by Mike Arnold S.A.R.M’s, or selective androgen receptor modulators, as they are called, have become all the rage among pharmaceutical researc
by Mike Arnold
S.A.R.M’s, or selective androgen receptor modulators, as they are called, have become all the rage among pharmaceutical researchers looking to cash in on the next-generation of low-risk anabolics. With a potentially high degree of selectivity for muscle over other bodily tissues, their selling point lies in the ability to provide steroid-like effects without the unwanted androgenic, progestagenic, and estrogenic side effects inherent to traditional AAS. Researchers have been careful to distance these new drugs from AAS in both name and marketing, being fearful of any negative repercussions that might result via association with the word “steroids”, but are these drugs really so different?
Although lacking the typical steroidal backbone found in traditional AAS molecules, their mechanism of action is essentially the same, with both S.A.R.M’s and steroids generating their positive and negative effects through activation of the androgen receptor. These receptors are found not only in muscle fiber, but in numerous other bodily tissues, such as the skin, bone, prostate, larynx, and brain. When A.R.’s in these tissues are activated, they produce effects specific to their locality. For example, activating A.R.’s within muscle tissue stimulates protein synthesis (i.e. growth), while activating A.R.’s in the larynx causes the vocal chords to lengthen (resulting in a deeper voice). Many of the side effects we associate with AAS use, such as hair loss, oily skin, acne, etc, are all caused by activation of the androgen receptor.
The main difference between S.A.R.M.’s and steroids is the degree to which they activate these receptors in non-muscle tissues. The more strongly an A.R. is activated, the more pronounced the effects of that activation will be. For example, DHT has a very potent androgenic effect on A.R.’s in the scalp, leading to significant hair loss in those that are genetically prone, while a drug like Anavar is known to be rather mild in this regard and therefore, few people report hair loss when using it. Steroids as a whole display a vast degree of selectivity in the various A.R. dependent tissues, which can range from almost S.A.R.M-like to very low. Furthermore, just because a steroid may be androgenically potent in one tissue, it does not necessarily mean it is potent in another.
This is why we can have a steroid that is brutal on the prostate, but easy on the hairline at the same time, and vice versa. While S.A.R.M.’s possess this same variability, it is nowhere near as extreme. For the most part, they exhibit a much higher degree of selectivity for muscle tissue over non-muscle tissues. In other words, they have a comparatively weak androgenic effect on non-muscle androgen receptors and are therefore much less likely to cause side effects in general.
Often, when attempting to ascertain a steroid’s general androgenic potency, the typical bodybuilder will search out the drug’s androgenic rating; a measure of androgenic potency used in Vida and other medical resources. According to previous studies, testosterone possesses an A:A ratio of (anabolic/androgenic ratio) of “100:100”, while Dianabol and Anavar come in at “200:50” and “600:20”, respectively. The problem with A:A ratios is that a steroid’s androgenic rating is determined by assessing androgenic potency in only ONE tissue—the prostate. It tells us virtually nothing about how the drug may act in other tissues. Therefore, if one is using these ratings as a means of assessing a steroid’s overall androgenic character, they can be extremely deceptive and likely to lead one to false conclusions. For instance, Masteron, despite possessing an androgenic rating of just 25-40 (quite low by conventional standards), is known to be quite harsh on the hair line, indicating an above average androgenic potency in scalp A.R.’s. This is in direct contrast to its androgenic rating and could easily deceive the uneducated user into thinking that Masteron is a weak androgen in general; a mistake only realized when the user begins experienced unwanted side effects.
The point here is that androgenic ratings are essentially worthless for measuring androgenic potency in anything other than the prostate. In order to determine a steroid’s overall androgenic character, its effect must be evaluated in each tissue individually. Unfortunately, it is not common practice for pharmaceutical researchers to assign androgenic ratings to non-prostate tissues, leaving us with one option for ascertaining a drug’s androgenic potency throughout the rest of the body—real-world use. When it comes to steroids, the collective experience of generations of bodybuilders have provided us with a pretty good idea of which steroid does what, but with S.A.R.M.’s being much newer to the scene, and with many of them not yet available even on the black/grey-market, there is much less real-world experience to draw from when attempting to form conclusions.
However, several S.A.R.M.’s have now been available for 1 or more years, providing us with ample opportunity for experimentation, feedback, and evaluation across a broad group of people. Much of this recent feedback has been centered on the S.A.R.M. RAD-140, which has captured a fair amount of interest among both bodybuilders and fitness enthusiasts alike. But with a handful of proven S.A.R.M.’s already available, what differentiates this SARM from the rest of the pack? There are a few interesting characteristics that instantly stand out, one of which is the compound’s comparatively weak androgenic effect on the prostate. Unlike the other popular SARM’s, which possess an androgenic potency only slightly under what is seen with the mildest AAS, RAD-140 is on a whole other level. Just to give you an idea of how unlikely this drug is to negatively affect the prostate, let’s look at some statistics.
When compared to testosterone propionate, clinical trials revealed that RAD-140 must be dosed at a full 30 mg/day just to provide the same degree of prostate stimulation as .5 mg of testosterone/day. In other words, RAD-140 affects the prostate with 1/60th the potency of testosterone, putting its androgenic rating at under 2 (to give you an idea how low this is, a steroid like trenbolone comes in at 500, while Anavar comes in at 20). Not only does this make it by far the safest drug ever developed in terms of prostate health, but it was even shown to antagonize the negative effects of testosterone on the prostate (when administered concurrently) at a dosage of .3 mg/kg/day, which translates into 30 mg/day for a 100 kg (220 lb) individual. In laymen’s terms, this means that RAD-140 actually reduces the negative effects of testosterone on the prostate, so even those who have no desire to use RAD-140 for its anabolic effects (traditional steroid users) may find value in this compound as a preventative medication, especially in cases where prostate enlargement is already a problem or where there is a genetic propensity for prostate issues.
Sounds good so far, but what about RAD’s effect in non-prostate tissues? As mentioned previously, it is rare for a drug’s androgenic potency to be measured in other tissues, despite their direct association with a multitude of unwanted side effects throughout the body. With RAD-140 in the same boat, we are forced to rely on anecdotal evidence for answers. Fortunately, user reports have been favorable, with claims of androgenic side effects being basically non-existent. Given RAD’s extremely low androgenic rating, this isn’t really surprising, but one should still be aware of the possibility for unwanted side effects at higher dosing ranges, no matter how unlikely. None the less, RAD-140’s overall androgenic character appears to be extremely mild, making it one of the safest anabolics for not only men, but also for women looking to avoid masculinization.
When it comes to bodyfat, the facts are less clear, but from what we can see, RAD-140 appears to have a positive, dose-dependent effect on fat loss—typical of most drugs which provide their effects via androgen receptor stimulation. None the less, RAD-140 should not be viewed as a fat loss drug, nor should any S.A.R.M.’s/AAS, as their effect on fat loss is minimal even in the best cases. One of the most important factors in the success of any S.A.R.M. hinges on its ability to be administered orally, as the prospect of daily injections does not go over well with most individuals, especially non-bodybuilders. Fortunately, RAD-140 possesses a high degree of oral bioavailability, allowing users to bypass the injection process while maintaining a high degree of effectiveness. As expected, RAD-140 is also non-toxic to the liver, with clinical trials revealing minimal elevations in liver enzymes even when administered at 10X the maximum effective dose.
Unlike traditional oral AAS, which are notoriously injurious to the lipid profile, RAD-140 appears to have no adverse effect in this area. In fact, clinical trials demonstrate the ability of RAD-140 to reduce total lipids, which not only eliminates this major cardiovascular risk factor, but may even promote improvements in cardiovascular health. Another interesting aspect of RAD-140 is its ability to protect brain function (in a manner similar to testosterone) via the preservation of neuronal functioning. This reduces the likelihood of developing neurodegenerative disease (ex. Alzheimer’s, Parkinson’s, Huntington’s), etc) while protecting brain function in general. While this effect is common to androgens, it is the first time that it has been studied in a S.A.R.M, making it a newsworthy discovery in its own right.
All of these benefits are great, but how effective is it as a muscle builder? Clinical trials reveal that RAD-140 is about 40% more myotrophic than testosterone, with .3 mg of RAD-140 being equal to about .5 mg of testosterone. Now, before you go thinking this stuff is a superior muscle builder to testosterone, hold on a second. While RAD-140 was shown to be a better muscle builder than testosterone when administered at lower dosages, one needs to keep in mind that its maximum effective dose is also much lower than testosterone, making testosterone the better mass-builder at higher dosages. However, S.A.R.M.’s are hardly ever dosed in excess of around a couple hundred mg per week, making RAD-140 a solid choice for those wishing to accelerate progress with minimal risk. While the following may seem like common sense, I should also mention that RAD-140 was shown to supply an additive effect on muscle growth when used alongside testosterone; an effect shared by AAS as a whole.
RAD-140 is an interesting compound which shares both similarities and differences with other drugs in its class. While it may not be the most potent S.A.R.M. from a muscle building standpoint, it appears to be an exceedingly weak androgen, particularly in the prostate and most likely in other tissues as well. This makes it an ideal candidate for those wishing to accelerate progress with minimal risk and a great choice for older bodybuilders with prostate issues attempting to build/maintain muscle mass. In conclusion, RAD-140’s low-risk profile, substantial anabolic effect, and several unique benefits make it a viable alternative to other S.A.R.M.’s on the market.