifen belong SARMs are capable to join receptors of sex hormones, only not women's, but men's - androgens and to interact with them. But without having the same structure as anabolic steroids, SARMs don't give in to impact of the enzymes transforming testosterone to other connections having effects, undesirable to health.

Creating this class of medicines, scientists expected to lower an adverse effect of testosterone on a prostate. As it is accepted, first of all any substances and connections research on animals; in case of receipt of positive effects and having made sure in safety of their acceptance, conduct clinical trials in public then start in production. Often only one positive results in experiences on rats happen enough that medicine came into the view of "chemical" athletes and those began to be influenced by it independently.

Approximately the same situation has developed also with SARMs — as soon as have begun to write about this child of James Dalton in available literature, having reported that their reception leads to growth of muscle bulk, they right there have appeared in the illegal way in hands of body builders. Andarine better known in the world of sport as ‘S4 ′ was one of the first, despite ambiguous conclusions of researches, in this number. And after him practically at once and Ostarine known as GTX-024. Both medicines already were implemented in online stores before there were official confirmations that Ostarine really promotes a gain of muscle bulk at people and is rather safe in application. However in elite sport and at threat of anti-doping control ostarine is extremely risky and undesirable medicine as his metabolites are defined within three months and more - depending on a dose and specific features of metabolism at the athlete. There are no data on other SARMAM yet.

So, in September, 2011 in the "Cachexia, Sarkopeniya and Muscles" magazine (‘Journal Cachexia Sarcopenia Muscle’), p. 153 — 161, there was article with the name speaking for itself "The selective modulator of androgenic receptors GTx-024 improves the muscle bulk and physical functions at healthy elderly men and women in a postmenopause: results of the double blind person, placebo - a controlled research of a phase II". The results of reception of GTx-024 referred by scientists to statistically significant were given in this article: 12 week course of oral reception of 3 mg of drug lead to a gain of dry muscle bulk, peer 1,4 kg and to depression of fatty weight in 300 grams in the absence of any exercise stresses. Lower dosages of substance resulted in less expressed results. Official conclusion of researchers sounded so: GTx-024 showed dozozavisimy improvement of the general muscle bulk of a body and physical functions, is well transferred. GTx-024 can be useful to prophylaxis and/or treatment of a catabolism of the muscle bulk bound to cancer and other chronic diseases". Perhaps, 1.4 kg of muscle bulk in 12 weeks aren't a lot of, but it is officially received and recorded result. Please pay attention to Meldonium

Now the pharmaceutical companies have several types of SARMs concerning which the first stages of clinical trials were in public successfully complete and which can be available for legal sale already soon, and till that time, practice of their application in the sports purposes will already for certain be created, however, at the moment even proceeding from small amount of the above-stated information, it is possible to gain an impression about a dosage, duration of acceptance and side effects.

Researches

At the moment any selective modulator of androgenic receptors isn't really selective. They shows only higher anabolic index, at the same time the ratio anabolic to androgenic activity makes from 3:1 to 10:1 (at Testosteron-Depotum the ratio is peer to 1:1)

Practically all selective modulators of androgenic receptors are issued in the form of tablets and don't cause injury of a liver.

It is the optimum choice for women as they exert the minimum impact on a libido, sexual characters, cholesterin level in bloods, a liver, etc.

Legal status of SARM'S

The most part of SARM'S have the legal status. In jurisprudence with high probability of SARM's will be recognized as drugs.

Ostarine and cardarin (by mistake belongs to SARMs) are entered in the list of strong substances for Art. 234 of the Criminal Code of the Russian Federation. The ban is initiated by the Ministry of Internal Affairs of the Russian Federation in August, 2016. Legally ostarine and cardarin have equated to anabolic steroids.

Stages of SARMs testing

Clinical testing:

• Ostarine (MK-2866, GTx-024) - affects bone and muscular fabrics
• BMS-564,929 - affects mainly muscular tissue
• Ligandrol - Ligandrol or Anablicum (the laboratory code of LGD-4033) - is similar to Ostarine

Preclinical testing:

• AC-262,356
• JNJ-28330835
• LGD-2226 - influences bones and muscles, studying is suspended because of high toxicity
• LGD-3303
• S-40503 - affects mainly a bone tissue (treatment of osteoarthrosis)
• S-23 - as a men's contraceptive
• YK-11 - the Japanese SARM at a development stage which is also inhibitor of a miostatin
• RAD140 - development of the Radius company, is suitable for intake, in addition to anabolic effect causes increase in endurance and has neuroprotective effect

Are suspended:

• Andarin - Andarine (the laboratory code of S-4) - development isn't kept any more
• Kardarin - (Synonyms: Cardarine, Endurobol, Peroximod, Hennos, the laboratory code of GW-501516) - development isn't kept in connection with cancerogenic action any more
• Other (doesn't treat SARMs):
• Reversol (Reverol, edrophonium or SR9009) - connection suitable for intake, is developed by Scripps Research Institute. The main effects - increase in endurance (due to formation of new mitochondrions), treatment of obesity, a muscular hypertrophy. The mechanism of action consists in linkng with the molecule Rev-ErbA alpha in an organism which performs various regulatory functions.
• Ibutamoren - Ibutamoren, Nutrobal (MK-677) - growth hormone secretion stimulator accepted inside.
• Laksogenin (5a-hydroxy-laxogenin or Anogenin) - vegetable steroid sapogenin, studied by Japanese in 1960. Now began to move ahead actively in sport though any positive effects at the person aren't proved.
• AICAR - means for increase in endurance