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SARMS FAQ

What are SARMS?

SARMS, also known as Selective Androgen Receptor Modulators – what are they?.


The androgen receptor (AR) is a member of the steroid hormone family, and plays an important role in the physiology of tissues. This receptor includes glucocorticoids, mineralocorticoid receptors, ER, PR and vitamin D3 receptor – key points for this article. 

The AR ligands include circulating testosterone and local dihydrotestosterone which bind to AR to activate it. However there are limits to the metabolism and reactivity with other receptors to how effective the use of therapeutic steroidal androgens actually work. 

SARMS were discovered to “select tissue” receptors to promote their beneficial effects of androgens without the unwanted side effects. 

Androgen receptors are found all over the body – muscle, bone, prostate, secondary sexual organs and seminal vesicles. But in bodybuilding terms, the only part that we really want to see effects of size, mass and strength on is the muscles (1). 

When any androgen cell is stimulated by testosterone this activates an enzyme called 5-a-reductase that converts testosterone into dihydrotestosterone (DHT) – an androgen hormone that is 10x more powerful than testosterone. Activation of the AR is achieved through binding of the DHT ligand to the binding point of AR, which then causes conformational changes and phosphorylation and final binding to the androgen responsive element (ARE). The ARE then modulates the transcription of the androgen responsive genes.  If testosterone is too high an enzyme called aromatase converts testosterone into estrogen, which then exerts estrogen like effects in the cell. A small amount on this naturally occurs, as estrogen is needed in a man’s body as well as testosterone (2). But too much estrogen and this is when female like symptoms start to occur.   

Under normal circumstances, the body carefully regulates its androgen production through feedback mechanisms to prevent imbalances. Taking any form of anabolic steroid, SARM or estrogen modulator disrupts this natural mechanism in a good or bad way. 

The main androgen modulators that athletes used are found in the form of “anabolic steroids”. These are known to increase muscle mass, growth and strength. 

It must be noted, that testosterone is not classed as an anabolic steroid –as it is a naturally occurring hormone in the body. The problem with using anabolics, is the side effects (depending on the type used), however as long as someone trains well the use of anabolic steroids is highly effective. This is why SARMS were discovered, to find the positive effects of anabolic steroids, without the negative effects of the steroid (3). 

Popular SARMS?

The most popular SARMS and their half-lives are detailed below (NOTE: A half-life is the time it takes for roughly half of the product to be removed by the body in natural processes):

1.    MK-2866 (Ostarine) – stimulates muscle growth through activation of satellite cells, and can boost activity of insulin like growth factor gene (IGF-1). Similar gains to using low doses of EQ, Primo or Anavar. 
Half Life – 24hours
Most males can use 25mg/day 3-8 week cycle. Women to use 10mg/day for a lower time frame. (4).

2.    LGD-4033 (Ligandrol) – raises anabolic activity in muscles and bones whilst reducing muscle wasting. Specifically bings to the coregulators of AR in muscles and bones. Being developed for the treatment of cachexia and bone wastage. May cause mild testosterone suppression bt nothing like tyical anabolics. Typically for males only at 10-22mg/day, 3-6 week cycle then off (5).
Half life – 24-36 hours
Between 3-10mg per day

3.    GSX-007 (Andarine) – developed to help prevent muscle wasting. Dose of 50-75mg per day due to short half life. 
Half life – 3-4 hours
Dosing – 50mg per day

4.    GW – 501516 (Cardarine) – a PPAR-delta receptor stimulator. PPAR-delta is found in the muscles and can increase energy, fat burning, muscle building and endurance. Cardarine binds to this – most PPAR-delta is in the muscles and can activate a lot of genes important for energy use. Cardarine technically isn’t a SARM, as it doesn’t act directly on the AR but due to its activation of PPAR-delta fibres in muscles this increases physical performance and can therefore increase muscle mass. Cardarine is also effective for fat burning as it activates fat burning genes (ABCA1 and CPT1) that allow more energy used from stores fat (6). 
When PPAR gene  is activated it causes muscle fibers to increase their use of intramuscular fat stores and increased use of oxygen – therefore making the athlete have more endurance (7).

Half life – 16-24 hours. So space doses out every 10-12 hours.
Dosing - 10mg per day for 8 weeks combined with effective training

5.    SR9009 Stenabolic – a fairly new compound (Rev-ErbA ligand) that can increase endurance and fat loss. Rev-RrbA regulated adipogenesis (fat utilisation for energy).

Half life – 4-5 hours
Dosing: 30mg per day split into 6 doses.

6.    MK-677 Ibutamoren – increase growth hormone through mimicking the action of ghrelin and binding to ghrelin receptors in the brain. Ghrelin receptors stimulate growth hormone release. Nutrobol can also increase IGF-1 levels, a potent muscle building compound in the body Side effect of increase in appetite and potential increase in joint pain (8).
Half Life – 6 hours
Dosing – 25mg per day

7.    RAD-140 Radarine – RAD140 stimulates AR receptors in bones and muscles whilst inhibiting the prostate and seminal vesicles – this means it doesn’t affect natural testosterone. Can improve cellular health ad viability through MAPK pathway. Does 20-30mg per day. Not yet approved for Humans, but isn’t banned by WADA, unlike ostarine which is its counterpart - please always check with the relevant authority for up to date banned lists.
Half life – 20 hours
Dosing – 20-30mg per day

Others SARMS include, S-40503, LGD-2226, LGC-121071, LG7, BMS 564929, ACP-105 and S-23.
 

Are SARMS safe?

Most of the SARMS that have been developed so far are sought to overcome the potential virilisation and/or aromitisatizing effects of steroidal androgens. This was achieved by searching for tissue selective agonists of the AR that could potentially active the AR in specific tissues whilst sparing others. 

The SARMS currently developed are non-steroidal, which means they are not susceptible to the enzymatic metabolism of target tissues. Remember, there were certain enzymes that converted DHT into metabolites, or synthesised testosterone from the precursor androstenedione, SARMS are not affected by these enzymes. This means that the SARMS do not convert or break down into the unwanted molecules that cause side effects, like DHT and estrogen. 

The anabolic-to-androgenic ratio of steroids is 1:1. That is, you get the muscle building the same effect as you may get man boobs for example. 
This is where SARMS can come into play. They are more selective in boosting the anabolic effects of muscle building rather than causing the androgenic side effects. This ratio can start as little as 3:1 or go as high as 10:1. 

SARMS are a group of synthetic drugs that mimic the effects of testosterone in muscle and bone with minimal impact on other organs and reduced side effects COMPARED to that of anabolic agents. The theory therefore is that you can have the perks of steroids without the side effects
 

Can you stack SARMS?

Stacking SARMS together refers to taking a variety of SARMS at the same time to achieve a synergistic effect and speed up the process of bulking. Below are the two best stacks to take for bulking (in a calorie surplus, heavy training to increase muscle mass and body weight).  

BULKING Stack – 
Andarine – 50mg per day (split into dose every 3 hours)
Ostarine – 25mg per day (1 dose)
Ligandrol – 25mg per day (1 dose)

OR a heavier stack for more experienced users
Ligandrol – 25mg per day (1 dose)
Radarine – 20mg per day (1 dose)
Ibutamoren – 25mg per day (split between morning and evening)

Recomp Stack - this stack is particularly used by an individual who is not looking to increase or decrease muscle mass, but looking to increase overall lean body mass by decreasing body fat %. 

Ligandrol – 10mg per day (1 dose)
Andarine – 50mg per day (split into dose every 3 hours)
Cardarine – 20mg per day (split morning and evening)
Ostarine – 25mg per day (1 dose)
 

Best SARMS for Cutting?

During a cutting diet (calorie deficit to lose weight), most people wish to retain as much muscle mass as possible. This can be achieve through weight training and the use of agents to help preserve muscle mass. The below compounds when stacked together inhibit accelerate muscle wastage and are also known to help increase lipolysis (fat burning).

Ostarine – 25mg per day (1 dose)
Andarine – 50mg per day (split into dose every 3 hours)
Cardarine – 20mg per day (split morning and evening)
SR9009 – 30mg per day (split into dose every four hours)
  

Are SARMS legal?

All SARMS but RAD-140 are banned by The World Anti-Doping Agency (WADA) and most other global sporting organisations. Therefore if you are competing in a tested event or a sanctioned sort that specifically prohibits the use of anabolic agents, then SARMS aren’t for you. However if you are not planning to compete, then SARMS could be part of your daily routine, providing you only buy from a reputable company and do not sell them on. 


What are the side effects?

Depending on the SARM itself, there are reported minimal side effects. Due to the fact that SARMS are non-steroidal, they do not metabolise, aromatise or have virilisation effects compared to anabolic steroids. This means that SARMS can produce the same effects as testosterone injections without estrogen conversion (DHT and estrogen metabolites). 
Some side effects that have been noted are:

Mild appetite increase from MK-677. 
Mild natural testosterone suppression from LGD-4033. Other side effects can be increase thirst, increased sex drive (surely not a bad thing), potential increased headaches and acne (over use cases). 

 

SARMS VS Prohormones

A prohormone is a chemical precursor, so they act on the intended hormone, but also carry the side effects with it. The prohormones can impact natural hormone production and other biological systems and may also be toxic to the liver. Due to this, they should be carefully controlled and cycled. SARMS on the other hand were designed to be a much safer alternative to steroids and are technically developed to help combat muscle wasting diseases, not for bodybuilding purposes – but it is due to these effects that they are popular with the bodybuilding community. 

SARMS can be considered a better alternative to prohormones due to lack of side effects and also that you might not need a post cycle therapy (PCT) with SARMS (check individually on each SARM first). A PCT is usually used to allow the bodie’s natural hormones to get back to their normal range. If you are experienced in using products such as these, then prohormones may work very well for you, but it may be better to start with a SARM and build up – as should be done in any case. Both are effective and show data to back up claims of muscle building without the use of anabolic steroids (particularly for the needle-phobics).  

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