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Dimebolin is an orally-available antihistamine drug with a long history of clinical use in Russia [1][2][3][4].

Dimebolin has been proposed to be useful for treating neurodegenerative disorders, including Alzheimer's disease (AD) and Huntington's disease (HD). Dimebon might exhibit efficacy by blocking NMDA receptors or voltage-gated Ca2+ channels and by preventing mitochondrial permeability pore transition [3].

Dimebolin is an orally-available antihistamine drug. Dimebon improved survival of cerebellar granule cells during long-term incubation with Aβ25-35. Dimebolin also blocked potential-dependent Ca(2+) entry into neurons by about 20% by blocking L-type Ca(2+) channels [4]. In the cerebellum cell culture, Dimebolin protected neurons against the neurotoxic action of Aβ25-35 with EC50 value of 25 μM. On isolated rat ileum intestine, Dimebolin displayed Ca2+-blocking properties with IC50 value of 57 μM. Dimebon also exhibited anticholinesterase activity with IC50 values of 7.9 μM and 42 μM for butyryl-choline esterase and acetylcholine esterase, respectively [5].

In rats treated with the neurotoxin AF64A, Dimebolin exhibited cognition and memory-enhancing properties. In mice, Dimebolin prevented NMDA-induced seizures with EC50 value of 42 ± 6 mg/kg [5].

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