PF-03654746

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]

PF-03654746
Identifiers
  • 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)
  • CCNC(=O)[C@H]1C[C@@](C1)(F)C2=CC(=C(C=C2)CN3CCCC3)F
  • 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)

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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