Colbert
New member
I found this article about SARMs on a blog and thought I it would be a good idea to share it.
Link:
Need To Build Muscle Inc. Official Blog
Enjoy!
Needtogetaas Does Selective Androgen Receptor Modulators (S.A.R.Ms)
Posted by Needtogetaas | June 17th, 2011
Selective Androgen Receptor Modulators (S.A.R.Ms) provide the positives of testosterone including and not limited to increased muscle mass, fat loss, and bone density; while preventing the negative side effects of androgens which include prostats issues, hair loss, acne, and liver problems. The Androgen Receptor is the receptor that androgens such as testosterone and DHT bind to. The bounded androgen receptors will combine with another androgen receptor to travel the nucleuos an androgen cell where gene transcription of DNA to RNA takes place. This is the process in which androgenic hormones exert their anabolic effects on muscle tissue. SARMs have the capability to take the place of the androgen, and as a result; bring forth plenty of the same positive effects on muscle tissue as anabolic steroids like testosterone and DHT. Steroidal SARMs have been around since the 1940s, a lot of nonsteroidal SARMs do not provide as substrates for CYP19 aromatase enzyme or 5***945;-reductase enzyme which acts as full agonists in muscle and bone and as partial agonists in prostate are currently in development. The differing interactions of steroidal and nonsteroidal compounds with AR contribute to their specific pharmacologic actions. Ligand binding induces specific conformational changes in the ligand binding domain, which could modulate exterior topology and protein-protein interactions between AR and co-regulators, leading to tissue-specific gene regulation. Preclinical studies have demonstrated the ability of SARMs to increase muscle and bone mass dramatically in preclinical rat models with constant changing of prostate sparing. Phase I trials of SARMs in humans have also reported significant increases in lean body mass.
Selective Androgen Receptor Modulators (S.A.R.Ms) S-4
Anadrine is a S.A.R.M or SARM for shot, which is a selective androgen receptor modulator with one of the most androgenic, being 1/3 the strength as of testosterone at binding to the androgen receptor. Acetamidoxolutamide or S4 is fast acting and its half life is of 4 hours. It may be able to reduce the size of prostate if used at a honest dosage which is why SARM’s is being looked at as replacement for Androgen Deprived Therapy or ADT for short. One of s4’s great attributes is the fact that it causes a drying out/hardening effect of the muscle along the tightening of the skin. It does in turn bind extremely well to the androgen muscle tissue receptors, leading to more lean body mass which is why you as bodybuilder would want to get your hands on some as quickly as possible
S4 creates drastic fat loss by binding to the androgen receptors it allows for fat to be oxidized, part of the reason why one dries out so well while using it, the other part being that it does not aromatize. Common side effects with SARMS Is blurred night vision or vision becoming all one color at night. This is do to its minding to cretin receptors and gene transcription however side effects quickly subside after use. Side effects with SARMS are more often seen when dosing is on the high end but some reports have been made even with low level doses. As often the case You will never know how you will react until you have tried it for your self.
Selective Androgen Receptor Modulators (S.A.R.Ms) S-1
Ostarine sARM displays plenty of promise at promoting lean body mass, its extremely potent, has a long half life, and displays no androgenic effects. In other words; it’s purely anabolic, something I know women would love to hear especially if they are looking to build muscle while keeping a feminine appeal. It binds strongly to the androgen receptor, but without the side effects normaly associated with high levels of DHT. It shows considerable properties as a hardening agent just slightly less than those of S4, wich itself is 1/3 as androgenic as Testosterone. Its ability to cause fat los means it can be used on a cutting cycle and can be stacked effectivley with thermogenic or or nervous system stimulators.
It’s ability to help heal those with debilitating injuries, and to speed up injury recovery makes its medicinal purposes highly demanded. Not to mention that this is without all the negative impact on your cholesterol, blood pressure, hair line/scalp, prostate, heart or any other bodily organ. Something to note is among the currently studied SARMs, Ostarine (mk 2866) recently showed, in a successful completed phase II clinical trial, to significantly increase the lean body mass aka LBM and physical performance compared to baseline in patient of both sexes affected by the cancer cachexia. They also had a reduction in serum lipids and LDL/HDL in the low cardiovascular risk class; these results can be extended to the bone in elderly men and postmenopausal women. These findings suggest that Ostarine may be useful for other conditions, only time will tell.
Nonsteroidal selective androgen receptor modulator Ostarine™ in cancer cachexia
Cancer cachexia is a complex syndrome, affecting up to 60% of the approximately 1.4 million patients diagnosed with cancer each year in the USA. This condition is characterized by progressive deterioration of a patient’s nutritional status, weight loss, anorexia, diminished quality of life and increased mortality and morbidity. Current therapy with progestational, anti-inflammatory and anabolic agents is often ineffective and has a large number of undesirable effects. The newly developed nonsteroidal selective androgen receptor modulator Ostarine™ has demonstrated promising results in Phase I and II clinical trials, increasing total lean body mass, enhancing functional performance and decreasing total tissue percent fat. This selective androgen receptor modulator may have the ability to perform as a potent anabolic agent with minimal side effects on other organs (prostate and hair follicles), thus presenting a new strategy in managing cancer cachexia. However, more extensive data is required before its efficacy is confirmed. (October 2009, Vol. 5, No. 8, Pages 1211-1220)
In a study, S1 and S4 are partial agonists; thus, in intact male rats, S1 and S4 compete with endogenous androgens and act as antagonists in prostate, such SARMs with antagonistic or low intrinsic activity in prostate might be useful in the treatment of BPH or prostate cancer. The suppressive effects of this class of SARMs on gonadotropin secretion in rats suggest potential application for male contraception. (Endocrinology. 2004;145:5420–5428.) Of course it would take more than 70mgs of S4 a day to have the SARM compete with one’s own endogenous androgen production. It would take a serious dose of S1 (over 30mgs) to see a drop in endogenous androgen production. If you look at the study, the main suppression of androgens was within the prostate which actually prevents BPH and prostate cancer. If you read this study you will see you get the good of androgens, and the bad of androgens gets taken out of the equation.
The discovery and development of SARMs provides the opportunity to design molecules that are not only orally active, but that target AR in different tissues to elicit the desired activity for each of the key indications benefiting from androgen therapy. For simplicity, we have listed the desired activity in tissues or specific parameters for one specific indication (i.e., male hypogonadism) side by side with a category for selected indications. The latter provides a menu of choices for the design of molecules that can address very specific needs in the treatment of different disorders. Thus, we envision that an ideal SARM for the treatment of primary or secondary male hypogonadism would have the following profile: orally active, ideally with a pharmacokinetic profile consistent with once a day administration, capable of stimulating prostate, seminal vesicles, and other sex accessory tissues at doses equipotent to those needed to provide increases in muscle mass and strength and fat-free mass, support bone growth, and maintain/restore libido, virilization, and male habitus. Unlike testosterone which, when converted to DHT in the prostate has an enhanced proliferative activity in relation to other peripheral tissues, these SARMs are not substrates for 5***945;-reductase activity, nor do they affect the activity of the enzyme. Other activities that are considered undesirable should be diminished or eliminated, such as potential liver toxicity, blood pressure effects and fluid retention, induction of gynecomastia, and overstimulation of erythropoiesis. On the other hand, use of SARMs for selected indications provides the rationale for developing molecules with distinct tissue specificity. For example, if the target is bone growth in elderly men with osteopenia or osteoporosis, but with no overt signs of hypogonadism, a more anabolic SARM with clear effects on bone and muscle, but lesser activity on prostate or other sex accessory tissues would be more desirable. (Negro-Vilar 84 (10): 3459)
I think that it is safe to say that 50mgs of Anadrine or 10mgs of Ostarine will not suppress the HTPA while enhancing protein synthesis, binding to muscle tissue and enhancing lean body mass. However keep in mind the administration of any outside androgens may not suppress the bodies production but it can and will hinder its recovery. So it is in my opinion that no form of SARMS should be used during the final recovery (post cycle therapy) stage of a cycle. SARMS are best used during a cycle, as a stand alone cycle, Pre post cycle therapy (pct), Or post pct as a bridge between cycles to keep ones gains.Wich brings us to our next topic, SARMs being used as a bridge in between cycles.
Used as a Bridge
A bridge is basically a description for using any anabolic agent that will help one preserve or add on the gains from your last anabolic androgenic steroid cycle until you make the initiation of starting your next cycle. A bridge between cycles is usually anywhere from 4-12 weeks depending on the individual’s purpose. Everyone’s opinion on bridges varies, some may feel it is a waste, others feel it can be a lot of money. For the serious bodybuilder or anyone serous about keeping their gains, a bridge is a must but many bodybuilders would have used a less suppressive androgenic anabolic steroid to preserve gains. The problem with that is that if you plans are to recover your HPTA from your last cycle, taking a exogenous hormone will not allow you to recover properly. Even Primobolan which has been touted to be the least suppressive of all steroids has been documented to decrease GnRH significantly with continuous use. So using it in the morning for the anabolic window response is out of question, even though you may be able to recover a solid amount of your endogenous hormones during sleep, which is only a theory and does not have clinical evidence backing it up. That is where SARM’s come in; preferably S-1 as it is virtually non-toxic and has a faster response in creating an anabolic environment. I suggest no more than 5-10mgs for your bridge, trust me, this dose range will be all that you need to maintain your gains and even add on gains till your next cycle. If you wanted to use SARMS S4 as a bridge then 25mg every day would be the perfect dose.
For the average chemically enhanced person SARMS is yet another tool we have at our disposal to achieve our goals and keep our gains. The most effective use for SARMS is of course the bridge. I have seen the Dbal bridge, Primo bridge, Masterone bridge , Tbol bridge, var/anavar bridge and every bridge you can think of. In my opinion the perfect bridge is ether 5mg-10mg S1 or 25mg S4 combined with Needtobuildmuscle’s Bridge 1 cap 3 times daily. This combination will give you every single effect as if still being on cycle well at the same time not shut down your hpta . Think about what being on cycle is like.
Your body is in a anabolic state, You feel a heightened sense of well being, You have accelerated nutrition retention, More blood volume and better blood oxygen levels, and you have more strength and endurance. A SARMS + Needtobuildmuscle Bridge combination gives you all of this and more. You can read more about bridge and purchase the product here Bridge . For sarms You can find good quality SARMS here Uniquemicals
As always my friends never stop killing that sh*t!
Link:
Need To Build Muscle Inc. Official Blog
Enjoy!
Needtogetaas Does Selective Androgen Receptor Modulators (S.A.R.Ms)
Posted by Needtogetaas | June 17th, 2011
Selective Androgen Receptor Modulators (S.A.R.Ms)
Selective Androgen Receptor Modulators (S.A.R.Ms) provide the positives of testosterone including and not limited to increased muscle mass, fat loss, and bone density; while preventing the negative side effects of androgens which include prostats issues, hair loss, acne, and liver problems. The Androgen Receptor is the receptor that androgens such as testosterone and DHT bind to. The bounded androgen receptors will combine with another androgen receptor to travel the nucleuos an androgen cell where gene transcription of DNA to RNA takes place. This is the process in which androgenic hormones exert their anabolic effects on muscle tissue. SARMs have the capability to take the place of the androgen, and as a result; bring forth plenty of the same positive effects on muscle tissue as anabolic steroids like testosterone and DHT. Steroidal SARMs have been around since the 1940s, a lot of nonsteroidal SARMs do not provide as substrates for CYP19 aromatase enzyme or 5***945;-reductase enzyme which acts as full agonists in muscle and bone and as partial agonists in prostate are currently in development. The differing interactions of steroidal and nonsteroidal compounds with AR contribute to their specific pharmacologic actions. Ligand binding induces specific conformational changes in the ligand binding domain, which could modulate exterior topology and protein-protein interactions between AR and co-regulators, leading to tissue-specific gene regulation. Preclinical studies have demonstrated the ability of SARMs to increase muscle and bone mass dramatically in preclinical rat models with constant changing of prostate sparing. Phase I trials of SARMs in humans have also reported significant increases in lean body mass.
Selective Androgen Receptor Modulators (S.A.R.Ms) S-4
Anadrine is a S.A.R.M or SARM for shot, which is a selective androgen receptor modulator with one of the most androgenic, being 1/3 the strength as of testosterone at binding to the androgen receptor. Acetamidoxolutamide or S4 is fast acting and its half life is of 4 hours. It may be able to reduce the size of prostate if used at a honest dosage which is why SARM’s is being looked at as replacement for Androgen Deprived Therapy or ADT for short. One of s4’s great attributes is the fact that it causes a drying out/hardening effect of the muscle along the tightening of the skin. It does in turn bind extremely well to the androgen muscle tissue receptors, leading to more lean body mass which is why you as bodybuilder would want to get your hands on some as quickly as possible
S4 creates drastic fat loss by binding to the androgen receptors it allows for fat to be oxidized, part of the reason why one dries out so well while using it, the other part being that it does not aromatize. Common side effects with SARMS Is blurred night vision or vision becoming all one color at night. This is do to its minding to cretin receptors and gene transcription however side effects quickly subside after use. Side effects with SARMS are more often seen when dosing is on the high end but some reports have been made even with low level doses. As often the case You will never know how you will react until you have tried it for your self.
Selective Androgen Receptor Modulators (S.A.R.Ms) S-1
Ostarine sARM displays plenty of promise at promoting lean body mass, its extremely potent, has a long half life, and displays no androgenic effects. In other words; it’s purely anabolic, something I know women would love to hear especially if they are looking to build muscle while keeping a feminine appeal. It binds strongly to the androgen receptor, but without the side effects normaly associated with high levels of DHT. It shows considerable properties as a hardening agent just slightly less than those of S4, wich itself is 1/3 as androgenic as Testosterone. Its ability to cause fat los means it can be used on a cutting cycle and can be stacked effectivley with thermogenic or or nervous system stimulators.
It’s ability to help heal those with debilitating injuries, and to speed up injury recovery makes its medicinal purposes highly demanded. Not to mention that this is without all the negative impact on your cholesterol, blood pressure, hair line/scalp, prostate, heart or any other bodily organ. Something to note is among the currently studied SARMs, Ostarine (mk 2866) recently showed, in a successful completed phase II clinical trial, to significantly increase the lean body mass aka LBM and physical performance compared to baseline in patient of both sexes affected by the cancer cachexia. They also had a reduction in serum lipids and LDL/HDL in the low cardiovascular risk class; these results can be extended to the bone in elderly men and postmenopausal women. These findings suggest that Ostarine may be useful for other conditions, only time will tell.
Here is the abtract for more proof of its positive effects:
Nonsteroidal selective androgen receptor modulator Ostarine™ in cancer cachexia
Cancer cachexia is a complex syndrome, affecting up to 60% of the approximately 1.4 million patients diagnosed with cancer each year in the USA. This condition is characterized by progressive deterioration of a patient’s nutritional status, weight loss, anorexia, diminished quality of life and increased mortality and morbidity. Current therapy with progestational, anti-inflammatory and anabolic agents is often ineffective and has a large number of undesirable effects. The newly developed nonsteroidal selective androgen receptor modulator Ostarine™ has demonstrated promising results in Phase I and II clinical trials, increasing total lean body mass, enhancing functional performance and decreasing total tissue percent fat. This selective androgen receptor modulator may have the ability to perform as a potent anabolic agent with minimal side effects on other organs (prostate and hair follicles), thus presenting a new strategy in managing cancer cachexia. However, more extensive data is required before its efficacy is confirmed. (October 2009, Vol. 5, No. 8, Pages 1211-1220)
Slightly Suppressive or NOT
In a study, S1 and S4 are partial agonists; thus, in intact male rats, S1 and S4 compete with endogenous androgens and act as antagonists in prostate, such SARMs with antagonistic or low intrinsic activity in prostate might be useful in the treatment of BPH or prostate cancer. The suppressive effects of this class of SARMs on gonadotropin secretion in rats suggest potential application for male contraception. (Endocrinology. 2004;145:5420–5428.) Of course it would take more than 70mgs of S4 a day to have the SARM compete with one’s own endogenous androgen production. It would take a serious dose of S1 (over 30mgs) to see a drop in endogenous androgen production. If you look at the study, the main suppression of androgens was within the prostate which actually prevents BPH and prostate cancer. If you read this study you will see you get the good of androgens, and the bad of androgens gets taken out of the equation.
In this study below, SARMs are being used as a replacement for Testosterone Replacement Therapy.
Currently used androgenic formulations for replacement therapy are largely restricted to injectable or skin delivery formulations of testosterone or testosterone esters. Marketed injectable forms of testosterone esters (such as testosterone enanthate, propionate, or cypionate) produce undesirable fluctuations in testosterone blood levels, with supraphysiological concentrations early, and subnormal levels towards the end of the period before the next injection, providing an unsatisfactory profile and in some cases undesired side effects. Skin patches do provide a better blood level profile of testosterone, but skin irritation and daily application still limit the usefulness and acceptability of this form of therapy. Oral preparations such as fluoxymesterone and 17***945;-methyltestosterone are not currently used due to concerns about liver toxicity linked to the 17***945;-alkyl group and because of somewhat lower efficacy. Thus, these compounds are considered obsolete and do not represent a viable form of therapy.
The discovery and development of SARMs provides the opportunity to design molecules that are not only orally active, but that target AR in different tissues to elicit the desired activity for each of the key indications benefiting from androgen therapy. For simplicity, we have listed the desired activity in tissues or specific parameters for one specific indication (i.e., male hypogonadism) side by side with a category for selected indications. The latter provides a menu of choices for the design of molecules that can address very specific needs in the treatment of different disorders. Thus, we envision that an ideal SARM for the treatment of primary or secondary male hypogonadism would have the following profile: orally active, ideally with a pharmacokinetic profile consistent with once a day administration, capable of stimulating prostate, seminal vesicles, and other sex accessory tissues at doses equipotent to those needed to provide increases in muscle mass and strength and fat-free mass, support bone growth, and maintain/restore libido, virilization, and male habitus. Unlike testosterone which, when converted to DHT in the prostate has an enhanced proliferative activity in relation to other peripheral tissues, these SARMs are not substrates for 5***945;-reductase activity, nor do they affect the activity of the enzyme. Other activities that are considered undesirable should be diminished or eliminated, such as potential liver toxicity, blood pressure effects and fluid retention, induction of gynecomastia, and overstimulation of erythropoiesis. On the other hand, use of SARMs for selected indications provides the rationale for developing molecules with distinct tissue specificity. For example, if the target is bone growth in elderly men with osteopenia or osteoporosis, but with no overt signs of hypogonadism, a more anabolic SARM with clear effects on bone and muscle, but lesser activity on prostate or other sex accessory tissues would be more desirable. (Negro-Vilar 84 (10): 3459)
I think that it is safe to say that 50mgs of Anadrine or 10mgs of Ostarine will not suppress the HTPA while enhancing protein synthesis, binding to muscle tissue and enhancing lean body mass. However keep in mind the administration of any outside androgens may not suppress the bodies production but it can and will hinder its recovery. So it is in my opinion that no form of SARMS should be used during the final recovery (post cycle therapy) stage of a cycle. SARMS are best used during a cycle, as a stand alone cycle, Pre post cycle therapy (pct), Or post pct as a bridge between cycles to keep ones gains.Wich brings us to our next topic, SARMs being used as a bridge in between cycles.
Used as a Bridge
A bridge is basically a description for using any anabolic agent that will help one preserve or add on the gains from your last anabolic androgenic steroid cycle until you make the initiation of starting your next cycle. A bridge between cycles is usually anywhere from 4-12 weeks depending on the individual’s purpose. Everyone’s opinion on bridges varies, some may feel it is a waste, others feel it can be a lot of money. For the serious bodybuilder or anyone serous about keeping their gains, a bridge is a must but many bodybuilders would have used a less suppressive androgenic anabolic steroid to preserve gains. The problem with that is that if you plans are to recover your HPTA from your last cycle, taking a exogenous hormone will not allow you to recover properly. Even Primobolan which has been touted to be the least suppressive of all steroids has been documented to decrease GnRH significantly with continuous use. So using it in the morning for the anabolic window response is out of question, even though you may be able to recover a solid amount of your endogenous hormones during sleep, which is only a theory and does not have clinical evidence backing it up. That is where SARM’s come in; preferably S-1 as it is virtually non-toxic and has a faster response in creating an anabolic environment. I suggest no more than 5-10mgs for your bridge, trust me, this dose range will be all that you need to maintain your gains and even add on gains till your next cycle. If you wanted to use SARMS S4 as a bridge then 25mg every day would be the perfect dose.
Making it simple for the user. A SARMS summer.
For the average chemically enhanced person SARMS is yet another tool we have at our disposal to achieve our goals and keep our gains. The most effective use for SARMS is of course the bridge. I have seen the Dbal bridge, Primo bridge, Masterone bridge , Tbol bridge, var/anavar bridge and every bridge you can think of. In my opinion the perfect bridge is ether 5mg-10mg S1 or 25mg S4 combined with Needtobuildmuscle’s Bridge 1 cap 3 times daily. This combination will give you every single effect as if still being on cycle well at the same time not shut down your hpta . Think about what being on cycle is like.
Your body is in a anabolic state, You feel a heightened sense of well being, You have accelerated nutrition retention, More blood volume and better blood oxygen levels, and you have more strength and endurance. A SARMS + Needtobuildmuscle Bridge combination gives you all of this and more. You can read more about bridge and purchase the product here Bridge . For sarms You can find good quality SARMS here Uniquemicals
As always my friends never stop killing that sh*t!
