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MK-0249

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MK-0249 is a histamine antagonist selective for the H₃ subtype.^[1]

[edit] References

^ Esbenshade TA, Browman KE, Bitner RS, Strakhova M, Cowart MD, Brioni JD (July 2008). "The histamine H3 receptor: an attractive target for the treatment of cognitive disorders". Br. J. Pharmacol. 154 (6): 1166–81. doi:10.1038/bjp.2008.147. PMC 2483387. PMID 18469850. //www.ncbi.nlm.nih.gov/pmc/articles/PMC2483387/.

H₁	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 Etodroxizine Etybenzatropine/Ethylbenztropine Etymemazine Flunarizine Histapyrrodine Homochlorcyclizine Hydroxyethylpromethazine Hydroxyzine Isopromethazine Isothipendyl Meclozine Mepyramine/Pyrilamine Mequitazine Methafurylene Methapyrilene Methdilazine Moxastine Niaprazine Orphenadrine Oxatomide Oxomemazine Phenindamine Pheniramine Phenyltoloxamine Pimethixene Piperoxan Pipoxizine Promethazine Propiomazine Pyrrobutamine Talastine Thenalidine Thenyldiamine Thiazinamium Thonzylamine Tolpropamine Tripelennamine Triprolidine 2nd generation: Acrivastine Alinastine Astemizole Azelastine Bamirastine Barmastine Bepiastine Bepotastine Bilastine Cabastinen Carebastine Cetirizine Clemastine Clemizole Clobenztropine Dorastine Ebastine Emedastine Epinastine Flezelastine Ketotifen Latrepirdine Levocabastine Linetastine Loratadine Mapinastine Mebhydrolin Mizolastine Moxastine Noberastine Octastine Olopatadine Perastine Piclopastine Rocastine Rupatadine Setastine Talastine Temelastine Terfenadine Zepastine 3rd generation: Desloratadine Fexofenadine Levocetirizine Ungrouped: Belarizine Efletirizine Elbanizine Flotrenizine Medrylamine Napactadine Pibaxizine Tagorizine Trelnarizine Trenizine Vapitadine Miscellaneous: Tricyclic antidepressants (amitriptyline, doxepin, trimipramine, etc) Tetracyclic antidepressants (mianserin, mirtazapine, etc) Typical antipsychotics (chlorpromazine, thioridazine, etc) Atypical antipsychotics (clozapine, olanzapine, quetiapine, etc)

H₂	Agonists: Amthamine Betazole Dimaprit Histamine HTMT Impromidine UR-AK49 Antagonists: Bisfentidine Burimamide Cimetidine Dalcotidine Donetidine Ebrotidine Etintidine Famotidine Lafutidine Lamtidine Lavoltidine/Loxtidine Lupitidine Metiamide Mifentidine Niperotidine Nizatidine Osutidine Oxmetidine Pibutidine Quisultazine/Quisultidine Ramixotidine Ranitidine Roxatidine Sufotidine Tiotidine Tuvatidine Venritidine Xaltidine

H₃	Agonists: α-Methylhistamine Cipralisant Histamine Imetit Immepip Immethridine Methimepip Proxyfan Antagonists: A-349,821 A-423,579 ABT-239 Betahistine Burimamide Ciproxifan Clobenpropit Conessine GSK-189,254 Impentamine Iodophenpropit JNJ-5,207,852 MK-0249 NNC-38-1,049 PF-03654746 Pitolisant SCH-79,687 Thioperamide VUF-5,681

H₄	Agonists: 4-Methylhistamine Histamine VUF-8,430 Antagonists: JNJ-7,777,120 Thioperamide VUF-6,002

VMAT	Inhibitors: Ibogaine Reserpine Tetrabenazine

HDC	Inhibitors: Catechin Meciadanol Naringenin Tritoqualine

DAO	Inhibitors: Aminoguanidine

Others

Endogenous	Histamine; Precursors: L-Histidine; Cofactors: Vitamin B6

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