Dimebon
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Dimebon
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| Systematic (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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| Identifiers | |
| CAS number | |
| ATC code | ? |
| PubChem | |
| Chemical data | |
| Formula | C21H25N3 |
| Mol. mass | 319.443 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
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| Legal status | |
| Routes | ? |
Dimebon (Dimebolin) is an antihistamine drug which has been used clinically in Russia since 1983.[1]
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.[2] 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. [3]
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.[4]
Dimebon appears to operate through multiple mechanisms of action, both blocking the action of neurotoxic beta-amyloid proteins and inhibiting L-type calcium channels,[5] modulating the action of AMPA and NMDA glutamate receptors,[6] and may exert a neuroprotective effect by blocking a novel target that involves mitochondrial pores,[7] which are believed to play a role in the cell death that is associated with neurodegenerative diseases and the aging process.[8] Research is continuing in both Russia and western nations into the potential applications of Dimebon as a neuroprotective and potential nootropic. [9]
[edit] References
- ^ Matveeva IA. Action of dimebon on histamine receptors. Farmakologiia i Toksikologiia. 1983 Jul-Aug;46(4):27-9. (Russian)
- ^ Lermontova NN, Lukoyanov NV, Serkova TP, Lukoyanova EA, Bachurin SO. Dimebon improves learning in animals with experimental Alzheimer's disease. Bulletin of Experimental Biology and Medicine. 2000 Jun;129(6):544-6.
- ^ Antihistamine Shows Promise in Treating Alzheimer’s, NYTimes.com, [[1]]
- ^ Bachurin S, Bukatina E, Lermontova N, Tkachenko S, Afanasiev A, Grigoriev V, Grigorieva I, Ivanov Y, Sablin S, Zefirov N. Antihistamine agent Dimebon as a novel neuroprotector and a cognition enhancer. Annals of the New York Academy of Sciences. 2001 Jun;939:425-35.
- ^ Lermontova NN, Redkozubov AE, Shevtsova EF, Serkova TP, Kireeva EG, Bachurin SO. Dimebon and tacrine inhibit neurotoxic action of beta-amyloid in culture and block L-type Ca(2+) channels. Bulletin of Experimental Biology and Medicine. 2001 Nov;132(5):1079-83.
- ^ Grigorev VV, Dranyi OA, Bachurin SO. Comparative study of action mechanisms of dimebon and memantine on AMPA- and NMDA-subtypes glutamate receptors in rat cerebral neurons. Bull Exp Biol Med. 2003 Nov;136(5):474-7.
- ^ Bachurin SO, Shevtsova EP, Kireeva EG, Oxenkrug GF, Sablin SO. Mitochondria as a target for neurotoxins and neuroprotective agents. Annals of the New York Academy of Sciences. 2003 May;993:334-44
- ^ Medivation's Dimebon(TM) Maintains Statistically Significant Benefit on All Five Efficacy Endpoints in Alzheimer's Disease Trial After One Year of Therapy
- ^ Shevtsova EF, Kireeva EG, Bachurin SO. Mitochondria as the target for neuroprotectors. Vestnik Rossiiskoi Akademii Meditsinskikh Nauk. 2005;(9):13-7. (Russian)
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