What are Selective Androgen Receptor Modulators?

Written by Ben Bunting: BA, PGCert. (Sport & Exercise Nutrition) // British Army Physical Training Instructor // S&C Coach.


Selective Androgen Receptor Modulators

If you are looking for a safer, more natural way to gain muscle and lose fat, you may want to look into using Selective Androgen Receptor Modulators (SARMs).

These non-steroidal, tissue-specific androgen derivatives act on the androgen receptor to stimulate muscle and bone growth while reducing the risks of anabolic steroids.

So, are they worth looking at, or would you be spinning the roulette?

SARMs are non-steroidal, tissue selective androgen derivatives

While SARMs are currently being tested for prostate cancer, osteoporosis, and cancer related cachexia, they may also prove useful in other situations.

In men, SARMs have been found to inhibit growth of certain tumors and promote bone growth. They are also being investigated for use as male contraceptives.

Currently, several SARMs are being tested for their effects in athletes and bodybuilders. Some athletes have been suspended from competition for testing positive for SARM metabolites.

For example, an NBA player and an NCAA basketball player were suspended after positive tests for LGD-4033. In addition, four UFC fighters were penalized for trace amounts of ostarine. 

Although SARMs are not yet approved for use in humans by the FDA, they are an attractive future therapy.

Some of the early clinical trials have found that SARMs are well-tolerated and are more convenient to administer than their steroidal counterparts. SARMs can also target certain organs in the body, such as the prostate and the breast.

SARMs have many potential applications in human health, from prostate cancer to contraception to osteoporosis, cachexia, and muscular dystrophies. 

SARMs act on the androgen receptor

Selective androgen receptor modulators are small molecule drugs that act on the androgen receptor (AR) and elicit anabolic effects in their target tissues. They have several benefits over traditional androgen therapies, including few side effects and excellent oral and transdermal bioavailability.

These compounds have recently been studied in various medical conditions, including prostate cancer, osteoporosis, Alzheimer's disease, and breast cancer.

The androgen receptor is widely expressed in human tissues, including bones and muscles. It plays an important role in sexual development, as well as in growth and bone maintenance.

Due to tissue-specific expression patterns, the AR exhibits diverse actions. SARMs are chemically engineered to selectively bind to the androgen receptor and exert their agonist and antagonist activities.

In addition, SARMs are well tolerated, and their oral bioavailability makes them an attractive treatment option for various medical conditions.

The action of SARMs on the androgen receptor begins when the drugs enter the cell's cytoplasm.

They displace the androgen receptor from heat shock proteins in the cell and act as transcription factors. These molecules also interact with different co-regulatory proteins in the cell to regulate the transcriptional response.

SARMs are small, non-steroidal molecules that bind to the androgen receptor (AR) in different tissues. They have the ability to block DHT production and limit the effects of estrogen on the body.

The effects of SARMs are reported to be beneficial for muscle and bone growth, and they may also be beneficial in treating bone conditions such as osteoporosis and cachexia.

They stimulate bone and muscle growth

They have been shown to improve athletic performance and prevent bone wasting in animal models, but evidence of their benefits in humans is limited. 

They are non-steroidal and inhibit 5 -reductase, which can convert androgens to estrogen.

These drugs reduce the risk of side effects by selectively binding to androgen receptors in targeted tissues.

They also inhibit the growth of breast cancer cells and reduce prostate size.

SARMs are being used as performance-enhancing drugs that are widely available to buy online.

These drugs increase testosterone levels by blocking the negative feedback loop of the hypothalamic-pituitary-gonadal axis. SARMs are not addictive and can be used for lean body mass gains.

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They may be used to treat cancer

SARMs (selective androgen receptor modulators) are an emerging class of drugs that may be used to treat cancer.

These compounds function as potent anabolic agents while it is reported that they have less of a neative impact on other organs. 

They may represent a new strategy for treating cancer cachexia. However, more human studies are required to confirm whether these compounds are effective for cancer patients.

SARMs are promising for treatment of hormone-resistant cancers. During the 1990s, the growing popularity of tamoxifen stimulated research on analogous drugs.

Several labs began developing lead compounds and specific pharmacophores. Early work focused on a class of small molecules called aryl-propionamides. These molecules exhibit agonist, partial agonist, or antagonist activity in different tissues.

This tissue-specificity makes them suitable for use in specific medical conditions and minimizes off-target effects.

They are still a health risk

SARMs, or selective androgen receptor modulators, are similar to anabolic steroids but are less toxic to the body.

While research on SARMs is still ongoing, it is apparent that they can have fewer negative side effects than regular steroids. They also have less adverse effects on the reproductive organs.

Anabolic steroids are the most commonly abused appearance and performance-enhancing drugs. Although their use was restricted to athletes before the 1980s, it has become increasingly common among recreational users. 

Although there is limited research in humans, they have shown promising results in animal studies.

Several oral SARMs are under development for the treatment of muscle wasting and functional limitations associated with aging. However, none of these drugs has been approved by the US Food and Drug Administration.

As such there are warnings against their use by the FDA who state that SARMs can increase the risk of a cardiovascular event and liver damage. 

Furthermore, as SARMs are a relative newcomer, their long term effects aren't known, nor are all of the potential side effects.

When using SARMs, it's important to get blood tests done to check your hormone levels, liver values, and other health markers.

It's also important to take at least 12 weeks off after finishing your cycle to prevent adverse effects on your organs. There are many over the counter PCT products on the market.

Many are designed to boost testosterone production while managing estrogen levels.

They may affect sperm count

Selective androgen receptor modulators, or SARMs, may decrease sperm count, according to a new study. While these compounds are not as damaging as anabolic steroids, they still have the potential to reduce sperm count.

This is because they do not cause the massive shutdown of androgen receptors that anabolic steroids cause.

The potential side effects of SARMs, including decreased sperm count, have to be considered before using them.

The hormone androgens play a major role in male phenotype, and they control the expression of many target genes that are important for male fertility.

Selective androgen receptor modulators can interfere with male sexual function, preventing the androgen from binding to androgen receptors and causing the expression of a specific gene.

BPA is one such antiandrogen, and has been linked to adverse effects on the male reproductive system, including the sperm count, sperm motility, and reproductive organ weight.

In one study, BPA exposure reduced male specific cytochrome P450 enzymes, causing oxidative stress in the testes.

This can affect sperm cell function by impairing DNA fragmentation and decreasing intracellular adenosine triphosphate levels.

Selective androgen receptor modulators have anti-reproductive effects in experimental animals and in epidemiological studies of males exposed to BPA.

Studies have shown that urinary BPA concentrations correlate with sperm counts in males.

SARMS Conclusion

SARMs are also used in medical research to treat certain conditions. According to the available literature they can stimulate the release of anabolic hormones by activating receptors in the muscles and bones.

These compounds are being studied to see if they can help fight cancer, osteoporosis, and heart failure.

They may be able to boost lean muscle mass, increase endurance, and improve overall health and performance.

However, SARMs are not approved for human use, most studies are based on animal models and they may have long term effects that we are not aware of, plus they may increase liver damage or the risk of suffering from a stroke or other cardiovascular event. 

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