| 词条 | 3-Methyl-19-methyleneandrosta-3,5-dien-17β-ol |
| 释义 |
| Verifiedfields = | Watchedfields = | verifiedrevid = | IUPAC_name = (8R,9S,10S,13S,14S,17S)-10-Ethenyl-3,13-dimethyl-2,7,8,9,11,12,14,15,16,17-decahydro-1H-cyclopenta[a]phenanthren-17-ol | image = 3-Methyl-19-methyleneandrosta-3,5-dien-17β-ol.svg | width = | 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 = | CAS_supplemental = | ATC_prefix = | ATC_suffix = | ATC_supplemental = | PubChem = 24896626 | IUPHAR_ligand = | DrugBank_Ref = | DrugBank = | ChemSpiderID_Ref = | ChemSpiderID = 23306322 | UNII = | KEGG = | ChEBI = | ChEMBL = 398456 | C=21 | H=30 | O=1 | molecular_weight = 298.47 g/mol | SMILES = CC1=CC2=CC[C@H]3[C@@H]4CC[C@@H]([C@]4(CC[C@@H]3[C@]2(CC1)C=C)C)O | StdInChI_Ref = | StdInChI = 1S/C21H30O/c1-4-21-12-9-14(2)13-15(21)5-6-16-17-7-8-19(22)20(17,3)11-10-18(16)21/h4-5,13,16-19,22H,1,6-12H2,2-3H3/t16-,17-,18-,19-,20-,21-/m0/s1 | StdInChIKey_Ref = | StdInChIKey = PPGVWCDLIZEUNC-PXQJOHHUSA-N | synonyms = 3-Methyl-19-methyleneandrosta-3,5-dien-17β-ol }}3-Methyl-19-methyleneandrosta-3,5-dien-17β-ol is a synthetic, steroidal estrogen and a selective agonist of the ERβ.[1] It was discovered serendipitously and was the lead compound among a series of androsta-3,5-dienes as ERβ ligands.[1][2] Its affinity (IC50) for the ERβ was found to be 9 nM and it showed 62- and 160-fold binding selectivity for this receptor over the {{abbrlink|AR|androgen receptor}} and the ERα, respectively.[1] The EC50 of the compound for the ERβ was found to be 69 nM and its intrinsic activity was 92% (relative to that of estradiol).[1] As such, it is a potent ERβ agonist with high affinity and selectivity.[1] References1. ^1 2 3 4 {{cite journal | vauthors = Blizzard TA, Gude C, Morgan JD, Chan W, Birzin ET, Mojena M, Tudela C, Chen F, Knecht K, Su Q, Kraker B, Mosley RT, Holmes MA, Rohrer SP, Hammond ML | title = Androstene-3,5-dienes as ER-beta selective SERMs | journal = Bioorg. Med. Chem. Lett. | volume = 17 | issue = 22 | pages = 6295–8 | year = 2007 | pmid = 17890084 | doi = 10.1016/j.bmcl.2007.09.001 | url = }} {{Estrogen receptor modulators}}{{DEFAULTSORT:Methyl-19-methyleneandrosta-3,5-dien-17β-ol, 3-}}{{steroid-stub}}{{genito-urinary-drug-stub}}2. ^{{cite journal | vauthors = Khalil RA | title = Estrogen, vascular estrogen receptor and hormone therapy in postmenopausal vascular disease | journal = Biochem. Pharmacol. | volume = 86 | issue = 12 | pages = 1627–42 | year = 2013 | pmid = 24099797 | pmc = 3840081 | doi = 10.1016/j.bcp.2013.09.024 | url = }} 4 : Alcohols|Androstanes|Selective ERβ agonists|Synthetic estrogens |
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