PF-03654746

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PF-03654746
(IUPAC) ime
(1R,3R)-N-etil-3-fluoro-3-[3-fluoro-4-(pirolidin-1-ilmetil)fenil]ciklobutan-1-karboksamid
Klinički podaci
Identifikatori
ATC kod nije dodeljen
PubChem[1][2] 16119086
Hemijski podaci
Formula C18H24F2N2O 
Mol. masa 322,392
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status

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,[3] kao i za potencijalne antialergijske primene.[4][5][6][7]

Reference[uredi - уреди | uredi izvor]

  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). "PubChem as a public resource for drug discovery.". Drug Discov Today 15 (23-24): 1052–7. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  edit
  2. Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). "Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities". Annual Reports in Computational Chemistry 4: 217–241. doi:10.1016/S1574-1400(08)00012-1. 
  3. 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
  4. 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. 
  5. 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): P254. doi:10.1016/j.jalz.2009.04.272. 
  6. 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. 
  7. 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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