PF-03654746
IUPAC ime | |
---|---|
(1R,3R)-N-etil-3-fluoro-3-[3-fluoro-4-(pirolidin-1-ilmetil)fenil]ciklobutan-1-karboksamid | |
Identifikatori | |
ATC kod | none |
PubChem | CID 16119086 |
Hemijski podaci | |
Formula | C18H24F2N2O |
Molarna masa | 322,392 |
SMILES
| |
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
- ^ 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
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
Spoljašnje veze
- p
- r
- u
Histaminergici
VMAT |
---|
HDC | |
---|---|
HNMT | |
DAO | Inhibitori: Aminoguanidin |
Endogeni | Histamin; Prekursori: L-Histidin; Kofaktori: Vitamin B6 |
---|
PF-03654746 на Викимедијиној остави.