PF-03654746
PF-03654746 is a potent and selective histamine H3 receptor antagonist developed by Pfizer and currently undergoing clinical trials for the treatment of ADHD, as well as potential anti-allergy applications.[1][2][3][4]
References
- ^ 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. edit
- ^ Soares, H.; Wager, T. T.; Schmidt, A. W.; Sweeney, F. J.; McLellan, T. J.; Nelson, F. R.; Spracklin, D.; Wang, E. Q. et al. (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. edit
- ^ 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. edit
- ^ Wijtmans, M.; Denonne, F.; Célanire, S.; Gillard, M.; Hulscher, S.; Delaunoy, C.; Van Houtvin, N.; Bakker, R. A. et al. (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. edit
|
|
|
Receptor
ligands |
|
|
Agonists: 2-Pyridylethylamine • Betahistine • Histamine • HTMT • UR-AK49
Antagonists: "1st generation": 4-Methyldiphenhydramine • Alimemazine • Antazoline • Azatadine • Bamipine • Benzatropine (Benztropine) • Bepotastine • Bromazine • Brompheniramine • Buclizine • Captodiame • Carbinoxamine • Chlorcyclizine • Chloropyramine • Chlorothen • Chlorphenamine • Chlorphenoxamine • Cinnarizine • Clemastine • Clobenzepam • Clocinizine • Cyclizine • Cyproheptadine • Dacemazine • Deptropine • Dexbrompheniramine • Dexchlorpheniramine • Dimenhydrinate • Dimetindene • Diphenhydramine • Diphenylpyraline • Doxylamine • Embramine • Etybenzatropine (Ethylbenztropine) • Etymemazine • Histapyrrodine • Homochlorcyclizine • Hydroxyethylpromethazine • Hydroxyzine • Isopromethazine • Isothipendyl • Meclozine • Mepyramine (Pyrilamine) • Mequitazine • Methafurylene • Methapyrilene • Methdilazine • Moxastine • Niaprazine • Orphenadrine • Oxatomide • Oxomemazine • Phenindamine • Pheniramine • Phenyltoloxamine • Pimethixene • Piperoxan • Promethazine • Propiomazine • Pyrrobutamine • Talastine • Thenalidine • Thenyldiamine • Thiazinamium • Thonzylamine • Tolpropamine • Tripelennamine • Triprolidine; "2nd generation": Acrivastine • Astemizole • Azelastine • Cetirizine • Clemizole • Clobenztropine • Ebastine • Emedastine • Epinastine • Ketotifen • Latrepirdine • Levocabastine • Loratadine • Mebhydrolin • Mizolastine • Olopatadine • Rupatadine • Setastine • Terfenadine; "3rd generation": Desloratadine • Fexofenadine • Levocetirizine; Miscellaneous: Tricyclic antidepressants ( Amitriptyline, Doxepin, Trimipramine, etc) • Tetracyclic antidepressants ( Mianserin, Mirtazapine, etc) • Serotonin antagonist and reuptake inhibitors ( Trazodone, Nefazodone) • Typical antipsychotics ( Chlorpromazine, Thioridazine, etc) • Atypical antipsychotics ( Clozapine, Olanzapine, Quetiapine, etc)
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
Reuptake
inhibitors |
|
|
Enzyme
inhibitors |
|
|
| Others |
|
|