| 词条 | ORG-2058 |
| 释义 |
| Verifiedfields = | Watchedfields = | verifiedrevid = | IUPAC_name = (8R,9S,10R,13S,14S,16R,17S)-16-ethyl-17-(2-hydroxyacetyl)-13-methyl-2,6,7,8,9,10,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-one | image = ORG-2058.svg | width = 250px | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = | CAS_number = 24320-06-7 | CAS_supplemental = | ATC_prefix = | ATC_suffix = | ATC_supplemental = | PubChem = 119086 | IUPHAR_ligand = | DrugBank_Ref = | DrugBank = | ChemSpiderID_Ref = | ChemSpiderID = 106407 | UNII = | KEGG = | ChEBI = | ChEMBL = 2311103 | synonyms = 16α-Ethyl-21-hydroxy-19-norprogesterone; 16α-Ethyl-21-hydroxy-19-norpregn-4-ene-3,20-dione | C=22 | H=32 | O=3 | SMILES = CC[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)CC[C@@H]4[C@H]3CC[C@@]2([C@H]1C(=O)CO)C | StdInChI_Ref = | StdInChI = 1S/C22H32O3/c1-3-13-11-19-18-6-4-14-10-15(24)5-7-16(14)17(18)8-9-22(19,2)21(13)20(25)12-23/h10,13,16-19,21,23H,3-9,11-12H2,1-2H3/t13-,16+,17-,18-,19+,21-,22+/m1/s1 | StdInChIKey_Ref = | StdInChIKey = IJLXLZGJDSJGIQ-BILPMHSYSA-N }}ORG-2058, also known as 16α-ethyl-21-hydroxy-19-norprogesterone, is a progestin of the 19-norprogesterone group which was never marketed.[1][2] It has high affinity for the progesterone receptor (775% of that of progesterone) and has been used in scientific research to study the role of the progesterone receptor in the body.[2] The drug has no affinity for the estrogen receptor or the glucocorticoid receptor (less than 0.2% of the affinities of estradiol and dexamethasone, respectively)[3] and has slight affinity for the mineralocorticoid receptor, but less than that of progesterone.[4] See also
References1. ^{{cite book|author1=Martin Negwer|author2=Hans-Georg Scharnow|title=Organic-chemical drugs and their synonyms: (an international survey)|url=https://books.google.com/books?id=zmpqAAAAMAAJ|year=2001|publisher=Wiley-VCH|isbn=978-3-527-30247-5|page=2350}} {{Progesterone receptor modulators}}{{Steroid-stub}}{{Genito-urinary-drug-stub}}2. ^1 {{cite journal|last1=Fleischmann|first1=Gerhard|last2=Beato|first2=Miguel|title=Characterization of the progesterone receptor of rabbit uterus with the synthetic progestin 16α-ethyl-21-hydroxy-19-norpregn-4-ene-3,20-dione|journal=Biochimica et Biophysica Acta (BBA) - General Subjects|volume=540|issue=3|year=1978|pages=500–517|issn=0304-4165|doi=10.1016/0304-4165(78)90180-0}} 3. ^{{cite journal | vauthors = Bergink EW, Loonen PB, Kloosterboer HJ | title = Receptor binding of allylestrenol, a progestagen of the 19-nortestosterone series without androgenic properties | journal = J. Steroid Biochem. | volume = 23 | issue = 2 | pages = 165–8 | year = 1985 | pmid = 3928974 | doi = | url = }} 4. ^{{cite book|author1=Edward Brad Thompson|author2=Marc E. Lippman|title=Steroid receptors and the management of cancer|url=https://books.google.com/books?id=k8xrAAAAMAAJ|year=1979|publisher=CRC Press|isbn=978-0-8493-5477-9|quote=Org 2058 competed slightly, but less than progesterone, for mineralocorticoid binding.}} 5 : Abandoned drugs|Alcohols|Diketones|Norpregnanes|Progestogens |
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