PF-03654746

PF-03654746
Identifiers
IUPAC name
  • trans-N-Ethyl-3-fluoro-3-[3-fluoro-4-(1-pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC18H24F2N2O
Molar mass322.392 g·mol−1
3D model (JSmol)
SMILES
  • CCNC(=O)[C@H]1C[C@@](C1)(F)C2=CC(=C(C=C2)CN3CCCC3)F
InChI
  • InChI=1S/C18H24F2N2O/c1-2-21-17(23)14-10-18(20,11-14)15-6-5-13(16(19)9-15)12-22-7-3-4-8-22/h5-6,9,14H,2-4,7-8,10-12H2,1H3,(H,21,23)/t14-,18-
  • Key:SXMBKHYDZOCBMT-PPUGGXLSSA-N
  (verify)

PF-03654746 is a potent and selective histamine H3 receptor antagonist developed by Pfizer and currently undergoing clinical trials for the treatment of ADHD, Tourette syndrome[1] as well as potential anti-allergy applications.[2][3][4][5]

References

  1. ↑ Clinical trial number NCT01475383 for "Study Evaluating The Safety And Efficacy Of PF-03654746 In Adult Subjects With Tourette's Syndrome" at ClinicalTrials.gov
  2. ↑ Soares H, Wager TT, Schmidt AW, Sweeney FJ, McLellan TJ, Nelson FR, Spracklin D, Wang EQ, Faessel H, Pinter GW, Li X (2010). "The Effects of an H3 Receptor Antagonist in a Nasal Allergen Challenge Model". Journal of Allergy and Clinical Immunology. 125 (2): AB191. doi:10.1016/j.jaci.2009.12.750.
  3. ↑ "H3 receptor antagonism increases methylhistamine levels in the cerebrospinal fluid of dogs and healthy human volunteers". Alzheimer's & Dementia. 5 (4): P254. doi:10.1016/j.jalz.2009.04.272. S2CID 54316270.
  4. ↑ Gemkow MJ, Davenport AJ, Harich S, Ellenbroek BA, Cesura A, Hallett D (May 2009). "The histamine H3 receptor as a therapeutic drug target for CNS disorders". Drug Discovery Today. 14 (9–10): 509–15. doi:10.1016/j.drudis.2009.02.011. PMID 19429511.
  5. ↑ Wijtmans M, Denonne F, Célanire S, Gillard M, Hulscher S, Delaunoy C, Bakker RA, Defays S, Gérard J, Grooters L, Hubert D (2010). "Histamine H3 receptor ligands with a 3-cyclobutoxy motif: a novel and versatile constraint of the classical 3-propoxy linker". MedChemComm. 1: 39. doi:10.1039/c0md00056f.
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