VU-0238429

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VU-0238429
(IUPAC) ime
1-(4-metoksibenzil)-5-(trifluorometoksi)indol-2,3-dion
Klinički podaci
Identifikatori
ATC kod ?
PubChem[1][2] 42633508
ChemSpider[3] 24606034
ChEMBL[4] CHEMBL466253 YesY
Hemijski podaci
Formula C17H12F3NO4 
Mol. masa 351,276 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status

VU-0238429 je lek koji deluje kao selektivni pozitivni alosterni modulator za muskarinski acetilholinski receptor M5. On je bio prvi selektivni ligand razvijen za M5 podtip.[5] VU-0238429 je strukturni derivat raznije otkrivenih M1-selektivnih pozitivnih alosternih modulatora poput VU-0119498.[6][7]

Reference[uredi - уреди | uredi izvor]

  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). "PubChem as a public resource for drug discovery.". Drug Discov Today 15 (23-24): 1052–7. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  edit
  2. Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). "Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities". Annual Reports in Computational Chemistry 4: 217–241. doi:10.1016/S1574-1400(08)00012-1. 
  3. Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). "Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining". J Cheminform 2 (1): 3. PMID 20331846. doi:10.1186/1758-2946-2-3.  edit
  4. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). "ChEMBL: a large-scale bioactivity database for drug discovery". Nucleic Acids Res 40 (Database issue): D1100–7. PMID 21948594. doi:10.1093/nar/gkr777.  edit
  5. Bridges TM, Marlo JE, Niswender CM et al. (June 2009). "Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins". Journal of Medicinal Chemistry 52 (11): 3445–8. PMID 19438238. doi:10.1021/jm900286j. 
  6. Conn PJ, Jones CK, Lindsley CW (March 2009). "Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders". Trends in Pharmacological Sciences 30 (3): 148–55. PMC 2907736. PMID 19201489. doi:10.1016/j.tips.2008.12.002. 
  7. Bridges T. M., Kennedy J. P., Hopkins C. R., Conn P. J., Lindsley C. W. (2010). "Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators". Bioorganic & Medicinal Chemistry Letters 20 (19): 5617. doi:10.1016/j.bmcl.2010.08.042. 

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