Metribolone (developmental code R1881, also known as methyltrienolone) is a synthetic and orally active anabolic–androgenic steroid (AAS) and a 17α-alkylated nandrolone (19-nortestosterone) derivative which was never marketed for medical use but has been widely used in scientific research as a hot ligand in androgen receptor (AR) ligand binding assays (LBAs) and as a photoaffinity label for the AR.[1][2][3] More precisely, metribolone is the 17α-methylated derivative of trenbolone. It was investigated briefly for the treatment of advanced breast cancer in women in the late 1960s and early 1970s, but was found to produce signs of severe hepatotoxicity at very low dosages, and its development was subsequently discontinued.[2][4]
^Elks J (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. pp. 654–. ISBN 978-1-4757-2085-3.
^ abWilliam Llewellyn's Anabolics. Molecular Nutrition LLC. 2011. pp. 546–. ISBN 978-0-9828280-1-4.
^Brinkmann AO, Kuiper GG, de Boer W, Mulder E, Bolt J, van Steenbrugge GJ, van der Molen HJ (January 1986). "Characterization of androgen receptors after photoaffinity labelling with [3H]methyltrienolone (R1881)". Journal of Steroid Biochemistry. 24 (1): 245–249. doi:10.1016/0022-4731(86)90058-0. PMID 2422446.
^Cite error: The named reference Brueggemeier2006 was invoked but never defined (see the help page).
Metribolone (developmental code R1881, also known as methyltrienolone) is a synthetic and orally active anabolic–androgenic steroid (AAS) and a 17α-alkylated...
mibolerone and metribolone had similar affinity for the progesterone receptor (PR) but that mibolerone only had around half the affinity of metribolone for the...
of doping in sports with trenbolone esters by professional athletes. Metribolone Anvisa (2023-03-31). "RDC Nº 784 - Listas de Substâncias Entorpecentes...
of trenbolone and the 7α-methyl derivative of metribolone, as well as the δ9,11 analogue of metribolone and the δ9,11, 17α-methylated derivative of trestolone...
substances, and is therefore banned from use in most major sports. Dienedione Metribolone "The World Anti-Doping Code: The 2012 Prohibited List" (PDF). World Anti-Doping...
closely related to dimethyltrienolone, as well as to mibolerone and metribolone. Dimethyldienolone shows high affinity for the androgen and progesterone...
but has been used in scientific research. Due to its close relation to metribolone (methyltrienolone), it is thought that TMT may produce hepatotoxicity...
affinity of oxandrolone for the androgen receptor is about 0.3% of that of metribolone. Activation of the androgen receptor stimulates protein synthesis, which...
study, it showed only 0.00084% of the affinity of the anabolic steroid metribolone (100%) for the human AR (Ki = 140 μM and 1.18 nM, respectively). In any...
affinity of metribolone for the androgen receptor, δ4-tibolone has relatively high affinity of about 35% of the affinity of metribolone for this receptor...
values within 4 weeks. Etonogestrel has about 20% of the affinity of metribolone and 50% of the affinity of levonorgestrel for the androgen receptor (AR)...
non-17α-alkylated trenbolone and the 17α-alkylated ethylestrenol (ethylnandrol) and metribolone (R-1881), as well as the 17α-alkylated designer steroids norboletone...
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