Dimebolin

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IUPAC_name = 2,3,4,5-Tetrahydro-2,8-dimethyl-5-(2-(6-methyl-3-pyridyl)ethyl)-1H-pyrido(4,3-b)indole


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CAS_number = 3613-73-8
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PubChem = 197033
DrugBank =
C=21 | H=25 | N=3
molecular_weight = 319.443 g/mol
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Dimebolin Hydrochloride (brand name Dimebon) is an antihistamine drug which has been used clinically in Russia since 1983. [cite journal
author=Matveeva IA
title=Action of dimebon on histamine receptors
journal=Farmakologiia i Toksikologiia
year=1983
month=July-August
volume=46
issue=4
pages=27-29
language=Russian
pmid=]

Research is continuing in both Russia and western nations into potential applications as a neuroprotective and potential nootropic. [cite journal
author=Shevtsova EF, Kireeva EG, Bachurin SO
title=Mitochondria as the target for neuroprotectors
journal=Vestnik Rossiiskoi Akademii Meditsinskikh Nauk
year=2005
issue=9
pages=13-17
language=Russian]

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. [cite journal
author=Lermontova NN, Lukoyanov NV, Serkova TP, Lukoyanova EA, Bachurin SO
title=Dimebon improves learning in animals with experimental Alzheimer's disease
journal=Bulletin of Experimental Biology and Medicine
year=2000
month=June
volume=129
issue=6
pages=544-546
pmid= ] 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. [cite news
title=Antihistamine Shows Promise in Treating Alzheimer’s
publisher=New York Times
date=2007-06-11
url=http://www.nytimes.com/2007/06/11/business/11drug.html?ei=5090&en=6dd260f0ecf61466&ex=1339214400&partner=rssuserland&emc=rss&pagewanted=print] Dimebolin showed promising results in a Phase III-equivalent double blind trial in Russia with mild–moderate stage patients. [cite news
author=Phend Crystal, Jasmer Robert
date=2008-07-17
title=Old Antihistamine Pops Up as Potential Alzheimer's Therapy
url=http://www.medpagetoday.com/Geriatrics/AlzheimersDisease/tb/10174
journal=Medpage Today] [cite journal
title=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
author=Doody Rachelle S et al
journal=Lancet
date=2008-07-19
volume=372
pages=207–215
pmid=] It 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 it may also have cognition-enhancing effects in healthy individuals, in the absence of neurodegenerative disease pathology. [cite journal
author=Bachurin S, Bukatina E, Lermontova N, Tkachenko S, Afanasiev A, Grigoriev V, Grigorieva I, Ivanov Y, Sablin S, Zefirov N
title=Antihistamine agent Dimebon as a novel neuroprotector and a cognition enhancer
journal=Annals of the New York Academy of Sciences
year=2001
month=Jun
issue=939
pages=425-435
pmid=]

Pharmacology

Dimebolin appears to operate through multiple mechanisms of action, both blocking the action of neurotoxic beta-amyloid proteins and inhibiting L-type calcium channels, [cite journal
author=Lermontova NN, Redkozubov AE, Shevtsova EF, Serkova TP, Kireeva EG, Bachurin SO
title=Dimebon and tacrine inhibit neurotoxic action of beta-amyloid in culture and block L-type Ca(2+) channels
journal=Bulletin of Experimental Biology and Medicine
year=2001
month=Nov
volume=132
issue=5
page=1079-1083
pmid= ] modulating the action of AMPA and NMDA glutamate receptors, [cite journal
author=Grigorev VV, Dranyi OA, Bachurin SO
title=Comparative study of action mechanisms of dimebon and memantine on AMPA- and NMDA-subtypes glutamate receptors in rat cerebral neurons
journal=Bull Exp Biol Med
year=2003
month=November
volume=136
issue=5
pages=474-477 ] and may exert a neuroprotective effect by blocking a novel target that involves mitochondrial pores, [cite journal
author=Bachurin SO, Shevtsova EP, Kireeva EG, Oxenkrug GF, Sablin SO
title=Mitochondria as a target for neurotoxins and neuroprotective agents
journal=Annals of the New York Academy of Sciences
year=2003
month=May
volume=993
pages=334-344
pmid= ] which are believed to play a role in the cell death that is associated with neurodegenerative diseases and the aging process. [cite press release
date=2007-06-11
url=http://www.prnewswire.com/cgi-bin/stories.pl?ACCT=104&STORY=/www/story/06-11-2007/0004605280&EDATE=
title=Medivation's Dimebon(TM) Maintains Statistically Significant Benefit on All Five Efficacy Endpoints in Alzheimer's Disease Trial After One Year of Therapy]

References

ee also

* Donepezil
* Galantamine
* Memantine
* Rivastigmine