词条 | Disufenton sodium |
释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 405853279 | IUPAC_name = Disodium 4-[(Z)-(tert-butyl-oxidoazaniumylidene)methyl]benzene-1,3-disulfonate | image = Disufenton sodium.png | 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|correct|??}} | CAS_number = | ATC_prefix = none | ATC_suffix = | PubChem = 6440181 | ChEMBL_Ref = {{ebicite|changed|EBI}} | ChEMBL = 1627056 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | UNII_Ref = {{fdacite|changed|FDA}} | UNII = 7M1J3HN9VO | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D03875 | ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} | ChemSpiderID = 28530805 | C=11 | H=13 | N=1 | Na=2 | O=7 | S=2 | molecular_weight = 381.33 g/mol | smiles = CC(C)(C)[N+]([O-])=Cc1ccc(cc1S(=O)(=O)[O-])S(=O)(=O)[O-].[Na+].[Na+] | StdInChI_Ref = {{stdinchicite|changed|chemspider}} | StdInChI = 1S/C11H15NO7S2.2Na/c1-11(2,3)12(13)7-8-4-5-9(20(14,15)16)6-10(8)21(17,18)19;;/h4-7H,1-3H3,(H,14,15,16)(H,17,18,19);;/q;2*+1/p-2 | StdInChIKey_Ref = {{stdinchicite|changed|chemspider}} | StdInChIKey = XLZOVRYBVCMCGL-UHFFFAOYSA-L }} Disufenton sodium (NXY-059, Cerovive) is the disulfonyl derivative of the neuroprotective spin trap phenylbutylnitrone or "PBN". It was under development at the drug company AstraZeneca. A 2005 phase-3 clinical trial[1][2] called "SAINT-1" reported some efficacy in the acute treatment of ischemia injury due to stroke. However, a 2006 attempt to repeat this trial indicated no significant activity. After ruling out other causes, the authors tentatively attributed the positive results in the first trial to "chance".[1] AstraZeneca then terminated the development programme.[3] PBN and its derivatives hydrolyze and oxidize in vitro to form respectively MNP-OH (AKA, NtBHA) and its parent spin-trap MNP. References1. ^1 {{cite journal | doi = 10.1056/NEJMoa052980 | title = NXY-059 for Acute Ischemic Stroke | year = 2006 | last1 = Lees | first1 = Kennedy R. | last2 = Zivin | first2 = Justin A. | last3 = Ashwood | first3 = Tim | last4 = Davalos | first4 = Antonio | last5 = Davis | first5 = Stephen M. | last6 = Diener | first6 = Hans-Christoph | last7 = Grotta | first7 = James | last8 = Lyden | first8 = Patrick | last9 = Shuaib | first9 = Ashfaq| displayauthors = 8 | journal = New England Journal of Medicine | volume = 354 | issue = 6 | pages = 588–600 | pmid = 16467546}} 2. ^{{cite journal | pmid = 17068304 | year = 2006 | last1 = Lees | first1 = KR | last2 = Davalos | first2 = A | last3 = Davis | first3 = SM | last4 = Diener | first4 = HC | last5 = Grotta | first5 = J | last6 = Lyden | first6 = P | last7 = Shuaib | first7 = A | last8 = Ashwood | first8 = T | last9 = Hardemark | first9 = HG | displayauthors = 8| title = Additional outcomes and subgroup analyses of NXY-059 for acute ischemic stroke in the SAINT I trial | volume = 37 | issue = 12 | pages = 2970–8 | doi = 10.1161/01.STR.0000249410.91473.44 | journal = Stroke: A Journal of Cerebral Circulation}} 3. ^Renovis: Press Release {{webarchive |url=https://web.archive.org/web/20061028094321/http://investors.renovis.com/phoenix.zhtml?c=148297&p=irol-newsArticle&t=Regular&id=921678& |date=October 28, 2006 }} External links
5 : Free radicals|AstraZeneca|Tert-butyl compounds|Benzenesulfonates|Organic sodium salts |
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