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]

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 DaY
Hemijski podaci
Formula C17H12F3NO4 
Mol. masa 351,276 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status

Reference uredi

  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. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.  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. DOI:10.1186/1758-2946-2-3. PMID 20331846.  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. DOI:10.1093/nar/gkr777. PMID 21948594.  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. DOI:10.1021/jm900286j. PMID 19438238. 
  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. DOI:10.1016/j.tips.2008.12.002. PMC 2907736. PMID 19201489. 
  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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