SARMs S4
SARMS And BRIDGING.
Is This The Perfect Drug To Use In-Between steroid Cycles?
SARMS is the latest addition to the enhanced athletes arsenal and it’s creating a storm of controversy. It may very well be most significant advancement in muscle development since the invention of Dianabol back in 1956. A bold statement for sure. But SARMS is truly an incredible compound with many applications, most significantly, as a viable anabolic enhancement to be used in-between steroid cycles.
SARMS is not a steroid. It is the veritable “next step” beyond steroids. It’s a Selective Androgen Receptor Modulator, which essentially means it targets the androgen receptors in a way where they’re most beneficial while avoiding the nasty side effects that go along with traditional androgenic drugs.
Due to that elusive combination of good without the bad, SARMS has been hailed as the “Holy Grail of Muscle Growth.” It’s what all athletes have been waiting and wishing for. Think of it as pizza without calories, alcohol without the hangover and safe sex without condoms. Is that possible? Yes it is. But there are limitations. (Damn!) But rest assured, they’re minor. There is a catch – there always is. But in the case of SARMS, the catch isn’t that bad.
For one thing, SARMS will not work like mega doses of steroids. You would not be able to take supraphysiological dosages in order to gain massive size on the order of a gram of testosterone. Its benefits work within a specific dosage range . In that regard, SARMS is unique. A good comparison would be to aspirin, which will always lower a temperature from a fever, but no lower than 98.6. However, MORE aspirin will not improve the condition. There’s that “sweet spot” where it works its magic with virtually no risk. SARMS is like that. In controlled dosages it’s a non toxic, non suppressive compound that works like steroids, but without the side effects. But beyond a certain dosage, it doesn’t work much better. It’s a sort of “built in safety net.” 50ml a day is an effective dosage with 100mls a day being the cut-off point to avoid any negative side effects.
The potential and the possibilities are as compelling as they are enticing, but one area where SARMS is becoming increasingly popular is in the area of “bridging.”
A “bridge” is essentially a description of using any compound that will maintain the gains of the former cycle on through to the next cycle, months later. How to best do that has been a controversial topic for some time. In the past, bodybuilders have attempted to sustain the effects of a steroid cycle by using a milder , less suppressive steroid (such as Primobolin) in-between cycles. Another method of attempting a “bridge” was to use a short acting oral in the A.M so that it would not be active past a four hour window. In this way one may (theoretically) recover over-night, resulting in the body managing to restore its natural hormonal balance. Unfortunately, neither game plan was especially successful for even a low dose of any steroid will cause suppression and hinder recovery. But remember, SARMS isn’t a steroid. It works on an entirely different principle – that of being “selective” to muscle. And at 50 mls a day it’s been shown to have no suppressive effects. (Unless dosing exceeds several months). This makes SARMS the perfect choice to be used in-between cycles. You won’t make massive gains while on but you’ll hold onto your gains and still be in an “enhanced” state without fear of suppression. Not a bad deal.
It would make far more sense to “bridge” using SARMS on its own, or with natural supplements in order for the body to maintain ultimate anabolism without suppression. As much as using a less suppressive steroid may seem to make sense, ANY steroid even in low dosages will suppress, delay recovery, and ultimately work against the process of recovering from a cycle. It will also minimize the results of the NEXT cycle since the receptors would not have had a chance to replenish. This is what makes SARMS superior for this purpose.
Another similar method that’s becoming popular is to use SARMS as a “mini-cycle” in-between steroid cycles. In other words, once you finish your course of steroids and do a proper PCT and settle into being “natural”, after a while you can use SARMS daily for a 4 week run. In this way you can bump up gains, increase muscle density, improve lifts and burn fat – all without deregulating androgen receptors or compromising the HPTA. (Hypothalamic Pituitary Testicular Axis). Never before has this been possible.
A PCT following a SARMS cycle may not be necessary. Some OTC supplements may be all you need to get back to baseline. SARMS won’t aromatize so there’s no fear of developing gyno or other estrogen related conditions.
SARMS has many uses and having an anabolic/androgenic advantages while off cycle may be the most significant of all.
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SARMS And The New Post Cycle Therapy
SARMS S-4 is a revolutionary advancement in the field of muscle development through anabolic enhancement. Simply put, SARMS targets the androgen receptors in a “selective” manner (Hence the term Selective Androgen Receptor Modulators), zeroing in on the “good “ aspects while negating the bad(1). In this way, you get the benefits of enhanced androgenic effects – strength, increased muscle and heightened libido – without the negative side effects of traditional anabolic/androgenic steroids -- prostate enlargement(2), increased blood pressure, testicular atrophy, hair loss and elevated cholesterol(3)(4). And it does it all in an orally bio-available form that is not liver toxic. Sound interesting? It should. SARMS is changing the landscape of bobybuilding in a big way. And for those who already use steroids as a part of the process, SARMS has several interesting applications, most significantly, in the area of Post Cycle Therapy(5).
Part of this usage is another advantage that is especially appealing to those who use steroids on a regular basis. In controlled dosages, SARMS is relatively non-suppressive. This opens up considerable possibilities in regard to utilizing SARMS to enhance a typical steroid cycle, but more significantly, it becomes a tremendous tool in the area of PCT.
Coming off of steroids is the most complicated, and often confusing part of the process. The athlete wants to maintain gains, avoid the “crash” of reduced strength and muscle growth and yet, recover his natural hormonal balance. It’s a tricky balance of drugs, supplements and ultimately luck. Some fare better than others and many consider the down time inevitability. But with the advent of SARMS S-4, not only can the transition be made more tolerable, it is now possible to avoid the down sides of coming off of a steroid cycle(6). One can maintain the gains and even continue growing after the cessation of steroids.
The most logical method of PCT use would be to implement SARMS as a “taper” at the end of a cycle. In other words, once you stop using steroids, the body can obviously no longer support the muscle growth it achieved in an enhanced state. Natural testosterone is lower. And nitrogen retention is lessened. That’s where SARMS fits the bill. By using SARMS following the end of a cycle, the body can begin to recover yet still receive both the anabolic and androgen benefits. Muscles will still be able to absorb increased nitrogen from protein sources, thus increasing muscle tissue growth and the androgenic qualities will insure that strength is maintained(7). Recovery time will also be reduced. You can still work out hard without fear of overtraining and the increased workload will lead to further improvement. In short, this means no crash and no loss of gains. Essentially, you’re still “on” but you’re recovering. Sounds perfect, doesn’t it? Well, it’s not perfect, but it’s pretty damn close to it. Never before has anything like this been possible and the potential is amazing(8).
The only drawback of using SARMS (if it even be considered a drawback) is the fact that its androgenic ratio is closer to a mild steroid such as Primobolin than it is to testosterone. So by itself, one could not and should not expect tremendous gains in mass from it. Increasing the dosage beyond 50-100 mls a day is not recommended since at that point the risk/benefit ratio shifts unfavorably – not that the side effects are severe, but that’s where continued use could lead to suppression, and then you’re defeating the purpose of using it for PCT(9)
Another steroid with which SARMS can be compared is Proviron. The main similarity in regard to the physical result is a noticeable “hardness” and increased density to the muscles. Proviron is also only mildly suppressive and then, only in high dosages for extended duration, which is why it too is a popular add-on at the end of a cycle. Neither drug can aromatize and also work as an anti estrogen. (Another advantage in PCT). The main difference between Proviron and SARMS is that Proviron is DHT based making it especially hard on the hairline and prostate -- NOT what you want when trying to restore sex drive and stamina. SARMS has been shown to cause less prostate hypertrophy than all other steroids(10). In fact, in some studies SARMS has been shown to decrease prostate weight similar to the 5 alpha reductase inhibitor, Finesteride(11). How perfect is that?
Higher dosages have also been shown to lead to vision disturbances (much like with Clomid). Still, at 50mg - 100mg a day the results are impressive and virtually side effect free. A good way to incorporate SARMS into PCT is to begin using 50mls a day at the same time as you begin using other PCT ancillaries – depending on what drugs and supplements you prefer and/or found to be effective. You then can continue using SARMS and supplements which will allow the HPTA to begin functioning on its own without the help of other drugs such as HCG or Clomid(12). The added benefit would be continued strength and libido and an increased muscularity. Instead of being a time when you experience the loss of gains, it will become a time when the gains become solidified and you can look better than ever(13).
It won’t be long before the term PCT and SARMS are inexorably linked. The way PCT is conducted will be changed forever. In fact, it already is.
REFERENCES:
Drug Discov Today. 2007 Mar;12(5-6):241-8. Epub 2007 Feb 7.
Expanding the therapeutic use of androgens via selective androgen receptor modulators (SARMs).
Gao W, Dalton JT.
Division of Pharmaceutics, College of Pharmacy, The Ohio State University, 500 W 12th Avenue, Columbus, OH 43210, USA
Expert Opin Investig Drugs. 2006 Apr;15(4):377-87.
Therapeutic potential of the SARMs: revisiting the androgen receptor for drug discovery.
Segal S, Narayanan R, Dalton JT.
1GTx, Inc., Memphis, TN 38163, USA
Curr Opin Investig Drugs. 2006 Oct;7(10):873-81.
Selective androgen receptor modulators: in pursuit of tissue-selective androgens.
Omwancha J, Brown TR.
Johns Hopkins Bloomberg School of Public Health, Department of Biochemistry and Molecular Biology, Division of Reproductive Biology, 615 North Wolfe Street, Baltimore, MD 21205, USA
J Biol Chem. 2009 Dec 25;284(52):36367-76. Epub 2009 Oct 21.
Identification of anabolic selective androgen receptor modulators with reduced activities in reproductive tissues and sebaceous glands.
Schmidt A, Harada S, Kimmel DB, Bai C, Chen F, Rutledge SJ, Vogel RL, Scafonas A, Gentile MA, Nantermet PV, McElwee-Witmer S, Pennypacker B, Masarachia P, Sahoo SP, Kim Y, Meissner RS, Hartman GD, Duggan ME, Rodan GA, Towler DA, Ray WJ.
Department of Molecular Endocrinology/Bone Biology, Merck Research Laboratories, West Point, Pennsylvania 1948, USA
Nucl Recept Signal. 2008;6:e010. Epub 2008 Nov 26.
Selective androgen receptor modulators in preclinical and clinical development.
Narayanan R, Mohler ML, Bohl CE, Miller DD, Dalton JT.
Preclinical Research and Development, GTx, Inc., Memphis, Tennessee, USA
Handb Exp Pharmacol. 2010;(195):99-126.
Synthetic anabolic agents: steroids and nonsteroidal selective androgen receptor modulators.
Thevis M, Schänzer W.
Center for Preventive Doping Research - Institute of Biochemistry, German Sport University Cologne, Am Sportpark Müngersdorf 6, 50933, Cologne, Germany
Pharmacokinetics of S-3-(4-acetylamino-phenoxy)-2-hydroxy-2-methyl-N-(4-nitro-3-trifluoromethyl-phenyl)-propionamide in rats, a non-steroidal selective androgen receptor modulator
J. D. KEARBEY,† D. WU,† W. GAO,† D. D. MILLER,‡ and J. T. DALTON†* †Division of Pharmaceutics, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA.
‡Department of Pharmaceutics, Graduate Health Sciences Center, College of Pharmacy, University of Tennessee, Memphis, TN 38163, USA
J Clin Endocrinol Metab. 1999 Oct;84(10):3459-62.
Selective androgen receptor modulators (SARMs): a novel approach to androgen therapy for the new millennium.
Negro-Vilar A.
Ligand Pharmaceuticals, Inc., San Diego, California 92121, USA
Discovery and biological characterization of a novel series of androgen receptor modulators.
Zhou C, Wu G, Feng Y, Li Q, Su H, Mais DE, Zhu Y, Li N, Deng Y, Yang D, Wang MW
Design, synthesis, and biological characterization of metabolically stable selective androgen receptor modulators.
Marhefka CA, Gao W, Chung K, Kim J, He Y, Yin D, Bohl C, Dalton JT, Miller DD
Antiandrogens in prostate cancer.
Reid P, Kantoff P, Oh W.
Lank Center for Genitourinary Oncology, Dana Farber-Partners Cancer Care, Boston, MA 02115, USA
Emerging drugs for hypogonadism.
Edelstein D, Dobs A, Basaria S.
Johns Hopkins University School of Medicine, Division of Endocrinology and Metabolism, Baltimore, MD, USA
Anabolic applications of androgens for functional limitations associated with aging and chronic illness.
Bhasin S, Storer TW
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SARMS versus Pro-Hormones and Pro steroids
Which One Wins As The Best Alternative To steroids?
When Pro-Hormones first hit the scene, anticipation was high. But it didn’t take long before it became obvious that these compounds were pretty weak in replicating the muscle building effects of real steroids. And to make matters worse, they carried most of the same negative side effects of steroids. That was not a winning combination. Over the years there were (supposed) improvements, one pretty much as bad as the next, until a new invention hit the market – the designer steroid. These didn’t act as precursors to anabolic and androgenic receptors, instead, they were actual steroids that have been manipulated in a way that they were able to get in under the wire of being classified as a controlled substance. They actually worked pretty well. And they were the best legal alternative to anabolic steroids to date. But times have changed.
Technically, Pro-hormones and pro-steroids are no longer allowed to be sold but it wouldn’t take much of a search to track some down. Many commercial health food stores still carry a copious line of pro-hormones and their collective imitators – all using various titles to manage staying commercially available. Unfortunately, these products have one major drawback. Not only are they as liver toxic as 17AA oral steroids, they’ve been shown to be kidney toxic as well. These risks should not be understated. Liver and kidney problems often go undetected until sever damage has been inflicted. Still, to many who did not want to go the route of dealing with the black market for steroids, they’re willing to take the risk since were the only choice. Until now.
The latest addition to non-steroidal muscle builders is SARMS but unlike Pro hormones or Pro steroids, they aren’t an imitation of steroids -- they’re an improvement. And they aren’t being promoted by amateur chemists and supplement companies. Some of the top scientists and pharmaceutical companies are working on getting this to the market. But it’s available NOW. (For research purposes).
SARMS (Selective Androgen Receptor Modulators ) are a unique class of androgen receptor molecules. The intent is to have the same effects as steroids but are much more “selective” in their action – similar to testosterone but without the negative side effects, most notably prostate enlargement and possible carcinoma. Another benefit is that no injection is required. It comes in a non-toxic oral form that has a half-life of between 2.6 and 5.3 hours(1). The goal is to allow the customized response of entering muscle tissue that are the target of the therapy which in return will respond as they would to testosterone. Other tissues where undesirable side effects (such as the prostate) are produced will not be affected(2). To add to the benefits a new class of sarms called "sarms S-4" has shown to have little to no effect on the hpta unlike pro hormones or designer steroids. This means no post cycle therapy is needed after a cycle of S-4 and potensaily life long complications are avoided(3). S-4 has also shown little to no ability to convert to estrogen so gyno "a common problem with pro hormones" is also avoided(4).
To many researchers, scientist, pharmacologists and just about anyone familiar with anabolic enhancement, this is obviously a huge leap in the area of anabolic/androgenic enhancement. Whereas pro-hormones were sort-of like steroids, in that they create a facsimile some of the effects, SARMS delivers steroid-like results in a big way. Comparing SARMS to pro-hormones is like comparing a 47” HD flat screen Television to a 12” black and white TV with tubes. There’s just no way one isn’t light years better than the other.(5) And everyone who has tried both would agree.
Pro-Hormones and Pro-steroids are all based on a flawed principle – attempted to act similarly to steroids, yet avoid classification by altering some of the molecular structure. That’s the problem. Once you alter a molecule chain, it changes everything. And although some of the effects may remain, it’s essentially a fraudulent version of what you’re attempting to replicate. Pro hormones are actually discarded forms of steroids. The pharmaceutical companies deemed them so inferior they abandoned the technology. It was this same technology that was resurrected for no other reason other than to get a drug on the market that could be sold as a supplement. SARMS is the opposite. It isn’t an imitation. It’s the next stage(6). Because Pro Hormones and designer steroids are made to be "like steroids" or are in fact a steroid analog they pose the problem of making WADA tested athletes test positive for steroids when tested. Sarms S-4 however does no such thing and to this date there is no way to test for Sarms S-4 ether in a athletes blood or urine So a athlete can safely take S-4 without fear of testing hot for a wada banned substance.
SARMS.were developed for the same reasons as steroids – to prevent muscle wasting through increased nitrogen retention. The main difference is that instead of using the old technology on which all steroid are based, it incorporated state of the art discoveries. The results were astonishing – so much so that research has begun in the medical community in Europe and the results have been extremely positive. Those more adventurous individuals have already begun incorporating SARMS for muscle building purposes and Hormone Replacement. And it looks as if SARMS is here to stay.
SARMS produces what many consider “high quality” muscle. The gains are very solid, unlike the results from many pro-hormones that are mostly water weight. SARMS also has the added benefit of not being capable of aromatizing to estrogen(7).
It’s arguable that SARMS is actually superior to pharmaceutical grade steroids. 50-100 mg a day will yield a similar result to 25- 50mg of an oral steroid like turinabol, but without the toxicity. Be that as it may, it’s evident that a cycle of SARMS far superior to any pro-hormone or pro-steroid.
So there’s really no contest here. SARMS blows away any Pro-hormone or OTC Pro-steroid on the market. One cycle is all it‘ll take to convince you.
REFERENCES:
resorption in rats. AAPS Pharm Sci. 2003;5 Abstract R6167.
9.Marhefka CA, Gao W, Chung K, Kim J, He Y, Yin D, Bohl C, Dalton JT, Miller DD. Design, synthesis, and biological characterization of metabolically stable selective androgen receptor modulators. Journal of Medicinal Chemistry. 2003
Yin D, Gao W, Kearbey JD, Xu H, Chung K, He Y, Marhefka CA, Veverka KA, Miller DD, Dalton JT. Pharmacodynamics of selective androgen receptor modulators. Journal of Pharmacology and Experimental Therapeutics. 2003;304:1334–1340. [PubMed
Endocrinology. 2005 Nov;146(11):4887-97. Epub 2005 Aug 11.
Selective androgen receptor modulator treatment improves muscle strength and body composition and prevents bone loss in orchidectomized rats.
Gao W, Reiser PJ, Coss CC, Phelps MA, Kearbey JD, Miller DD, Dalton JT.
Division of Pharmaceutics, College of Pharmacy and Department of Oral Biology, The Ohio State University, 500 West 12th Avenue, L. M. Parks Hall, Room 242, Columbus, Ohio 43210, USA
Pharmacokinetics of S-3-(4-acetylamino-phenoxy)-2-hydroxy-2-methyl-N-(4-nitro-3-trifluoromethyl-phenyl)-propionamide in rats, a non-steroidal selective androgen receptor modulator
J. D. KEARBEY,† D. WU,† W. GAO,† D. D. MILLER,‡ and J. T. DALTON†*
†Division of Pharmaceutics, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA.
‡Department of Pharmaceutics, Graduate Health Sciences Center, College of Pharmacy, University of Tennessee, Memphis, TN 38163, USA
Selective androgen receptor modulator treatment improves muscle strength and body composition and prevents bone loss in orchidectomized rats.
Gao W, Reiser PJ, Coss CC, Phelps MA, Kearbey JD, Miller DD, Dalton JT.
Division of Pharmaceutics, College of Pharmacy and Department of Oral Biology, The Ohio State University, 500 West 12th Avenue, L. M. Parks Hall, Room 242, Columbus, Ohio 43210, USA
In vivo metabolism and final disposition of a novel nonsteroidal androgen in rats and dogs.
Perera MA, Yin D, Wu D, Chan KK, Miller DD, Dalton J.
Division of Pharmaceutics, College of Pharmacy, The Ohio State University, 500 West 12th Ave., Columbus, OH 43210, USA
Pharmacokinetics of S-3-(4-acetylamino-phenoxy)-2-hydroxy-2-methyl-N-(4-nitro-3-trifluoromethyl-phenyl)-propionamide in rats, a non-steroidal selective androgen receptor modulator
J. D. KEARBEY,† D. WU,† W. GAO,† D. D. MILLER,‡ and J. T. DALTON†*
†Division of Pharmaceutics, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA.
‡Department of Pharmaceutics, Graduate Health Sciences Center, College of Pharmacy, University of Tennessee, Memphis, TN 38163, USA.