VU-0238429

From Wikipedia, the free encyclopedia
Jump to: navigation, search
VU-0238429
VU0238429 structure.png
Systematic (IUPAC) name
1-(4-methoxybenzyl)-5-(trifluoromethoxy)indole-2,3-dione
Clinical data
Legal status ?
Identifiers
CAS number  YesY
ATC code ?
PubChem CID 42633508
ChemSpider 24606034 YesY
ChEMBL CHEMBL466253 YesY
Chemical data
Formula C17H12F3NO4 
Mol. mass 351.276 g/mol
 YesY (what is this?)  (verify)

VU-0238429 is a drug which acts as a selective positive allosteric modulator for the muscarinic acetylcholine receptor M5. It was the first selective ligand developed for the M5 subtype,[1] and is structurally derived from older M1-selective positive allosteric modulators such as VU-0119498.[2][3] Replacing the O-methyl- by a phenylgroup further improves the receptor subtype selectivity (VU-0400265).


References[edit]

  1. ^ 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. 
  2. ^ 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. 
  3. ^ 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.  edit