guardianactual
MuscleChemistry Registered Member
Dimethandrolone is a new UGL steroid derivative of nanolone. I came across it on my aas source, they just started selling it. Here's what is said about it.
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</br> Monster anabolic dimethandrolone does not aromatize
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</br> The prospects for the new anabolic steroid dimethandrolone – full name 7a,11b-dimethyl-19-nortestosterone – are looking increasingly good. According to researchers at US-based Bioqual, the chance of users being subjected to oestrogenic side-effects is nil. In test-tube experiments dimethandrolone did not convert into oestrogenic compounds.
</br>
</br> Dimethandrolone is a nandrolone-type of compound with two extra methyl groups on C7 and C11. These methyl groups make dimethandrolone a really powerful porcupine anabolic. Bioqual researchers published results of an animal study on dimethandrolone already in 2006. [Endocrinology. 2006 Jun;147(6):3016-26.] These showed that dimethandrolone has a powerful anabolic effect, it doesn’t affect the prostate and also has a considerable progesterone-like effect. According to another study that is now four years old, dimethandrolone is 136 times more powerful than testosterone. [Bioorg Med Chem Lett. 2005 Feb 15;15(4):1213-6.]
</br>
</br> Yeehaw. At congresses on male contraceptives, though, researchers have reported contradictory effects on the fertility of experimental animals that were given dimethandrolone. When given low doses, animals become sterile, but apparently not when given high doses. [Science Daily October 1, 2007]
</br>
</br> In a study that will soon appear in the Journal of Steroid Biochemistry and Molecular Biology, the researchers describe how they got a,11b-dimethyl-19-nortestosterone to react in a test tube with synthetic aromatase. Aromatase is the enzyme that converts anabolic and androgenic steroid hormones like testosterone into estradiol. Aromatase is responsible for seventy percent of the gynos that you see in bodybuilders. Well, that’s our estimate.
</br>
</br> The figure below shows what happened when the researchers added testosterone to the enzyme. The amount of testosterone decreases, and the amount of estradiol increases.
</br>
</br> The next graph shows what happened when the researchers repeated the experiment with dimethandrolone instead of testosterone.
</br>
</br> Nothing at all. The oestrogen that would have been produced if the aromatase enzyme did get to work on dimethandrolone is 7a,11b-dimethyl-estradiol. When the scientists synthesized that oestrogen and tested it in test tubes, they noticed that it interacted ten per cent less well with the a- and b-receptor for estradiol than estradiol itself. If the enzyme had worked, then the oestrogenic effect would still have been considerable.
</br>
</br> The researchers repeated the above experiment with MENT or 7a-methyl-19-nortestosterone. MENT was pretty hip for a while in the anabolics scene, and it looked set to enter the market. But when it turned out not to work so well in oral form, whereas the new dimethandrolone can be taken orally, interest waned.
</br>
</br> The graph below shows what aromatase does with MENT.
</br>
</br> MENT does aromatize – a bit. The oestrogen that is produced, 7a-methyl-estradiol, is a teeny-weeny bit stronger than ordinary estradiol.
</br>
</br> When the researchers repeated the experiment again with 11b-methyl-19-nortestosterone they discovered that the nandrolone-analogue doesn’t aromatize at all either. It therefore seems likely that it is the 11b-methyl group that prevents aromatase from interacting with dimethandrolone. Theoretically it might be possible that another enzyme, 5a-reductase, the enzyme that converts testosterone in DHT, converts dimethandrolone into steroid compounds with a weak oestrogenic effect. But the researchers also think that 5a-reductase won’t work on dimethandrolone either. They told this during the Annual Meeting of the Endocrine Society in Toronto, Canada in 2007. In animal tests that have not yet been published, they have not discovered any signs of an oestrogenic effect of dimethandrolone.
</br>
</br> We know enough. A new anabolic steroid will be launched soon. Sources: J Steroid Biochem Mol Biol. 2008 Jun;110(3-5):214-22. Endocrinology. 2006 Jun;147(6):3016-26. Bioorg Med Chem Lett. 2005 Feb 15;15(4):1213-6. Science Daily October 1, 2007.
</br>
</br> 7alpha,11beta-Dimethyl-19-nortestostero... [Bioorg Med Chem Lett. 2005] - PubMed - NCBI 7alpha,11beta-Dimethyl-19-nortestosterone: a potent and selective androgen response modulator with prostate-sparing properties.Cook CE, Kepler JA. Organic and Medicinal Chemistry, Science and Engineering Group, Research Triangle Institute, PO Box 12194, Research Triangle Park, NC 27709, USA. [email protected]
</br>
</br> 7alpha,11beta-Dimethyl-19-nortestosterone, made by 1,6-methyl addition to 17beta-acetoxy-11beta-methylestra-4,6-dien-3-one, was a highly potent and selective androgen response modulator, with enhanced androgen receptor binding, androgenic activity and anabolic:androgenic ratio over its two monomethyl homologs. PMID: 15686944 [PubMed - indexed for MEDLINE]
</br>
</br> Dimethandrolone (7alpha,11beta-di... [J Steroid Biochem Mol Biol. 2008] - PubMed - NCBI Dimethandrolone (7alpha,11beta-dimethyl-19-nortestosterone) and 11beta-methyl-19-nortestosterone are not converted to aromatic A-ring products in the presence of recombinant human aromatase.Attardi BJ, Pham TC, Radler LC, Burgenson J, Hild SA, Reel JR. Division of Reproductive Endocrinology and Toxicology, BIOQUAL Inc., 9600 Medical Center Drive, Rockville, MD 20850, USA. [email protected]
</br>
</br> Dimethandrolone undecanoate (DMAU: 7alpha,11beta-dimethyl-19-nortestosterone 17beta-undecanoate) is a potent orally active androgen in development for hormonal therapy in men. Cleavage of the 17beta-ester bond by esterases in vivo leads to liberation of the biologically active androgen, dimethandrolone (DMA), a 19-norandrogen. For hormone replacement in men, administration of C19 androgens such as testosterone (T) may lead to elevations in circulating levels of estrogens due to aromatization. As several reports have suggested that certain 19-norandrogens may serve as substrates for the aromatase enzyme and are converted to the corresponding aromatic A-ring products, it was important to investigate whether DMA, the related compound, 11beta-methyl-19-nortestosterone (11beta-MNT), also being tested for hormonal therapy in men, and other 19-norandrogens can be converted to aromatic A-ring products by human aromatase. The hypothetical aromatic A-ring product corresponding to each substrate was obtained by chemical synthes
</br>
</br> Dimethandrolone (DMA), the 17beta-undecanoic acid ester of dimethandrolone (DMAU; 7alpha,11beta-dimethyl-19-nortestosterone) is a potent androgen currently in development for therapeutic uses in men. Cleavage of the 17beta-ester bond liberates the biologically active DMA. In this study we investigated the activity of DMAU and DMA both in vivo and in vitro. DMAU was active orally in castrate rat bioassays, and when administered sc, a single dose produced prolonged androgenic activity and suppression of LH with sustained circulating levels of DMA. DMA, other 19-norandrogens, and C-19 androgens bound to recombinant rat androgen receptor with high affinity and were equipotent in stimulating luciferase activity (EC50, 10(-10) -10(-9) M) in CV-1 cells cotransfected with a human androgen receptor expression vector and a luciferase reporter plasmid with three hormone response elements. Because various 19-norandrogens are also known to bind to progestin receptors (PR) and to possess progestational activity in vivo, we evaluated the binding affinity of DMA for rabbit PR and recombinant human PR-A and PR-B and its ability to induce PR-mediated transcription and endogenous alkaline phosphatase activity in T47DCO human breast cancer cells. DMA and related 19-norandrogens bound with high affinity to both rabbit and human PR, whereas the less active 11alpha-methyl stereoisomer of DMA and C-19 androgens showed low or negligible binding to PR. In T47DCO cells, 10(-8) M DMA and other 19-norandrogens stimulated transcription of a progestin/glucocorticoid/androgen response element-thymidine kinase-luciferase reporter plasmid to the same extent as R5020, the potent progestin promegestone (EC50, approximately 10(-9) M), but C-19 androgens had no effect. Antiprogestins were potent inhibitors of transactivation and alkaline phosphatase activity induced by DMA and other 19-norandrogens in T47DCO cells, whereas antiandrogens were weak inhibitors.
</br>
</br> Monster anabolic dimethandrolone does not aromatize
</br>
</br> The prospects for the new anabolic steroid dimethandrolone – full name 7a,11b-dimethyl-19-nortestosterone – are looking increasingly good. According to researchers at US-based Bioqual, the chance of users being subjected to oestrogenic side-effects is nil. In test-tube experiments dimethandrolone did not convert into oestrogenic compounds.
</br>
</br> Dimethandrolone is a nandrolone-type of compound with two extra methyl groups on C7 and C11. These methyl groups make dimethandrolone a really powerful porcupine anabolic. Bioqual researchers published results of an animal study on dimethandrolone already in 2006. [Endocrinology. 2006 Jun;147(6):3016-26.] These showed that dimethandrolone has a powerful anabolic effect, it doesn’t affect the prostate and also has a considerable progesterone-like effect. According to another study that is now four years old, dimethandrolone is 136 times more powerful than testosterone. [Bioorg Med Chem Lett. 2005 Feb 15;15(4):1213-6.]
</br>
</br> Yeehaw. At congresses on male contraceptives, though, researchers have reported contradictory effects on the fertility of experimental animals that were given dimethandrolone. When given low doses, animals become sterile, but apparently not when given high doses. [Science Daily October 1, 2007]
</br>
</br> In a study that will soon appear in the Journal of Steroid Biochemistry and Molecular Biology, the researchers describe how they got a,11b-dimethyl-19-nortestosterone to react in a test tube with synthetic aromatase. Aromatase is the enzyme that converts anabolic and androgenic steroid hormones like testosterone into estradiol. Aromatase is responsible for seventy percent of the gynos that you see in bodybuilders. Well, that’s our estimate.
</br>
</br> The figure below shows what happened when the researchers added testosterone to the enzyme. The amount of testosterone decreases, and the amount of estradiol increases.
</br>
</br> The next graph shows what happened when the researchers repeated the experiment with dimethandrolone instead of testosterone.
</br>
</br> Nothing at all. The oestrogen that would have been produced if the aromatase enzyme did get to work on dimethandrolone is 7a,11b-dimethyl-estradiol. When the scientists synthesized that oestrogen and tested it in test tubes, they noticed that it interacted ten per cent less well with the a- and b-receptor for estradiol than estradiol itself. If the enzyme had worked, then the oestrogenic effect would still have been considerable.
</br>
</br> The researchers repeated the above experiment with MENT or 7a-methyl-19-nortestosterone. MENT was pretty hip for a while in the anabolics scene, and it looked set to enter the market. But when it turned out not to work so well in oral form, whereas the new dimethandrolone can be taken orally, interest waned.
</br>
</br> The graph below shows what aromatase does with MENT.
</br>
</br> MENT does aromatize – a bit. The oestrogen that is produced, 7a-methyl-estradiol, is a teeny-weeny bit stronger than ordinary estradiol.
</br>
</br> When the researchers repeated the experiment again with 11b-methyl-19-nortestosterone they discovered that the nandrolone-analogue doesn’t aromatize at all either. It therefore seems likely that it is the 11b-methyl group that prevents aromatase from interacting with dimethandrolone. Theoretically it might be possible that another enzyme, 5a-reductase, the enzyme that converts testosterone in DHT, converts dimethandrolone into steroid compounds with a weak oestrogenic effect. But the researchers also think that 5a-reductase won’t work on dimethandrolone either. They told this during the Annual Meeting of the Endocrine Society in Toronto, Canada in 2007. In animal tests that have not yet been published, they have not discovered any signs of an oestrogenic effect of dimethandrolone.
</br>
</br> We know enough. A new anabolic steroid will be launched soon. Sources: J Steroid Biochem Mol Biol. 2008 Jun;110(3-5):214-22. Endocrinology. 2006 Jun;147(6):3016-26. Bioorg Med Chem Lett. 2005 Feb 15;15(4):1213-6. Science Daily October 1, 2007.
</br>
</br> 7alpha,11beta-Dimethyl-19-nortestostero... [Bioorg Med Chem Lett. 2005] - PubMed - NCBI 7alpha,11beta-Dimethyl-19-nortestosterone: a potent and selective androgen response modulator with prostate-sparing properties.Cook CE, Kepler JA. Organic and Medicinal Chemistry, Science and Engineering Group, Research Triangle Institute, PO Box 12194, Research Triangle Park, NC 27709, USA. [email protected]
</br>
</br> 7alpha,11beta-Dimethyl-19-nortestosterone, made by 1,6-methyl addition to 17beta-acetoxy-11beta-methylestra-4,6-dien-3-one, was a highly potent and selective androgen response modulator, with enhanced androgen receptor binding, androgenic activity and anabolic:androgenic ratio over its two monomethyl homologs. PMID: 15686944 [PubMed - indexed for MEDLINE]
</br>
</br> Dimethandrolone (7alpha,11beta-di... [J Steroid Biochem Mol Biol. 2008] - PubMed - NCBI Dimethandrolone (7alpha,11beta-dimethyl-19-nortestosterone) and 11beta-methyl-19-nortestosterone are not converted to aromatic A-ring products in the presence of recombinant human aromatase.Attardi BJ, Pham TC, Radler LC, Burgenson J, Hild SA, Reel JR. Division of Reproductive Endocrinology and Toxicology, BIOQUAL Inc., 9600 Medical Center Drive, Rockville, MD 20850, USA. [email protected]
</br>
</br> Dimethandrolone undecanoate (DMAU: 7alpha,11beta-dimethyl-19-nortestosterone 17beta-undecanoate) is a potent orally active androgen in development for hormonal therapy in men. Cleavage of the 17beta-ester bond by esterases in vivo leads to liberation of the biologically active androgen, dimethandrolone (DMA), a 19-norandrogen. For hormone replacement in men, administration of C19 androgens such as testosterone (T) may lead to elevations in circulating levels of estrogens due to aromatization. As several reports have suggested that certain 19-norandrogens may serve as substrates for the aromatase enzyme and are converted to the corresponding aromatic A-ring products, it was important to investigate whether DMA, the related compound, 11beta-methyl-19-nortestosterone (11beta-MNT), also being tested for hormonal therapy in men, and other 19-norandrogens can be converted to aromatic A-ring products by human aromatase. The hypothetical aromatic A-ring product corresponding to each substrate was obtained by chemical synthes
</br>
</br> Dimethandrolone (DMA), the 17beta-undecanoic acid ester of dimethandrolone (DMAU; 7alpha,11beta-dimethyl-19-nortestosterone) is a potent androgen currently in development for therapeutic uses in men. Cleavage of the 17beta-ester bond liberates the biologically active DMA. In this study we investigated the activity of DMAU and DMA both in vivo and in vitro. DMAU was active orally in castrate rat bioassays, and when administered sc, a single dose produced prolonged androgenic activity and suppression of LH with sustained circulating levels of DMA. DMA, other 19-norandrogens, and C-19 androgens bound to recombinant rat androgen receptor with high affinity and were equipotent in stimulating luciferase activity (EC50, 10(-10) -10(-9) M) in CV-1 cells cotransfected with a human androgen receptor expression vector and a luciferase reporter plasmid with three hormone response elements. Because various 19-norandrogens are also known to bind to progestin receptors (PR) and to possess progestational activity in vivo, we evaluated the binding affinity of DMA for rabbit PR and recombinant human PR-A and PR-B and its ability to induce PR-mediated transcription and endogenous alkaline phosphatase activity in T47DCO human breast cancer cells. DMA and related 19-norandrogens bound with high affinity to both rabbit and human PR, whereas the less active 11alpha-methyl stereoisomer of DMA and C-19 androgens showed low or negligible binding to PR. In T47DCO cells, 10(-8) M DMA and other 19-norandrogens stimulated transcription of a progestin/glucocorticoid/androgen response element-thymidine kinase-luciferase reporter plasmid to the same extent as R5020, the potent progestin promegestone (EC50, approximately 10(-9) M), but C-19 androgens had no effect. Antiprogestins were potent inhibitors of transactivation and alkaline phosphatase activity induced by DMA and other 19-norandrogens in T47DCO cells, whereas antiandrogens were weak inhibitors.
