Dimebolin is an orally-available drug, approved in Russia for use as a non-selective antihistamine, that has shown promise in the treatment of neurodegenerative diseases, including Alzheimer’s 1,2 and Huntington’s disease.3 In addition to reported activity in preventing the onset and progression of disease by being neuroprotective, dimebolin appears to promote clinical improvement by increasing cognitive function.4,2 At the cellular level, dimebolin appears to have diverse effects, inhibiting the neurotoxic action of β-amyloid and blocking L-type calcium channels,5 inhibiting NMDA-type glutamate receptors,6 and preventing mitochondrial leakage.7
1
Lermontova, N.N., Lukoyanov, N.V., Serkova, T.P., et al. Dimebon improves learning in animals with experimental Alzheimer’s disease. Bull Exp Biol Med129(6)640-642(2000).
2
Doody, R.S., Gavrilova, S.I., Sano, M., et al. 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. Lancet372207-215(2008).
3
Wu, J., Li, Q., and Bezprozvanny, I. Evaluation of dimebon in cellular model of Huntington’s disease. Mol Neurodegener3(15)(2008).
4
Bachurin, S., Bukatina, E., Lermontova, N., et al. Antihistamine agent dimebon as a novel neuroprotector and a cognition enhancer. Ann N Y Acad Sci939425-435(2001).
5
Lermontova, N.N., Redkozubov, A.E., Shevtsova, E.F., et al. Dimebon and tacrine inhibit neurotoxic action of β-amyloid in culture and block L-type Ca2+ channels. Bull Exp Biol Med132(5)1079-1083(2001).
6
Grigor'ev, V.V., Dranyi, O.A., and Bachurin, S.O. Comparative study of action mechanisms of dimebon and memantine on AMPA- and NMDA-subtypes glutamate receptors in rat cerebral neurons. Bull Exp Biol Med136(5)474-477(2003).
7
Bachurin, S.O., Shevtsova, E.P., Kireeva, E.G., et al. Mitochondria as a target for neurotoxins and neuroprotective agents. Ann N Y Acad Sci993334-344(2003).
Wu, J., Li, Q., and Bezprozvanny, I. Evaluation of dimebon in cellular model of Huntington’s disease. Mol Neurodegener3(15)(2008).
Bachurin, S., Bukatina, E., Lermontova, N., et al. Antihistamine agent dimebon as a novel neuroprotector and a cognition enhancer. Ann N Y Acad Sci939425-435(2001).
Grigor'ev, V.V., Dranyi, O.A., and Bachurin, S.O. Comparative study of action mechanisms of dimebon and memantine on AMPA- and NMDA-subtypes glutamate receptors in rat cerebral neurons. Bull Exp Biol Med136(5)474-477(2003).
Doody, R.S., Gavrilova, S.I., Sano, M., et al. 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. Lancet372207-215(2008).
Lermontova, N.N., Lukoyanov, N.V., Serkova, T.P., et al. Dimebon improves learning in animals with experimental Alzheimer’s disease. Bull Exp Biol Med129(6)640-642(2000).
Bachurin, S.O., Shevtsova, E.P., Kireeva, E.G., et al. Mitochondria as a target for neurotoxins and neuroprotective agents. Ann N Y Acad Sci993334-344(2003).
Lermontova, N.N., Redkozubov, A.E., Shevtsova, E.F., et al. Dimebon and tacrine inhibit neurotoxic action of β-amyloid in culture and block L-type Ca2+ channels. Bull Exp Biol Med132(5)1079-1083(2001).