| 词条 | Radafaxine |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 464379587 | IUPAC_name = (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethylmorpholin-2-ol | image = Radafaxine Structural Formulae.png | width = 164 | 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 = {{cascite|changed|??}} | CAS_number = 106083-71-0 | ATC_prefix = none | ATC_suffix = | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 1172928 | PubChem = 9795056 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 7970823 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = Q47741214K | C=13 | H=18 | Cl=1 | N=1 | O=2 | molecular_weight = 292.20 g/mol | smiles = Clc1cccc(c1)[C@]2(O)OCC(N[C@H]2C)(C)C | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C13H18ClNO2/c1-9-13(16,17-8-12(2,3)15-9)10-5-4-6-11(14)7-10/h4-7,9,15-16H,8H2,1-3H3/t9-,13+/m0/s1 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = RCOBKSKAZMVBHT-TVQRCGJNSA-N }}Radafaxine is drug candidate designated GW-353,162[1] by GlaxoSmithKline, investigated for treatment of restless leg syndrome and as an NDRI antidepressant. GlaxoSmithKline was targeting Radafaxine for regulatory filing in 2007,[2] but development was discontinued in 2006 due to "poor test results".[3] ChemistryIt is a potent metabolite of bupropion, the compound in GlaxoSmithKline's Wellbutrin. More specifically, "hydroxybupropion" is an analogue of bupropion, and radafaxine is an isolated isomer ((2S,3S)-) of hydroxybupropion.[4] Therefore, radafaxine builds on at least some of the properties of bupropion in humans.[5] EffectsIn various clinical trials, radafaxine has been studied as a treatment for clinical depression, obesity, and neuropathic pain. Radafaxine is described as a norepinephrine-dopamine reuptake inhibitor (NDRI). Unlike bupropion (which has a much higher effect on dopamine reuptake), radafaxine seems to have a higher potency on norepinephrine. Radafaxine has about 70% of bupropion's efficacy in blocking dopamine reuptake, and 392% of efficacy in blocking norepinephrine reuptake, making it fairly selective for inhibiting the reuptake of norepinephrine over dopamine.[6][7] This, according to GlaxoSmithKline, may account for the increased effect of radafaxine on pain and fatigue.[8] At least one study suggests that radafaxine has a low abuse potential similar to bupropion.[9] See also
References1. ^Restless Legs Syndrome: First Approval {{webarchive|url=https://web.archive.org/web/20061219222440/http://www.bioportfolio.com/reports/DMD_Restless%20Legs%20Syndrome%20First%20Approval.htm |date=2006-12-19 }} 2. ^{1} Reviews Novel Therapeutics For CNS Disorders And Confirms Strong Pipeline Momentum - News, Search Jobs, Events {{webarchive|url=https://web.archive.org/web/20070928041150/http://www.biospace.com/news_story.aspx?StoryID=18222420&full=1 |date=2007-09-28 }} 3. ^Independent.co.uk: GSK breakthrough on bird flu vaccine {{webarchive|url=https://web.archive.org/web/20071001051510/http://news.independent.co.uk/business/news/article1199374.ece |date=2007-10-01 }}. 4. ^{{MeshName|radafaxine}} 5. ^GlaxoSmithKline Reviews Novel Therapeutics for CNS Disorders and Confirms Strong Pipeline Momentum 6. ^{{cite journal | last1 = Xu | first1 = H | last2 = Loboz | first2 = KK | last3 = Gross | first3 = AS | last4 = McLachlan | first4 = AJ |name-list-format=vanc| year = 2007 | title = Stereoselective analysis of hydroxybupropion and application to drug interaction studies | url = | journal = Chirality | volume = 19 | issue = 3| pages = 163–70 | doi = 10.1002/chir.20356 | pmid = 17167747 }} 7. ^{{cite journal | last1 = Bondarev | first1 = ML | last2 = Bondareva | first2 = TS | last3 = Young | first3 = R | last4 = Glennon | first4 = RA |name-list-format=vanc| year = 2003 | title = Behavioral and biochemical investigations of bupropion metabolites | url = | journal = Eur J Pharmacol | volume = 474 | issue = 1| pages = 85–93 | doi = 10.1016/S0014-2999(03)02010-7 | pmid = 12909199 }} 8. ^Microsoft PowerPoint - slides_05_burch.ppt {{webarchive|url=https://web.archive.org/web/20070928035216/http://213.219.8.102/pdfs/gsk/cns_seminar/353162.pdf |date=2007-09-28 }} 9. ^Radafaxine External links
7 : Norepinephrine-dopamine reuptake inhibitors|Nicotinic antagonists|Bicyclic antidepressants|Chloroarenes|Morpholines|Alcohols|Abandoned drugs |
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