The reliable androgen receptor modulator or SARM is a new class of androgen receptor ligand. (The name follows the terminology currently used for similar molecules that target estrogen receptors, "selective estrogen receptor modulators," such as tamoxifen.)
They are intended to have the same kind of effects as androgenic drugs such as anabolic steroids but are far more selective in their actions, allowing them to be used more useful than the relatively limited use of anabolic steroids.
Video Selective androgen receptor modulator
Comparison with testosterone
Currently used androgens for male hormone replacement therapy are usually injections or skin formulations of testosterone or testosterone esters. The injected form of testosterone ester (such as testosterone enanthate, propionate, or cypionate) results in undesirable fluctuations in testosterone blood levels, with levels too high immediately after injection and too low afterwards. The skin patch gives a better blood profile profile of testosterone, but skin irritation and daily application still limit its usefulness.
SARM provides an opportunity to design molecules that can be orally transmitted, but selectively target androgen receptors in different tissues differently. The objective of the study in this area is to allow for a tailored response: The tissue that the targeted therapy will respond to such as on testosterone; other networks where undesirable side effects will not be generated.
None of SARM has been developed completely selectively for anabolic effects in muscle or bone tissue without producing androgenic effects in tissues such as the prostate gland, but some nonsteroidal androgens show anabolic ratios to androgenic effects greater than 3: 1 and higher. up to 90: 1 (RAD-140), compared with testosterone, which has a 1: 1 ratio.
This suggests that, while SARM tends to exhibit some virilizing effects when used at high doses (eg, use by bodybuilders), at lower therapeutic doses they may be effectively selective for anabolic effects, which would be important if SARM has clinical applications within treatment of osteoporosis in women. One of the important advantages of even the first generation SARM developed to date is that they are all orally active without causing liver damage, whereas most anabolic steroids are inactive orally and must be injected, and anabolic steroids that are orally active tend to cause dosage - damage independent heart, which can become life-threatening with excessive use. The study continues into more potent and selective SARM, as well as optimizing characteristics such as oral bioavailability and increased in-vivo in vivo, and seeing as first selective tissue SARM was only demonstrated in 2003, the compounds tested so far representing only the first generation of SARM and future development can result in a more selective agent than currently available. Selectivity on men
For example, if the target is bone growth in elderly men with osteopenia or osteoporosis, but without clear signs of hypogonadism, SARM targets bone and muscle tissue but with lower activity on the prostate or testis would be more desirable.
Selectivity on women
SARM for women ideally stimulates bone retention, or libido and other sexual functions that can be affected by androgens, with no negative side effects such as the development of male gender (virilization), increased LDL/HDL ratios, impaired liver function, and so on.
Maps Selective androgen receptor modulator
Example
Clinical trials
- Enobosarm (ostarine, MK-2866, GTx-024, S-22) - affects muscle and bone, directed primarily for osteoporosis but also a common treatment for andropause and reverses sarcopenia in the elderly and for cachexia in cancer patients.
- BMS-564,929 - primarily affects muscle growth, intended as a general treatment for andropause symptoms
- LGD-4033 (ligandrol) - pharmacological profile similar to enobosarm.
Pre-clinical
- AC-262,356
- JNJ-28330835
- LGD-2226 - affects muscle and bone
- LGD-3303
- S-40503 - selective for bone tissue, especially low virilization, is intended for osteoporosis and may be suitable for use in women
- S-23 - is being developed as a male hormonal contraceptive
- RAD140
Abandoned drug candidate
- Acetothiolutamide - an agonist full of high affinity AF in vitro , but very low activity in vivo due to poor pharmacokinetics
- Andarine ("S-4") - a partial agonist, aimed primarily at the treatment of benign prostatic hypertrophy
- LG-121071
- TFM-4AS-1
- YK-11
Availability
In 2013, several supplement companies began selling SARM as a supplement, in violation of the Health and Education Law of Food and Drug Supplement 1994 and DSHEA and the intellectual property rights of the patent holder of the compound. By 2017 it was found that many of the supplements sold online claiming to be SARM do not actually contain the chemicals involved.
The controversy reached mainstream media when the quarterback of Florida Gators, Will Grier, allegedly tested positive for LGD-4033, a claim that the University of Florida rejected.
On March 25, 2017, Joakim Noah was banned for twenty matches by the NBA for a positive test for the Selective Androgen Receptor Modulator LGD-4033.
See also
- Selective receptor modulators
- Selector of selective estrogen receptors
- Selective progesterone receptor modulator
- Selective glucocorticoid receptor agonists
References
Source of the article : Wikipedia
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