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20-September-2008 09:55:57 - Dimebon Dimebon Systematic IUPAC name 2,3,4,5-Tetrahydro-2,8-dimethyl-5-2-6-methyl-3-pyridylethyl- 1H-pyrido4,3-bindole Identifiers CAS number 3613-73-8 ATC code ? PubChem 197033 Chemical data Formula C21H25N3 Mol. mass 319.443 g/mol Pharmacokinetic data Bioavailability ? Metabolism ? Half life ? Excretion ? Therapeutic considerations Pregnancy cat. ? Legal status Routes ? Dimebolin Hydrochloride Dimebon is an antihistamine drug which has been used clinically in Russia since 1983.1 Research is continuing in both Russia and western nations into the potential applications of Dimebon as a neuroprotective and potential nootropic. 2 Contents 1 Uses 2 Pharmacology 3 References 4 See also Uses Recently Dimebolin has attracted renewed interest after being shown to have positive effects on persons suffering from Alzheimer's disease. Animal studies showing potential beneficial effects on Alzheimer's disease models were shown in Russian research in 2000.3 Preliminary results from human trials have also been promising. In an initial six-month phase II trial, results have shown that at 12 months there was significant improvement over placebo. 4 Dimebon showed promising results in a Phase III-equivalent double blind trial in Russia with mild-moderate stage patients.56 Dimebolin is an orally active small molecule that has been shown to inhibit brain cell death in preclinical studies of Alzheimer's disease and Huntington's disease, making it a potential treatment for these and other neurodegenerative diseases. Research suggests that Dimebon may also have cognition-enhancing effects in healthy individuals, in the absence of neurodegenerative disease pathology.7 Pharmacology Dimebon appears to operate through multiple mechanisms of action, both blocking the action of neurotoxic beta-amyloid proteins and inhibiting L-type calcium channels,8 modulating the action of AMPA and NMDA glutamate receptors,9 and may exert a neuroprotective effect by blocking a novel target that involves mitochondrial pores,10 which are believed to play a role in the cell death that is associated with neurodegenerative diseases and the aging process.11 References ^ Matveeva IA July-August 1983. Action of dimebon on histamine receptors in Russian. Farmakologiia i Toksikologiia 46 4: 27-29. ^ Shevtsova EF, Kireeva EG, Bachurin SO 2005. Mitochondria as the target for neuroprotectors in Russian. Vestnik Rossiiskoi Akademii Msinskikh Nauk 9: 13-17. ^ Lermontova NN, Lukoyanov NV, Serkova TP, Lukoyanova EA, Bachurin SO June 2000. Dimebon improves learning in animals with experimental Alzheimer's disease. Bulletin of Experimental Biology and Medicine 129 6: 544-546. ^ Antihistamine Shows Promise in Treating Alzheimer's, New York Times 2007-06-11. ^ Phend Crystal, Jasmer Robert 2008-07-17. Old Antihistamine Pops Up as Potential Alzheimer's Therapy. ^ Doody Rachelle S et al 2008-07-19. Effect of dimebon on cognition, activities of daily living, behaviour, and global function in patients with mild-to-moderate Alzheimer's disease: A randomised, double-blind, placebo-controlled study. Lancet 372: 207-215. ^ Bachurin S, Bukatina E, Lermontova N, Tkachenko S, Afanasiev A, Grigoriev V, Grigorieva I, Ivanov Y, Sablin S, Zefirov N Jun 2001. Antihistamine agent Dimebon as a novel neuroprotector and a cognition enhancer. Annals of the New York Academy of Sciences 939: 425-435. ^ Lermontova NN, Redkozubov AE, Shevtsova EF, Serkova TP, Kireeva EG, Bachurin SO Nov 2001. Dimebon and tacrine inhibit neurotoxic action of beta-amyloid in culture and block L-type Ca2+ channels. Bulletin of Experimental Biology and Medicine 132 5. ^ Grigorev VV, Dranyi OA, Bachurin SO November 2003. Comparative study of action mechanisms of dimebon and memantine on AMPA- and NMDA-subtypes glutamate receptors in rat cerebral neurons. Bull Exp Biol Med 136 5: 474-477. ^ Bachurin SO, Shevtsova EP, Kireeva EG, Oxenkrug GF, Sablin SO May 2003. Mitochondria as a target for neurotoxins and neuroprotective agents. Annals of the New York Academy of Sciences 993: 334-344. ^ 2007-06-11. Medivation's DimebonTM Maintains Statistically Significant Benefit on All Five Efficacy Endpoints in Alzheimer's Disease Trial After One Year of Therapy. Press release. See also Donepezil Galantamine Memantine Rivastigmine 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/Dimebon Categories: Nootropics | H1 receptor antagonists 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 Languages РуÑ?Ñ?кий This page was last modified on 5 August 2008, at 02:45
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