PF-03654746

PF-03654746
Systematic (IUPAC) name
trans-N-Ethyl-3-fluoro-3-[3-fluoro-4-(1-pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide
Identifiers
PubChem CID 16119086
ChemSpider 25069700
Chemical data
Formula C18H24F2N2O
Molar mass 322.392
  (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. ↑ Pfizer: "Study Evaluating The Safety And Efficacy Of PF-03654746 In Adult Subjects With Tourette's Syndrome", http://clinicaltrials.gov/ct2/show/NCT01475383, accessed 06 Jan 2012
  2. ↑ Romero Jr., F. A.; Allan, R. J.; Phillips, P. G.; Hutchinson, K.; Misfeldt, J. M.; Casale, T. B. (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. ↑ Soares, H.; Wager, T. T.; Schmidt, A. W.; Sweeney, F. J.; McLellan, T. J.; Nelson, F. R.; Spracklin, D.; Wang, E. Q.; Faessel, H.; Pinter, G. W.; Li, X.; Chappell, P. B. (2009). "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.
  4. ↑ Gemkow, M.; Davenport, A.; Harich, S.; Ellenbroek, B.; Cesura, A.; Hallett, D. (2009). "The histamine H3 receptor as a therapeutic drug target for CNS disorders". Drug Discovery Today 14 (9–10): 509–515. doi:10.1016/j.drudis.2009.02.011. PMID 19429511.
  5. ↑ Wijtmans, M.; Denonne, F.; Célanire, S.; Gillard, M.; Hulscher, S.; Delaunoy, C.; Van Houtvin, N.; Bakker, R. A.; Defays, S.; Gérard, J.; Grooters, L.; Hubert, D.; Timmerman, H.; Leurs, R.; Talaga, P.; De Esch, I. J. P.; Provins, L. (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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