词条 | Tideglusib |
释义 |
| drug_name = | IUPAC_name = 4-Benzyl-2-(naphthalen-1-yl)-1,2,4-thiadiazolidine-3,5-dione | image = Tideglusib2DACS.svg | width = 200 | image2 = Tideglusib-ball-and-stick-model.png | width2 = 200 | tradename = | Drugs.com = | MedlinePlus = | 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 = 865854-05-3 | ATCvet = | ATC_prefix = | ATC_suffix = | PubChem = 11313622 | ChemSpiderID = 9488589 | DrugBank = | C=19 | H=14 | N=2 | O=2 | S=1 | molecular_weight = 334.392 g/mol | smiles = O=C3SN(c1cccc2c1cccc2)C(=O)N3Cc4ccccc4 | StdInChI = 1S/C19H14N2O2S/c22-18-20(13-14-7-2-1-3-8-14)19(23)24-21(18)17-12-6-10-15-9-4-5-11-16(15)17/h1-12H,13H2 }} Tideglusib (NP-12, NP031112) is a potent, selective and irreversible[1] small molecule non-ATP-competitive glycogen synthase kinase 3 (GSK-3) inhibitor. Potential applicationsTideglusib is under investigation for multiple applications:
References1. ^{{cite journal|title=Evidence for Irreversible Inhibition of Glycogen Synthase Kinase-3 by Tideglusib|journal=The Journal of Biological Chemistry|date=January 2012|volume=287|issue=2|pages=893–904|doi=10.1074/jbc.M111.306472|pmid=22102280|pmc=3256883|author1=Domínguez, JM |author2=Fuertes, A |author3=Orozco, L |author4=del Monte-Millán, M |author5=Delgado, E |author6=Medina, M |url=http://www.jbc.org/content/287/2/893.full.pdf}} {{nervous-system-drug-stub}}2. ^{{cite journal | doi = 10.1016/j.jalz.2010.05.455 | title = Phase IIa clinical trial on Alzheimer's disease with NP12, a GSK3 inhibitor | year = 2010 | last1 = Teodoro Del Ser | journal = Alzheimer's & Dementia | volume = 6 | issue = 4 | pages = S147}} 3. ^{{cite journal | pmc = 3204427 | last1 = Eldar-Finkelman | first1 = H | last2 = Martinez | first2 = A | title = GSK-3 Inhibitors: Preclinical and Clinical Focus on CNS | volume = 4 | pages = 32 | doi = 10.3389/fnmol.2011.00032 | journal = Frontiers in Molecular Neuroscience | year = 2011 | pmid = 22065134}} 4. ^1 {{cite journal | doi = 10.3233/JAD-2012-120805 | pmid = 22936007 | year = 2013 | last1 = Del Ser | first1 = T | last2 = Steinwachs | first2 = KC | last3 = Gertz | first3 = HJ | last4 = Andrés | first4 = MV | last5 = Gómez-Carrillo | first5 = B | last6 = Medina | first6 = M | last7 = Vericat | first7 = JA | last8 = Redondo | first8 = P | last9 = Fleet | first9 = D | last10 = León | first10 = T | title = Treatment of Alzheimer's disease with the GSK-3 inhibitor tideglusib: A pilot study | volume = 33 | issue = 1 | pages = 205–15 | journal = Journal of Alzheimer's Disease| display-authors = 8 }} 5. ^{{cite web | title = FDA Grants Fast Track Status to Tideglusib (ZentylorTM) for Progressive Supranuclear Palsy | publisher = PR Newswire Europe Including UK Disclose | date = 10 September 2010 | accessdate = 11 August 2013 | url = http://search.proquest.com/docview/750175748}} 6. ^{{cite journal | doi = 10.1074/jbc.M111.306472 | title = Evidence for Irreversible Inhibition of Glycogen Synthase Kinase-3 by Tideglusib | year = 2011 | last1 = Dominguez | first1 = JM | last2 = Fuertes | first2 = A | last3 = Orozco | first3 = L | last4 = Del Monte-Millan | first4 = M | last5 = Delgado | first5 = E | last6 = Medina | first6 = M | journal = Journal of Biological Chemistry | volume = 287 | issue = 2 | pages = 893–904 | pmid = 22102280 | pmc = 3256883}} 7. ^{{Cite news |url=https://www.bbc.co.uk/news/uk-38524566 |title='Tooth repair drug' may replace fillings |last=Gallagher |first=James |date=2017-01-09 |newspaper=BBC News |access-date=2017-01-09}} 8. ^{{cite web|title=AMO-2|url=http://www.amo-pharma.com/amo_02.htm|website=AMO Pharmaceuticals|accessdate=2017-09-21}} 3 : Alzheimer's disease research|Naphthalenes|Thiadiazoles |
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