| 词条 | Β-LGND2 |
| 释义 |
| Verifiedfields = | Watchedfields = | verifiedrevid = | IUPAC_name = 4-bromo-6,8-dihydroxy-2-(4-hydroxyphenyl)isoquinolin-1-one | image = Β-LGND2.svg | width = | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | class = Nonsteroidal estrogen; Selective ERβ agonist | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = | CAS_number = 1462971-30-7 | CAS_supplemental = 1644567-26-9 | ATC_prefix = | ATC_suffix = | ATC_supplemental = | PubChem = 24962206 | IUPHAR_ligand = | DrugBank_Ref = | DrugBank = | ChemSpiderID_Ref = | ChemSpiderID = | UNII = | KEGG = | ChEBI = | ChEMBL = | synonyms = β-LGND2; ER-β-selective ligand 2 | C=15 | H=10 | Br=1 | N=1 | O=4 | molecular_weight = 348.152 g/mol | SMILES = C1=CC(=CC=C1N2C=C(C3=CC(=CC(=C3C2=O)O)O)Br)O | StdInChI_Ref = | StdInChI = 1S/C15H10BrNO4/c16-12-7-17(8-1-3-9(18)4-2-8)15(21)14-11(12)5-10(19)6-13(14)20/h1-7,18-20H | StdInChIKey_Ref = | StdInChIKey = GLVQMSCCFOGRRG-UHFFFAOYSA-N }}β-LGND2, also known as ERβ-selective ligand 2 or as GTx-878, is a synthetic nonsteroidal estrogen and selective ERβ agonist which was under development by GTx for the treatment of benign prostatic hyperplasia, prostatitis, and rheumatoid arthritis but was never marketed.[1][2][3][4][5][6] It shows approximately 25-fold selectivity for activation of the ERβ over the ERα ({{abbrlink|EC50|half-maximal effective concentration}} = 2 nM and 52 nM, respectively).[3] β-LGND2 is an isoquinolinone derivative.[2][5] References1. ^https://adisinsight.springer.com/drugs/800027855 2. ^1 {{cite journal | vauthors = Yepuru M, Eswaraka J, Kearbey JD, Barrett CM, Raghow S, Veverka KA, Miller DD, Dalton JT, Narayanan R | title = Estrogen receptorbetaselective ligands alleviate high-fat diet- and ovariectomy-induced obesity in mice | journal = J. Biol. Chem. | volume = 285 | issue = 41 | pages = 31292–303 | date = October 2010 | pmid = 20657011 | pmc = 2951204 | doi = 10.1074/jbc.M110.147850 | url = }} 3. ^1 {{cite journal | vauthors = Ponnusamy S, Tran QT, Harvey I, Smallwood HS, Thiyagarajan T, Banerjee S, Johnson DL, Dalton JT, Sullivan RD, Miller DD, Bridges D, Narayanan R | title = Pharmacologic activation of estrogen receptor β increases mitochondrial function, energy expenditure, and brown adipose tissue | journal = FASEB J. | volume = 31 | issue = 1 | pages = 266–281 | date = January 2017 | pmid = 27733447 | pmc = 5161516 | doi = 10.1096/fj.201600787RR | url = | quote = We found that β-LGND2, also known as GTx-878 (GTx, Inc. (31)), reduces body weight and fat mass without altering feed consumption of high-fat diet (HFD)-fed WT, but not ER-βKO, mice.}} 4. ^{{cite journal | vauthors = Giddabasappa A, Eswaraka JR, Barrett CM, Bauler MN, Wu Z, Yepuru M, Miller DD, Dalton JT | title = β-LGND2, an ERβ selective agonist, inhibits pathologic retinal neovascularization | journal = Invest. Ophthalmol. Vis. Sci. | volume = 53 | issue = 8 | pages = 5066–75 | date = July 2012 | pmid = 22714897 | doi = 10.1167/iovs.12-9627 | url = }} 5. ^1 {{cite journal | vauthors = Paterni I, Granchi C, Katzenellenbogen JA, Minutolo F | title = Estrogen receptors alpha (ERα) and beta (ERβ): subtype-selective ligands and clinical potential | journal = Steroids | volume = 90 | issue = | pages = 13–29 | date = November 2014 | pmid = 24971815 | pmc = 4192010 | doi = 10.1016/j.steroids.2014.06.012 | url = }} 6. ^{{cite journal | vauthors = Mohler ML, Narayanan R, Coss CC, Hu K, He Y, Wu Z, Hong SS, Hwang DJ, Miller DD, Dalton JT | title = Estrogen receptor beta selective nonsteroidal estrogens: seeking clinical indications | journal = Expert Opin Ther Pat | volume = 20 | issue = 4 | pages = 507–34 | date = April 2010 | pmid = 20302450 | doi = 10.1517/13543771003657164 | url = }} External links
8 : Abandoned drugs|Bromoarenes|Isoquinolines|Ketones|Phenols|Selective ERβ agonists|Synthetic estrogens|Triols |
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