Chemistry:Toripristone
From HandWiki
Short description: Chemical compound
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| Other names | RU-40555; 17β-Hydroxy-11β-[4-[methyl(1-methylethyl)amino]phenyl]-17α-(1-propyn-1-yl)estra-4,9-dien-3-one |
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| Formula | C31H39NO2 |
| Molar mass | 457.658 g·mol−1 |
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Toripristone (INN; developmental code name RU-40555) is a synthetic, steroidal antiglucocorticoid as well as antiprogestogen which was never marketed.[1][2] It is reported as a potent and highly selective antagonist of the glucocorticoid receptor (GR) (Ki = 2.4 nM),[3][4] though it also acts as an antagonist of the progesterone receptor (PR).[5][6] The pharmacological profile of toripristone is said to be very similar to that of mifepristone, except that toripristone does not bind to orosomucoid (α1-acid glycoprotein).[5] The drug has been used to study the hypothalamic-pituitary-adrenal axis and has been used as a radiotracer for the GR.[4][3] Its INN was given in 1990.[2]
See also
References
- ↑ "Toripristone". Dictionary of Steroids. CRC Press. 23 May 1991. pp. 101–. ISBN 978-0-412-27060-4. https://books.google.com/books?id=AI7EnUyeEtUC&pg=PA101.
- ↑ 2.0 2.1 "International Nonproprietary Names for Pharmaceutical Substances". WHO Drug Information 3 (2): 18. 1989. https://mednet-communities.net/inn/db/media/docs/p-innlist61.pdf.
- ↑ 3.0 3.1 "Radiolabeled glucocorticoids as molecular probes for imaging brain glucocorticoid receptors by means of positron emission tomography (PET)". Mini Reviews in Medicinal Chemistry 8 (7): 728–739. June 2008. doi:10.2174/138955708784567403. PMID 18537728.
- ↑ 4.0 4.1 "Effect of chronic administration of selective glucocorticoid receptor antagonists on the rat hypothalamic-pituitary-adrenocortical axis". Neuropsychopharmacology 28 (6): 1056–1067. June 2003. doi:10.1038/sj.npp.1300158. PMID 12700716.
- ↑ 5.0 5.1 "From RU 38486 towards Dissociated Antiglucocorticoid and Antiprogesterone". Antihormones in Health and Disease. Frontiers of Hormone Research. 19. 1991. pp. 1–17. doi:10.1159/000419634. ISBN 978-3-8055-5297-4.
- ↑ "Progesterone receptor antagonists and progesterone receptor modulators for endometriosis". Cochrane Database of Systematic Reviews (5): CD009881. 2012. doi:10.1002/14651858.CD009881.
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