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20-September-2008 09:55:57 - H3 antagonist The correct title of this article is H3 antagonist. It features superscript or subscript characters that are substituted or omitted because of technical limitations. An H3-receptor antagonist is a classification of drugs used to block the action of histamine on the Histamine H3 receptor. Unlike the H1 and H2 receptors which have primarily peripheral actions, but cause sedation if they are blocked in the brain, H3 receptors are primarily found in the brain and are inhibitory autoreceptors located on histaminergic nerve terminals, which modulate the release of histamine. Histamine release in the brain triggers secondary release of excitatory neurotransmitters such as glutamate and acetylcholine via stimulation of H1 receptors in the cerebral cortex. Consequently unlike the H1 antagonist antihistamines which are sedating, H3 antagonists have stimulant and nootropic effects, and are being researched as potential drugs for the treatment of neurodegenerative conditions such as Alzheimer's disease. Examples of selective H3 antagonists include clobenpropit,1 ABT-239,2 ciproxifan,3 and A-349,821.4 References ^ Yoneyama H, Shimoda A, Araki L, et al March 2008. Efficient approaches to S-alkyl-N-alkylisothioureas: syntheses of histamine H3 antagonist clobenpropit and its analogues. J. Org. Chem. 73 6: 2096-104. doi:10.1021/jo702181x. PMID 18278935. ^ Fox GB, Esbenshade TA, Pan JB, Radek RJ, Krueger KM, Yao BB, Browman KE, Buckley MJ, Ballard ME, Komater VA, Miner H, Zhang M, Faghih R, Rueter LE, Bitner RS, Drescher KU, Wetter J, Marsh K, Lemaire M, Porsolt RD, Bennani YL, Sullivan JP, Cowart MD, Decker MW, Hancock AA 2005. Pharmacological properties of ABT-239 4-2-2-2R-2-Methylpyrrolidinylethyl-benzofuran-5-ylbenzonitrile: II. Neurophysiological characterization and broad preclinical efficacy in cognition and schizophrenia of a potent and selective histamine H3 receptor antagonist. J. Pharmacol. Exp. Ther. 313 1: 176-90. doi:10.1124/jpet.104.078402. PMID 15608077. ^ LLigneau X, Lin J, Vanni-Mercier G, Jouvet M, Muir JL, Ganellin CR, Stark H, Elz S, Schunack W, Schwartz J November 1998. Neurochemical and behavioral effects of ciproxifan, a potent histamine H3-receptor antagonist. J. Pharmacol. Exp. Ther. 287 2: 658-66. doi:10.1016/j.bcp.2007.01.002. PMID 9808693. ^ Esbenshade TA, Fox GB, Krueger KM, Baranowski JL, Miller TR, Kang CH, Denny LI, Witte DG, Yao BB, Pan JB, Faghih R, Bennani YL, Williams M, Hancock AA. Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist. Biochemical Pharmacology. 2004 Sep 1;685:933-45. PMID 15294456 v d e Receptor agonists, antagonists, and reuptake inhibitors BA/M 5-HT serotonin receptor Serotonin receptor agonist 5-HT4 Serotonin antagonist 5-HT3 Serotonin uptake inhibitor SSRI Dopamine receptor Dopamine agonist Dopamine antagonist Dopamine reuptake inhibitor Adrenergic receptor Adrenergic agonist Alpha, Beta 1/2 Adrenergic antagonist Alpha 1/2, Beta Adrenergic uptake inhibitor Histamine receptor Histamine agonist Histamine antagonist H1, H2, H3 AA GABA receptor GABA agonist GABA antagonist Glutamate receptor NMDA receptor NMDA receptor antagonist AMPA receptor Ampakine Excitatory amino acid agonist Excitatory amino acid antagonist ANS Acetylcholine receptor Cholinergic Muscarinic, Nicotinic Anticholinergic Muscarinic, Nicotinic/Ganglionic blocker/Neuromuscular-blocking drugs Acetylcholinesterase inhibitor Adrenergic receptor SANS only -- see above for details PANS Parasympathomimetic Cholinergic, Acetylcholinesterase inhibitor - Parasympatholytic Anticholinergic, Ganglionic blocker SANS Sympathomimetic Adrenergic agonist, Monoamine oxidase inhibitor - Sympatholytic Adrenergic antagonist, Alpha blocker, Ganglionic blocker v d e Histamine antagonists H1 or non-selective Alkylamines Bepotastine Bamipine Brompheniramine Chlorpheniramine Dexbrompheniramine Dexchlorpheniramine Dimethindene Metron S Pheniramine Pyrrobutamine Talastine Thenaldine Tolpropamine Triprolidine Ethanolamines Aminoalkyl ethers Bietanautine Bromazine/Bromodiphenhydramine Carbinoxamine Chlorphenoxamine Clemastine Diphenylpyraline Diphenhydramine Doxylamine Embramine p-Methyldiphenhydramine Moxastine Orphenadrine Phenyltoloxamine Setastine Ethylenediamines Chloropyramine Chlorothen Histapyrrodine Methafurylene Mepyramine Methapyrilene Pyrilamine Talastine Thenyldiamine Thonzylamine Tripelennamine Pyribenzamine Phenothiazine Tricyclics Ahistan Etymemazine Hydroxyethylpromethazine Isopromethazine Isothipendyl Mequitazine Methdilazine Oxomemazine Promethazine Thiazinamium Other Tricyclics Azatadine Clobenzepam Cyproheptadine Deptropine Isothipendyl Loratidine Piperazine Buclizine Chlorcyclizine Cinnarizine Clocinizine Hydroxyzine Niaprazine Oxatomide Benzhydryl compounds Cyclizine, Meclizine Others including selective, 2nd gen, 3rd gen Antazoline Astemizole Azatadine Azelastine Bepottastine Bamipine Cetoxine Clemizole Clobenztropine Deptropine Desloratadine Dimebon Ebastine Emedastine Epinastine Ketotifen Levocabastine Loratadine Mebhydrolin Mizolastine Phenindamine Pimethixene Pyrrobutamine Rupatadine Thenalidine Tritoqualine Alkylamine Acrivastine Tricyclic Olopatadine Piperazine Levocetirizine, Cetirizine Benzhydryl compounds Fexofenadine, Terfenadine H2 Cimetidine Famotidine Ranitidine Roxatidine Lafutidine Niperotidine Nizatidine H3 A-349,821 ABT-239 Burimamide Ciproxifan Clobenpropit Conessine Impentamine Iodophenpropit Thioperamide VUF-5681 H4 JNJ 7777120 Thioperamide VUF-6002 v d e Psychoanaleptics: psychostimulants, agents used for ADHD and nootropics N06B Centrally acting sympathomimetics Amphetamine - Amphetaminil - Atomoxetine - Dextroamphetamine - Dextromethamphetamine - Fencamfamin - Fenozolone - Fenetylline - Methylphenidate - Mesocarb - Pemoline - Pipradrol - Prolintane Xanthine derivatives Caffeine - Propentofylline Glutamate receptor Racetams Aniracetam - Nefiracetam - Oxiracetam - Phenylpiracetam - Piracetam - Pramiracetam Ampakines CX-516 - CX-546 - CX-614 - CX-691 - CX-717 - IDRA-21 - LY-503,430 - PEPA Eugeroics / Benzhydryl compounds Adrafinil - Armodafinil - Modafinil Histamine H3 receptor antagonists ABT-239 - Ciproxifan Other psychostimulants and nootropics Acetylcarnitine - Citicoline - Cyprodenate - Idebenone - Ispronicline - Deanol - Dimebon - Fipexide - Linopirdine - Meclofenoxate - Nizofenone - Pirisudanol - Pyritinol - Sulbutiamine - Taltirelin - Tricyanoaminopropene - Vinpocetine Retrieved from http://en..org/wiki/H3_antagonist Categories: Antihistamines Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page This page was last modified on 2 August 2008, at 05:1
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