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PF-03654746

S Vikipedije, slobodne enciklopedije
PF-03654746
IUPAC ime
(1R,3R)-N-etil-3-fluoro-3-[3-fluoro-4-(pirolidin-1-ilmetil)fenil]ciklobutan-1-karboksamid
Identifikatori
ATC kodnone
PubChemCID 16119086
Hemijski podaci
FormulaC18H24F2N2O
Molarna masa322,392
  • C2CCCN2Cc1ccc(cc1F)C3(F)CC(C3)C(=O)NCC

PF-03654746 je potentan i selektivan antagonist histaminskog H3 receptor koji je razvila kompanija Pfizer i trenutno je u kliničkim ispitivanjima za tretman ADHD-a, Toretovog sindroma,[1] kao i za potencijalne antialergijske primene.[2][3][4][5]

Reference

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  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: 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. (2009). „H3 receptor antagonism increases methylhistamine levels in the cerebrospinal fluid of dogs and healthy human volunteers”. Alzheimer's and Dementia. 5 (4): 254. 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. PMID 19429511. doi:10.1016/j.drudis.2009.02.011. 
  5. ^ Wijtmans, M.; Denonne, F.; Célanire, S.; Gillard, M.; Hulscher, S.; Delaunoy, C.; Van Houtvin, N.; Bakker, R. A.; Defays, S. (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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