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PF-514273

Summary

PF-514273 is a drug developed by Pfizer, which acts as an extremely selective antagonist for the CB1 receptor, with approximately 10,000x selectivity over the closely related CB2 receptor. This very high selectivity makes it useful for scientific research into these receptors, as many commonly used cannabinoid receptor antagonists also block the CB2 receptor to some extent.[1]

PF-514273
Identifiers
  • 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one
CAS Number
  • 851728-60-4 checkY
PubChem CID
  • 11316919
ChemSpider
  • 9491886 ☒N
UNII
  • 45FRJ4YGM2
CompTox Dashboard (EPA)
  • DTXSID80462142 Edit this at Wikidata
Chemical and physical data
FormulaC21H17Cl2F2N3O2
Molar mass452.28 g·mol−1
3D model (JSmol)
  • Interactive image
  • O=C1N(CC(F)(C)F)CCOc2c1nn(c2-c(cc4)ccc4Cl)-c3ccccc3Cl
  • InChI=1S/C21H17Cl2F2N3O2/c1-21(24,25)12-27-10-11-30-19-17(20(27)29)26-28(16-5-3-2-4-15(16)23)18(19)13-6-8-14(22)9-7-13/h2-9H,10-12H2,1H3
  • Key:FJMQJSUOOGOWBD-UHFFFAOYSA-N
 ☒NcheckY (what is this?)

References edit

  1. ^ Dow RL, Carpino PA, Hadcock JR, Black SC, Iredale PA, DaSilva-Jardine P, et al. (May 2009). "Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity". Journal of Medicinal Chemistry. 52 (9): 2652–5. doi:10.1021/jm900255t. PMID 19351113.