词条 | 3α-Hydroxytibolone |
释义 |
| Verifiedfields = | Watchedfields = | verifiedrevid = | IUPAC_name = (3R,7R,8R,9S,13S,14S,17R)-17-Ethynyl-7,13-dimethyl-2,3,4,6,7,8,9,11,12,14,15,16-dodecahydro-1H-cyclopenta[a]phenanthrene-3,17-diol | image = 3α-Hydroxytibolone.svg | width = 225px | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | class = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = | CAS_number = 100239-44-9 | CAS_supplemental = | ATC_prefix = | ATC_suffix = | ATC_supplemental = | PubChem = 10087021 | IUPHAR_ligand = | DrugBank_Ref = | DrugBank = | ChemSpiderID_Ref = | ChemSpiderID = 8262558 | UNII = 37T303O94A | KEGG = | ChEBI = | ChEMBL = | synonyms = ORG-4094; 7α-Methyl-17α-ethynylestr-5(10)-ene-3α,17β-diol | C=21 | H=30 | O=2 | molecular_weight = 314.469 g/mol | SMILES = C[C@@H]1CC2=C(CC[C@H](C2)O)[C@@H]3[C@@H]1[C@@H]4CC[C@]([C@]4(CC3)C)(C#C)O | StdInChI_Ref = | StdInChI = 1S/C21H30O2/c1-4-21(23)10-8-18-19-13(2)11-14-12-15(22)5-6-16(14)17(19)7-9-20(18,21)3/h1,13,15,17-19,22-23H,5-12H2,2-3H3/t13-,15-,17-,18+,19-,20+,21+/m1/s1 | StdInChIKey_Ref = | StdInChIKey = YLEUWNOTNJZCBN-CZTKNSHGSA-N }}3α-Hydroxytibolone (developmental code name ORG-4094) is a synthetic steroidal estrogen which was never marketed.[1][2] Along with 3β-hydroxytibolone and δ4-tibolone, it is a major active metabolite of tibolone, and 3α-hydroxytibolone and 3β-hydroxytibolone are thought to be responsible for the estrogenic activity of tibolone.[1][2]{{Relative affinities of noretynodrel, tibolone, and metabolites}}{{Absolute activities of tibolone and metabolites}} References1. ^1 {{cite journal|last1=Kuhl|first1=H|title=Pharmacology of estrogens and progestogens: influence of different routes of administration|journal=Climacteric|volume=8|issue=sup1|year=2009|pages=3–63|issn=1369-7137|doi=10.1080/13697130500148875|pmid=16112947}} {{Estrogen receptor modulators}}{{DEFAULTSORT:Hydroxytibolone, 3α-}}{{Genito-urinary-drug-stub}}{{Steroid-stub}}2. ^1 {{cite journal | vauthors = Escande A, Servant N, Rabenoelina F, Auzou G, Kloosterboer H, Cavaillès V, Balaguer P, Maudelonde T | title = Regulation of activities of steroid hormone receptors by tibolone and its primary metabolites | journal = J. Steroid Biochem. Mol. Biol. | volume = 116 | issue = 1-2 | pages = 8–14 | year = 2009 | pmid = 19464167 | doi = 10.1016/j.jsbmb.2009.03.008 | url = http://www.hal.inserm.fr/inserm-00396319/document}} 7 : Abandoned drugs|Alkenes|Alkynes|Diols|Estranes|Human drug metabolites|Synthetic estrogens |
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