SARMs

WHAT ARE SARMs

Selective Androgen Receptor Modulators (SARMs) are a class of theoretically therapeutic compounds that have properties similar to anabolic agents but with reduced androgenic properties. This means that SARMs have been designed and manufactured to have all or most of the benefits of anabolic steroids without the potential side effects.

SARMs are what the pharmaceutical industry calls agonist compounds. An agonist is a chemical that binds to a receptor and activates the receptor to produce a biological response or action. This property of the agonist drug allows SARMs the advantage of: androgen receptor specificity, tissue selectivity, and lack of steroid-related androgenic side effects.

The appeal of SARMs, according to some research, is that they provide the medical benefits of fighting muscle wasting disease (sarcopenia), deteriorating bone health (osteoporosis), hypogonadism (andropause), and even cancer, without the harsh side effects of the anabolic steroid.

SARMs have androgen receptors and tissue specificity, which is why they appear to have fewer side effects during studies. The secret is also the ability of SARMs to differentiate between anabolic and androgenic action in the body. According to the manufacturers, instead of giving you benefits with multiple side effects, the benefits seem similar to anabolic steroids with fewer side effects.

SARMs were originally developed for people with diseases such as muscle wasting, osteoporosis, anemia, and chronic fatigue. They were intended to be a healthier alternative to testosterone replacement therapy. Whether they will perform that function is yet to be determined.

Many SARMs candidate drugs have been the subject of preclinical and clinical studies by global pharmaceutical companies. SARMs are synthetic drugs designed to have testosterone-like effects.

SARMs are still being researched and tested for various medical conditions, but have not yet been approved by the Food and Drug Administration (FDA) for any use. SARMs are banned in all professional and college sports because they are synthetic drugs and not dietary supplements. They are marketed as research chemicals and sold as dietary supplements. This can be confusing as companies often underestimate the reality that their product is a drug and not a supplement.

SARMs provide the ability to design molecules that can be administered orally, but their target tissue androgen receptors selectively vary.

The goal of research in this area is to enable a personalized response. The tissues that are the target of therapy will respond as they would to testosterone. Other tissues where unwanted side effects are produced will not.

None of the developed SARMs are truly selective for anabolic effects in muscle or bone tissues without producing androgenic effects. In organs such as the prostate gland, several non-steroidal compounds have been shown to bind to androgen receptors. SARMs are likely to show some virilization when used in high doses (e.g., used by bodybuilders). At lower doses they are effectively selective for therapeutic uses which will be important if SARMs are to have clinical application in the treatment of osteoporosis in women.

A substantial advantage of SARMs is that they are orally active without causing known liver damage. Most anabolic steroids are not orally active and can cause dose-dependent liver damage. Research continues on more potent and selective SARMs, as well as on the optimization of characteristics such as oral bioavailability and increased half-life in vivo.

The Sarms used today are first generation compounds. Future development could produce more selective agents. The Androgen Receptor Explained: The androgen receptor is found on the X chromosome and is expressed in a mixed range of tissues. Androgens have been documented to have significant actions in muscle, bone, prostate, adipose tissue, and the reproductive, neural, immune, and hematopoietic systems. The AR receptor is a member of the nuclear steroid superfamily which is made up of over one hundred members and continues to grow with new research. Among the large family of protein receptors, only five vertebrate receptors have been identified; androgens, progesterone, estrogens, glucocorticoids and mineralocorticoids. Androgens are a group of steroid hormones responsible for male traits. These hormones bind to androgen receptors and thus cause temporary or permanent changes to the tissue.

Many SARMs are defined as ligands. A ligand is a small molecule that transmits a signal between or within cells. They attenuate their effect by binding to cellular proteins called receptors. After binding to the ligand, the receptor can then send its signal to other parts of the cell, causing a physiological change within that specific tissue.

SARMs are classified as intracellular androgen receptor agonists based on their ability to activate the transcription of androgen receptor target genes.

Understanding SARMs in their most basic biological active terms is a class of drugs that mimic testosterone. They fool their target cell by binding to specific androgen receptors causing changes within the cell.

The most popular SARMs

• Andarine (S4) Andarine, or S4, is a non-steroidal SARM developed by GTx, Inc. Researchers found that S4 is tissue-selective, stimulates anabolic organs more than androgenic organs, and creates greater anabolic activity than testosterone. It does not significantly suppress LH or FSH or increase estradiol levels. This means that S4 can increase muscle and bone mass without affecting the prostate. The main implementation of S4 in the bodybuilding industry is during a fat loss phase. S4 achieves this by decreasing LPL (Lipoprotein Lipase) and has also been reported to increase muscle mass and decrease water retention with constant use. S4 appears to be an exceptional compound for maximizing fat loss while preserving or slightly increasing muscle hypertrophy.

• Ostarine (MK 2866) Ostarine is an orally active non-steroidal SARM formulated by GTx, Inc. A 12-week, double-blind, placebo-controlled, phase II clinical study in 120 healthy elderly men (over 60) and postmenopausal women showed that Ostarine significantly increased muscle tissue, improved physical function and improved / increased insulin sensitivity. In the fitness industry, users typically dose Ostarine during the bulking and recomposition phases. During the bulking phases, some users report a 7-pound gain in lean body mass in just 8 weeks. Other users have reported a decrease in fat mass and slight increases in muscle and strength. A compound that offers benefits for both lean tissue enhancement and fat loss as well as strength gain seems hugely appealing to athletes and bodybuilders looking to take their training and body composition to the next level.

• Ligandrol (LGD 4033) LGD 4033 is an orally active non-testosterone SARM developed by Ligand Pharmaceuticals. He completed Phase I clinical trials involving multiple ascending doses in healthy volunteers. According to the National Institute of Health’s National Library of Medicine, in Phase I clinical trials, “researchers are testing a new drug or treatment for the first time in a small group of people to assess its safety, determine a safe dosage range, and identify side effects. ” According to the research, “These clinical studies have shown that humans can safely tolerate up to 22 mg per day of this compound for 14 consecutive days; this compound contributed to the increase in muscle mass, decrease in fat composition, increased strength as well as increased senses of well-being. LGD 4033 also appears to reduce the rate of bone turnover that appeals to osteoporosis sufferers. Based on these results, it appears that LGD 4033 is an excellent phased SARM of shear, reassembly, bulk or strength gain.

• Cardarine (GW 501516) GW 501516 is discussed last in this section as it is often mislabeled as a SARM. GW 501516 is a selective activator that binds to PPAR-delta receptors rather than androgen receptors. GW501516 works on different pathways but its effects are as impressive as any SARM compound. GW 501516 activates AMPK (activated protein kinase), which is responsible for the oxidation of fatty acids and stimulation of muscle glucose absorption (GLUT-4 transport). Further examinations in rats and monkeys showed that this compound not only helped burn fat and build muscle, but also eliminated the onset of diet-induced obesity and type II diabetes by increasing HDL cholesterol levels and lowering LDL cholesterol levels. This compound has a number of impressive benefits, but it has potential and a serious drawback. When GW 501516 is administered in excessively high dosages, animal subjects have shown an increased risk of cancerous tumors. While some studies have come up with this result, others consistently show that GW 501516 is completely harmless. GW 501516 does not interfere with homeostatic hormone levels, is not hepatotoxic, nor does it cause the typical side effects seen with anabolic or stimulating steroids such as Clenbuterol. Although GW 501516 is not technically a SARM, its use is still prohibited by professional athletes as it is considered a metabolic modulator that activates AMPK. In the fitness and bodybuilding community this compound is most commonly used to improve exercise endurance and aid in fat loss. While the dosage of 10 mg / day of GW 501516 in 8-week cycles is effective in significantly increasing both aerobic and anaerobic endurance.

• YK 11 (Myostine) YK 11 is administered orally and is considered to be one of the most potent SARMs on the market. YK 11 has a geometric structure and compound activity comparable to anabolic steroids. YK 11 may actually be a synthetic steroid mislabeled as a SARM. It was first studied by Japanese researcher Yuichiro Kanno in 2011 and then again in 2013. The compound was found to be a partial androgen receptor agonist with gene selective properties, leading researchers to suggest that the compound is a SARM. . Preliminary in vitro results on muscle cells are very promising, although they are still in the early stages of testing. It is still unclear how YK 11 works to improve lean muscle mass in humans. However, what we do know is that YK 11 could be a myostatin inhibitor. Myostatin is a protein that is released to limit muscle growth to ensure they don’t get too big and is genetically controlled. It is found predominantly in skeletal muscle. Studies show that individuals with a mutation that limits myostatin production are both more muscular and stronger than those with normal amounts. YK 11 can help inhibit the production of myostatin in the muscles by attaching itself to the androgen receptor. From there, it can cause the muscles to create more follistatin, which in turn limits myostatin levels allowing for greater muscle growth beyond genetic capacity. Kanno, the original Japanese researcher, found that YK 11 works via the androgen receptor, which is why he initially claimed it was a SARM. The confusion as to whether YK 11 is a SARM or a steroid lies in the naming conventions. More recent interpretations of this compound imply that the backbone of YK 11 is identical to that of anabolic steroids. There are three main benefits that have been observed in both initial studies and user-reported reviews. YK 11 can be comparable to testosterone in its ability to build muscle and strength. This suggests that YK 11 is potentially more potent than testosterone at producing impressive gains with limited side effects. YK 11 can block myostatin, allowing for continued lean body mass gains. The main benefit of YK 11 and the reason it shows tremendous promise in the bodybuilding world is its potential to activate more follistatin in the muscles. This subsequently blocks the production of myostatin. By blocking myostatin, a user could potentially produce huge gains with continued lean tissue growth. YK 11 shows the potential for rapid muscle growth, and many users report seeing YK 11 results in just a week of use. Users of this compound report achieving incredible results and gains in as little as 8 weeks.

• RAD140 (Testolone) RAD140 is a selective androgen receptor modulator which increases lean body mass and strengthens the effects of testosterone. It does this without the unwanted side effects of anabolic steroids. RAD140 is currently under development by the pharmaceutical company Radius. There is limited data since its initial discovery was originally published in 2010. However, the initial studies reported by Radius and anecdotal user reviews have been very promising for building lean muscle tissue. RAD140 was developed for the treatment of breast cancer and muscle atrophy in postmenopausal women. According to the Radius website, the FDA accepted their Investigational New Drug Application and the first human clinical trial was to begin in 2017. RAD140 works by binding to the androgen receptor. Different cells respond by releasing different proteins with only a few androgen receptors activated throughout the body. This stimulation causes the androgen receptor to be activated in bone and muscle cells, rather than increasing liver enzymes or affecting sexual tissue. RAD140 has the ability to bind androgens to make the body act as if it were getting a dose of testosterone. RAD140 can improve endurance, stamina and speed during high intensity workouts. Also, due to its ability to increase lean muscle tissue and reduce fat, high intensity workouts and interval training can be optimized every time and increase in muscle size and strength occurs. In fact, during the initial studies in monkeys, scientists observed an average weight gain of more than 10% in just 28 days. This was done using only RAD140 and without any of the negative side effects traditionally related to testosterone. RAD140 can reduce the side effects of testosterone when used together. When taken together with anabolic steroids, initial studies indicated that RAD140 reduces the side effects of testosterone stimulation on the prostate and seminal vesicles in monkeys. Additionally, many anabolic steroid users report problems with their liver health. However, during the 28-day study, these monkeys also showed minimal increases in liver enzymes at a dose 10 times the fully effective dose. According to Radius, RAD140 has a greater anabolic effect than testosterone. It interacts with hormone receptors in muscle and bone tissue in the same way as higher doses of testosterone. RAD140 does not interact with the aromatase enzyme, so it does not convert to estrogen like testosterone does. RAD140 can aid in weight loss by increasing the body’s natural ability to burn fat. According to Radius, RAD140 does not appear to have the same side effects as anabolic steroids on the reproductive organs. Initial studies in mice found that low doses of RAD140 are all it takes to stimulate muscle growth without affecting the size and shape of the prostate. RAD140 is safe for women. Like all SARMs, it has the ability to selectively stimulate bone and muscle growth by reducing the effects on sexual tissues such as the prostate, clitoris and breast tissue. RAD140 is being tested for the treatment of breast cancer. It is specifically designed for the treatment of androgen receptor positive and estrogen receptor positive breast cancer in postmenopausal women. In vitro studies completed in 2017 showed that RAD140 inhibits the growth of AR / ER + breast cancer cells. The results of these studies supported further investigations of RAD140 as a treatment for breast cancer and the first human clinical trials were carried out.

• MK 667 (Ibutamoren) MK 667 is a clinically tested secretagogue. A secretagogue increases your body’s natural secretion of growth hormone. It is supported by numerous clinical studies conducted to test its efficiency and safety. Research supports several benefits of MK 667, including its ability to increase growth hormone and IGF-1 levels. Like Cardarine, MK 667 is not a SARM. It is a GH secretagogue related to peptides. In particular, MK 667 is a potent, selective, long-acting, orally active, non-peptide ghrelin receptor agonist and a growth hormone secretagogue. MK 667 mimics the growth hormone (HGH) stimulating action of the endogenous hormone ghrelin. MK 667 has been shown to support (GH) – (IGH) axis activation and increase lean body mass without any change in total fat mass or visceral fat. It is being studied as a potential treatment for children and the elderly who have a deficiency of this hormone. Human studies have shown that it increases both muscle mass and bone mineral density, making it a promising potential therapy. As of June 2017, MK 667 is in the preclinical stage of development due to growth hormone deficiency. Since MK 667 is still an experimental research drug, it should be noted that it has not yet been approved to be marketed for consumption by humans in the United States. However, it has been used experimentally by some in the bodybuilding community. Since it chemically mimics the hormone ghrelin, it functions as a neuropeptide in the central nervous system and crosses the blood brain barrier. There is concern that a particularly longer half-life may overstimulate ghrelin receptors in the brain and lead to some harmful mental side effects, but there is no evidence to support these concerns. MK 667 blocks somatostatin receptors. These receptors inhibit the release of growth hormone in larger quantities. When somatostatin receptors cannot disrupt growth hormone, it amplifies the production of GHS-R. This is desired to increase size gain, a greater ability to achieve lean muscle mass, tendon and ligament healing at a faster rate, and fat oxidation more efficiently and effectively. The fact that brittle bones can regenerate dramatically implies why it has been linked to the treatment of osteoporosis. MK 667 has no effect on cortisol profiles. Nine healthy young men participated in a randomized, double-blind, three-period cross-comparison of orally administered placebo. They received 5 mg and 25 mg doses of MK 667 for 7 consecutive days. The 24-hour mean levels of total and free plasma cortisol and urinary excretion of free cortisol were similar in all conditions. Ghrelin receptors (GHSRs) are critical for the release of growth hormone. Mk 667’s job in this process is to bind to a GHSR receptor and copy its intended effect. The consequence is that your body uses an abundance of this hormone without substantially increasing other hormones. This does not affect cortisol levels and will not block the immune system from rapid recovery times. MK 667 has been shown to aid the cutting phase for burning muscle builders and encouraged healthier sleep patterns. Strengthening of bone density has also been present in numerous cases.

Please Note : This guide is intended for informational purposes only, in no way do I advise you to take this type of substances not yet approved for human use and in any case even less if not under the supervision of a specialized doctor.

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