anyone heard of this ?
- 06-12-2006, 12:07 AM
anyone heard of this ?
Dimethandrolone Undecanoate: A New Potent Orally Active Androgen with Progestational Activity
Barbara J. Attardi, Sheri A. Hild and Jerry R. Reel
BIOQUAL, Inc., Rockville, Maryland 20850
Address all correspondence and requests for reprints to: Dr. Barbara J. Attardi, Molecular Endocrinology Laboratory, BIOQUAL, Inc., 9600 Medical Center Drive, Rockville, Maryland 20850. E-mail: [email protected].
Dimethandrolone (DMA), the 17ß-undecanoic acid ester of dimethandrolone (DMAU; 7,11ß-dimethyl-19-nortestosterone) is a potent androgen currently in development for therapeutic uses in men. Cleavage of the 17ß-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 11-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, 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. DMA and DMAU also exhibited dose-dependent progestational activity in the estrogen-primed immature female rabbit, as assessed by induction of endometrial gland arborization. The dual androgenic and progestational activities of DMA make it a potential candidate for a single-agent male contraceptive as well as for androgen therapy in men, pending a successful outcome of pharmacokinetic and toxicity studies currently in progress.
- 06-12-2006, 12:23 AM
I did read an article awhile ago about testosterone undecanoate being looked at for male birth control but i am not familiar with this substance. Progestational activity does not sound appealing.
06-12-2006, 12:27 AM
06-12-2006, 12:33 AM
06-12-2006, 12:51 AM
yup, i believe i read about this in our news and articles section awhile back. the means of administration was an injection not the typical oral andriol. i guess they see something is this new substance but with PR binding ability i do not see why it would be better than the test injection.Originally Posted by mercedesdd
the whole idea is to inject a long acting substance that will cause a cease in production of LH, in other words mostly any steroid. The more long acting the better
06-12-2006, 12:57 AM
06-12-2006, 01:07 AM
there is a link to the birth control article i was talking about;
here is an excerpt:
The big Chinese study, for example, is injecting an altered version of testosterone called TU, for testosterone undecanoate. While results may not be available until early 2006, an earlier trial of TU found that monthly injections dropped sperm counts to zero or close to it in 296 of 308 men. But six of these men began making sperm again during the treatment. There were no serious side effects.
The current Chinese study, sponsored by the World Health Organization in collaboration with the Chinese government and Xianju Pharmaceutical Co., recruited more than 1,000 couples, although some have left the project. The goal is to see how well TU prevents pregnancy over two years in the sexual partners of men who respond to the drug.
Taking another tack, the nonprofit Population Council, based in New York, is working with a synthetic hormone called MENT. It's almost 10 times as powerful as testosterone, said council researcher Narender Kumar. The council is studying the idea of combining MENT implants with implants of a hormone used in female contraceptives, because they can act together to suppress sperm production.
06-12-2006, 01:08 AM
Man you sparked my intest on this andriol thing LOL. I just was reading a study the other day on pubmed( cant find it now) it stated that andriol and no abilitly to lower LH or FSH respectively.. So it is strange !!!
06-12-2006, 12:32 PM
this is not test undecanoate people. this is a nandrolone analogue....and PR activity isnt a bad thing - deca, tren and anadrol all work most of their magic through the PR.Originally Posted by jomi822
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