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DJLegacy2k1
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Study #1:
Suppression of natural testosterone production is a concern. While many have the impression that S-4 completely lacks suppressive activity at the hypothalamus and pituitary regardless of the dose, this notion is unsupported by the research. This preliminary (link) study on S-4 found that "The activities of S-4 on LH and FSH were similar to those produced by [testosterone propionate] TP. S-1 and S-4 partially suppressed LH production at dose rates of 0.5 mg/day or higher." An absolute dose of 0.5 mg/day is equivalent to 1.9 mg/kg/day in the rats studied. When corrected for body surface area and converted to dosing for humans, that's 0.31 mg/kg (1.9 * 0.162). As a theoretical extrapolation to a 200 lb (91kg) man, a dose of only 28 mg/day would start to "partially suppress LH production." Reports of suppression at only 50mg/day are consistent with the research on S-4.
Im working on getting the link to the study working...HERE: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2040238/?tool=pubmed
Study #2: http://pubs.acs.org/doi/abs/10.1021/jm900280m
3602 Journal of Medicinal Chemistry, 2009, Vol. 52, No. 12 Award Address
Nonsteroidal Selective Androgen Receptor Modulators (SARMs): Dissociating the Anabolic and Androgenic Activities of the Androgen Receptor for Therapeutic Benefit - Journal of Medicinal Chemistry (ACS Publications)
Section 1.5.2. Nonsteroidal AR Agonists. The Propionamides.
..the resulting compound known
in the literature as S-4 and in press releases as andarine (S-3-(4-acetylaminophenoxy)-2-hydroxy-2-methyl-N-(4-nitro-3-
trifluoromethylphenyl)propionamide) was
shown to possess SARM activity and allowed the pharmacodynamic exploration of this novel class of drugs.
Section 2.1.7. Andarine, the Prototypical Full Efficacy SARM.
Andarine was a SARM that served as the predominant model compound early in the development of the SARM field. Many of the landmark studies with andarine served as proofs-of-concept in the SARM field (e.g., concomitant myo- and osteoanabolism in the absence of VP proliferation, musculoskeletal performance enhancement, etc.). Preclinical characterization of andarine demonstrated high binding affinity for AR (Ki ) 4 nM) and ideal pharmacokinetics (complete oral bioavailability, plasma half-life consistent with daily oral dosing in rats and dogs) with no cross-reactivity with the other nuclear receptors. Myoanabolism was demonstrated in terms of maintenance and restoration of LA weight and restoration of soleus muscle strength in castrated rats. Likewise, osteoanabolism was observed in maintenance and restorative modes in male and female rats with improvements in biomechanical strength, cumulatively demonstrating musculoskeletal performance enhancement. The anabolic effects were also observed at the level of the entire organism as revealed by favorable body composition changes. Importantly, these anabolic effects were tissue-selective when compared to androgenic tissue and HPG axis effects, establishing andarine as a prototypical preclinical SARM. The peripheral and selective anabolic preclinical pharmacodynamic profile of andarine seemed highly promising and stimulated us to pursue landmark clinical trials of the SARMs, andarine and Ostarine. Although phase I studies with andarine were successful with no deficiencies noted , Ostarine was selected for advanced clinical development based on corporate strategy. Readers are cautioned to note that the name Ostarine is often mistakenly linked to the chemical structure of andarine. The chemical structure of Ostarine has not been publicly disclosed. The authors are unable to provide additional information. Collectively, these preclinical and clinical studies have provided the foundation for the massive body of SARM characterizations that are now published and patented (discussed below). Importantly, many of these pharmacodynamic observations have proven to be typical of subsequently published chemodiverse SARMs, as discussed in section 3.
-Legacy
Suppression of natural testosterone production is a concern. While many have the impression that S-4 completely lacks suppressive activity at the hypothalamus and pituitary regardless of the dose, this notion is unsupported by the research. This preliminary (link) study on S-4 found that "The activities of S-4 on LH and FSH were similar to those produced by [testosterone propionate] TP. S-1 and S-4 partially suppressed LH production at dose rates of 0.5 mg/day or higher." An absolute dose of 0.5 mg/day is equivalent to 1.9 mg/kg/day in the rats studied. When corrected for body surface area and converted to dosing for humans, that's 0.31 mg/kg (1.9 * 0.162). As a theoretical extrapolation to a 200 lb (91kg) man, a dose of only 28 mg/day would start to "partially suppress LH production." Reports of suppression at only 50mg/day are consistent with the research on S-4.
Im working on getting the link to the study working...HERE: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2040238/?tool=pubmed
Study #2: http://pubs.acs.org/doi/abs/10.1021/jm900280m
3602 Journal of Medicinal Chemistry, 2009, Vol. 52, No. 12 Award Address
Nonsteroidal Selective Androgen Receptor Modulators (SARMs): Dissociating the Anabolic and Androgenic Activities of the Androgen Receptor for Therapeutic Benefit - Journal of Medicinal Chemistry (ACS Publications)
Section 1.5.2. Nonsteroidal AR Agonists. The Propionamides.
..the resulting compound known
in the literature as S-4 and in press releases as andarine (S-3-(4-acetylaminophenoxy)-2-hydroxy-2-methyl-N-(4-nitro-3-
trifluoromethylphenyl)propionamide) was
shown to possess SARM activity and allowed the pharmacodynamic exploration of this novel class of drugs.
Section 2.1.7. Andarine, the Prototypical Full Efficacy SARM.
Andarine was a SARM that served as the predominant model compound early in the development of the SARM field. Many of the landmark studies with andarine served as proofs-of-concept in the SARM field (e.g., concomitant myo- and osteoanabolism in the absence of VP proliferation, musculoskeletal performance enhancement, etc.). Preclinical characterization of andarine demonstrated high binding affinity for AR (Ki ) 4 nM) and ideal pharmacokinetics (complete oral bioavailability, plasma half-life consistent with daily oral dosing in rats and dogs) with no cross-reactivity with the other nuclear receptors. Myoanabolism was demonstrated in terms of maintenance and restoration of LA weight and restoration of soleus muscle strength in castrated rats. Likewise, osteoanabolism was observed in maintenance and restorative modes in male and female rats with improvements in biomechanical strength, cumulatively demonstrating musculoskeletal performance enhancement. The anabolic effects were also observed at the level of the entire organism as revealed by favorable body composition changes. Importantly, these anabolic effects were tissue-selective when compared to androgenic tissue and HPG axis effects, establishing andarine as a prototypical preclinical SARM. The peripheral and selective anabolic preclinical pharmacodynamic profile of andarine seemed highly promising and stimulated us to pursue landmark clinical trials of the SARMs, andarine and Ostarine. Although phase I studies with andarine were successful with no deficiencies noted , Ostarine was selected for advanced clinical development based on corporate strategy. Readers are cautioned to note that the name Ostarine is often mistakenly linked to the chemical structure of andarine. The chemical structure of Ostarine has not been publicly disclosed. The authors are unable to provide additional information. Collectively, these preclinical and clinical studies have provided the foundation for the massive body of SARM characterizations that are now published and patented (discussed below). Importantly, many of these pharmacodynamic observations have proven to be typical of subsequently published chemodiverse SARMs, as discussed in section 3.
-Legacy
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