PF-04457845

Chemical compound
  • None
Legal statusLegal status
  • US: Investigational New Drug
Pharmacokinetic dataMetabolismCY3A4Identifiers
  • N-pyridazin-3-yl-4-[(3-[5-(trifluoromethyl)pyridin-2-yl]oxyphenyl)methylidene]piperidine-1-carboxamide
CAS Number
  • 1020315-31-4 checkY
PubChem CID
  • 24771824
ChemSpider
  • 26390839
UNII
  • H4C81M8YYW
ChEMBL
  • ChEMBL1651534
CompTox Dashboard (EPA)
  • DTXSID00144539 Edit this at Wikidata
Chemical and physical dataFormulaC23H20F3N5O2Molar mass455.441 g·mol−13D model (JSmol)
  • Interactive image
  • n4ncccc4NC(=O)N(CC3)CC\C3=C/c2cc(ccc2)Oc(cc1)ncc1C(F)(F)F
InChI
  • InChI=1S/C23H20F3N5O2/c24-23(25,26)18-6-7-21(27-15-18)33-19-4-1-3-17(14-19)13-16-8-11-31(12-9-16)22(32)29-20-5-2-10-28-30-20/h1-7,10,13-15H,8-9,11-12H2,(H,29,30,32)
  • Key:BATCTBJIJJEPHM-UHFFFAOYSA-N

JZP150 (formerly PF-04457845) is an inhibitor of the enzyme fatty acid amide hydrolase (FAAH), with an IC50 of 7.2nM, and both analgesic and antiinflammatory effects in animal studies comparable to naproxen.[1]

JZP150 is currently being developed by Jazz Pharmaceuticals and is in a Phase 2 trial in the US for PTSD. Patients will be given 0.3mg orally once per day for up to 12 weeks, or 4.0mg orally once per day for up to 12 weeks, or a placebo.[2]

See also

References

  1. ^ Johnson DS, Stiff C, Lazerwith SE, Kesten SR, Fay LK, Morris M, et al. (February 2011). "Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor". ACS Medicinal Chemistry Letters. 2 (2): 91–96. doi:10.1021/ml100190t. PMC 3109749. PMID 21666860.
  2. ^ "A Study of JZP150 in Adults With Posttraumatic Stress Disorder - Full Text View - ClinicalTrials.gov". clinicaltrials.gov.
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