RU-56187
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| Drug class | Nonsteroidal antiandrogen |
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| Formula | C14H12F3N3OS |
| Molar mass | 327.33 g·mol−1 |
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RU-56187 is a nonsteroidal antiandrogen which was never marketed.[1][2][3][4][5] It shows 92% of the affinity of testosterone for the androgen receptor and negligible affinity for other steroid hormone receptors.[1][2] The medication is a silent antagonist of the androgen receptor.[5] RU-56187 is 3- to 10-fold more potent as an antiandrogen than bicalutamide or nilutamide in animals.[1] Both RU-56187 and RU-58841 appear to be prodrugs of cyanonilutamide (RU-56279) in vivo in animals.[3]
See also
[edit]References
[edit]- ^ a b c Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): structure-activity relationships". Curr. Med. Chem. 7 (2): 211–47. doi:10.2174/0929867003375371. PMID 10637363.
- ^ a b Teutsch G, Goubet F, Battmann T, Bonfils A, Bouchoux F, Cerede E, Gofflo D, Gaillard-Kelly M, Philibert D (January 1994). "Non-steroidal antiandrogens: synthesis and biological profile of high-affinity ligands for the androgen receptor". J. Steroid Biochem. Mol. Biol. 48 (1): 111–9. doi:10.1016/0960-0760(94)90257-7. PMID 8136296. S2CID 31404295.
- ^ a b Cousty-Berlin D, Bergaud B, Bruyant MC, Battmann T, Branche C, Philibert D (October 1994). "Preliminary pharmacokinetics and metabolism of novel non-steroidal antiandrogens in the rat: relation of their systemic activity to the formation of a common metabolite". J. Steroid Biochem. Mol. Biol. 51 (1–2): 47–55. doi:10.1016/0960-0760(94)90114-7. PMID 7947350. S2CID 29752252.
- ^ Matias JR, Gaillard M (June 1995). "Local inhibition of sebaceous gland growth by topically applied RU 58841". Ann. N. Y. Acad. Sci. 761 (3): 56–65. Bibcode:1995NYASA.761...56M. doi:10.1111/j.1749-6632.1995.tb31369.x. PMID 7625751. S2CID 45086788.
- ^ a b Kemppainen JA, Langley E, Wong CI, Bobseine K, Kelce WR, Wilson EM (March 1999). "Distinguishing androgen receptor agonists and antagonists: distinct mechanisms of activation by medroxyprogesterone acetate and dihydrotestosterone". Mol. Endocrinol. 13 (3): 440–54. doi:10.1210/mend.13.3.0255. PMID 10077001.
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