| 词条 | Sulbutiamine |
| 释义 |
| Verifiedfields = changed | verifiedrevid = 470472774 | IUPAC_name = [4-[(4-amino-2-methyl-pyrimidin-5-yl)methyl-formyl-amino]-3-[2-[(4-amino-2-methyl-pyrimidin-5-yl)methyl-formyl-amino]-5-(2-methylpropanoyloxy)pent-2-en-3-yl]disulfanyl-pent-3-enyl] 2-methylpropanoate | image = sulbutiamine.svg | alt = Skeletal formula of sulbutiamine | width = 240 | image2 = Sulbutiamine 3D spacefill.png | alt2 = Space-filling model of the sulbutiamine molecule | tradename = | Drugs.com = {{drugs.com|international|sulbutiamine}} | routes_of_administration = Oral | elimination_half-life = 5 hours | excretion = Renal | CAS_number_Ref = {{cascite|changed|??}} | CAS_number = 3286-46-2 | ATC_prefix = A11 | ATC_suffix = DA02 | PubChem = 71124 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 16736830 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 42NCM1BW43 | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D01319 | C=32 | H=46 | N=8 | O=6 | S=2 | molecular_weight = 702.89 g/mol | smiles = Nc2nc(C)ncc2CN(C=O)C(/C)=C(/CCOC(=O)C(C)C)SSC(/CCOC(=O)C(C)C)=C(/C)N(C=O)Cc1cnc(C)nc1N | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C32H46N8O6S2/c1-19(2)31(43)45-11-9-27(21(5)39(17-41)15-25-13-35-23(7)37-29(25)33)47-48-28(10-12-46-32(44)20(3)4)22(6)40(18-42)16-26-14-36-24(8)38-30(26)34/h13-14,17-20H,9-12,15-16H2,1-8H3,(H2,33,35,37)(H2,34,36,38)/b27-21-,28-22- | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = CKHJPWQVLKHBIH-ZDSKVHJSSA-N | synonyms = Arcalion }} Sulbutiamine (brand name: Arcalion) is a synthetic derivative of thiamine (vitamin B1). In France, it is used to treat symptoms of weakness or fatigue. It is also sold as a dietary supplement. Sulbutiamine was discovered in Japan as part of an effort to develop useful thiamine derivatives. Medical useSulbutiamine is used to treat asthenia (symptoms of fatigue or weakness) in France.[1] It is not clear if it is effective.[2] Adverse effectsAdverse effects in clinical trials have included diarrhea, bladder infections, bronchitis, arthritic pain, back pain, asthma, abdominal pain, insomnia, constipation, gastroenteritis, diffuse pain, sinusitis, headache, kidney pain, vertigo, and sore throat.[2] HistoryEfforts to develop thiamine derivatives with better bioavaiability than thiamine were conducted in the 1950s, mainly in Japan. These efforts led to the discovery of allicin (diallyl thiosulfinate) in garlic, which became a model for medicinal chemistry efforts to create other thiamine disulfides. The results included sulbutiamine, fursultiamine (thiamine tetrahydrofurfuryl disulfide) and benfothiamine. These compounds are hydrophobic, easily pass from the intestines to the bloodstream, and are reduced to thiamine by cysteine or glutathione.[3]{{rp|302}}[4] It was first marketed in France by Servier in 1973 under the brand name Arcalion. The drug registration went through a validation procedure in France in the 1980s, which found that the use for treatment of fatigue was not supported by data.[2] Society and cultureThe French government does not pay for prescriptions of sulbutiamine.[1][5] Sulbutiamine is sold as a dietary supplement; it appears that endurance athletes may use it to try to enhance their performance.[6] It is also used as a nootropic dietary supplement; in 2014 the UK Medicines and Healthcare products Regulatory Agency seized a shipment of nootropics worth around £200,000 that included sulbutiamine.[7] ResearchBecause thiamine deficiency causes problems with memory and other cognitive functions, thiamine and analogs like sulbutiamine have been studied in clinical trials in the 1980s and 1990s for age-associated cognitive decline.[8] Sulbutiamine has been explored in clinical trials as a potential treatment for chronic fatigue syndrome.[2] The pharmacology of sulbutiamine has been studied in various mice and rats; as of 2014 it appeared that sulbutiamine might be more effective in raising thiamine phosphate levels in the brain than benfotiamine and fursultiamine, but this was not certain.[3]{{rp|303}} In a small 2017 study, sulbutiamine was reported to be effective in reducing fatigue in patients with multiple sclerosis.[9] See also
References1. ^1 {{cite web|title=Fiche info - Araclion 200 mg|url=http://base-donnees-publique.medicaments.gouv.fr/extrait.php?specid=64384738|publisher=Base de données publique des médicaments: ANSM of HAS et UNCAM.|access-date=28 January 2018|language=fr}} {{Vitamins}}2. ^1 {{cite journal | vauthors = Alraek T, Lee MS, Choi TY, Cao H, Liu J | title = Complementary and alternative medicine for patients with chronic fatigue syndrome: a systematic review | journal = BMC Complementary and Alternative Medicine | volume = 11 | pages = 87 | date = October 2011 | pmid = 21982120 | pmc = 3201900 | doi = 10.1186/1472-6882-11-87 }} 3. ^1 {{cite book|last1=Bettendorff|first1=Lucien|editor1-last=Zempleni|editor1-first=Janos|editor2-last=Suttie|editor2-first=John W.|editor3-last=Gregory|editor3-first=Jesse F.|editor4-last=Stover|editor4-first=Patrick J. | name-list-format = vanc |title=Handbook of vitamins|date=2014|publisher=CRC Press|location=Hoboken|isbn=9781466515574|pages=267–324|edition= Fifth |chapter=Chapter 7 - Thiamine}} 4. ^{{cite journal | vauthors = Volvert ML, Seyen S, Piette M, Evrard B, Gangolf M, Plumier JC, Bettendorff L | title = Benfotiamine, a synthetic S-acyl thiamine derivative, has different mechanisms of action and a different pharmacological profile than lipid-soluble thiamine disulfide derivatives | journal = BMC Pharmacology | volume = 8 | pages = 10 | date = June 2008 | pmid = 18549472 | pmc = 2435522 | doi = 10.1186/1471-2210-8-10 }} 5. ^1 2 {{cite journal |last1=Rane |first1=Wishvas | name-list-format = vanc |title=High Cost, Low Efficiency Medicines |journal=Economic and Political Weekly |date=1997 |volume=32 |issue=51 |pages=3251 |jstor=4406199}} 6. ^{{cite journal | vauthors = Kazlauskas R | title = Advances in sports drug testing: an overview | journal = Drug Testing and Analysis | volume = 2 | issue = 11-12 | pages = 523–5 | date = 2010 | pmid = 21204284 | doi = 10.1002/dta.251 }} {{open access}} 7. ^{{cite journal|title=Record seizure of experimental 'smart drugs' in UK|journal=Reactions Weekly|date=8 November 2014|volume=1526|issue=1|pages=4|doi=10.1007/s40278-014-4651-7}} 8. ^{{cite journal | vauthors = Riedel WJ, Jolles J | title = Cognition enhancers in age-related cognitive decline | journal = Drugs & Aging | volume = 8 | issue = 4 | pages = 245–74 | date = April 1996 | pmid = 8920174 | doi = 10.2165/00002512-199608040-00003 }} 9. ^{{cite journal | vauthors = Sevim S, Kaleağası H, Taşdelen B | title = Sulbutiamine shows promising results in reducing fatigue in patients with multiple sclerosis | journal = Multiple Sclerosis and Related Disorders | volume = 16 | pages = 40–43 | date = August 2017 | pmid = 28755683 | doi = 10.1016/j.msard.2017.05.010 }} 6 : Aromatic amines|Pyrimidines|Formamides|Isobutyrates|Organic disulfides|Thiamine |
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