PF-03654746
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(IUPAC) ime | |||
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(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 | ||
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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
- ↑ 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. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
- ↑ 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.
- ↑ 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. i dr.. (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.
- ↑ 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.
- ↑ Wijtmans, M.; Denonne, F.; Célanire, S.; Gillard, M.; Hulscher, S.; Delaunoy, C.; Van Houtvin, N.; Bakker, R. A. i dr.. (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
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Inhibitori: Aminoguanidin |
Histamin; Prekursori: L-Histidin; Kofaktori: Vitamin B6 |