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Bristol Meyers Squibb has developed a hydantoine type SARM named (7R,7aS) 2-chloro-4 (7-hydroxy-1,3-dioxotetrahydropyrrolo[1,2c]imidazol-2-yl) 3-methyl-benzonitrile, with the codename BMS 564929. [4] The synthesis of BMS 564929 is rather complicated. The right and the left part of the molecule each take five steps. Another three steps are necessary to put the two halves together and to finish the molecule.
BMS 564929 binds well to the androgen receptor and not to the other steroid receptors. BMS 564929 has no interactions with SHBG and it does not inhibit aromatase. Tests with rats show a better anabolic activity then testosterone propionate at the same dose, and a low androgenic activity. At higher doses BMS 564929 does inhibit the hypothalamus and\or the pituary and in this way lowers the secretion of LH and FSH.
An X-ray of the complex of BMS 564929 with the LBD of the androgen receptor shows some differences between BMS 564929 and dihydrotestosterone in their interaction with the LBD of the receptor. These differences seem to be large enough to enable mediation of the anabolic effect in the muscles and not the androgenic effect in the prostate. It is not yet completely clear how to explain all the differences.
BMS 564929 is orally available and metabolic transformations are slower then in the proionamide SARM's. The halflife time varies from eight to fourteen hours, and a low dose is possible.
20. Selective Androgen Receptor Modulators (SARM's)
**broken link removed**
Can anyone here synthesize this baby for research purposes??
BMS 564929 binds well to the androgen receptor and not to the other steroid receptors. BMS 564929 has no interactions with SHBG and it does not inhibit aromatase. Tests with rats show a better anabolic activity then testosterone propionate at the same dose, and a low androgenic activity. At higher doses BMS 564929 does inhibit the hypothalamus and\or the pituary and in this way lowers the secretion of LH and FSH.
An X-ray of the complex of BMS 564929 with the LBD of the androgen receptor shows some differences between BMS 564929 and dihydrotestosterone in their interaction with the LBD of the receptor. These differences seem to be large enough to enable mediation of the anabolic effect in the muscles and not the androgenic effect in the prostate. It is not yet completely clear how to explain all the differences.
BMS 564929 is orally available and metabolic transformations are slower then in the proionamide SARM's. The halflife time varies from eight to fourteen hours, and a low dose is possible.
20. Selective Androgen Receptor Modulators (SARM's)
**broken link removed**
Can anyone here synthesize this baby for research purposes??
