Biological Activity
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].
References
[1]. lermontova nn, lukoyanov nv, serkova tp, et al. dimebon improves learning in animals with experimental alzheimer's disease. bull exp biol med. 2000 jun;129(6):544-6.
[2]. doody rs, gavrilova si, 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. lancet. 2008 jul 19;372(9634):207-15.
[3]. wu j, li q, bezprozvanny i. evaluation of dimebon in cellular model of huntington's disease. mol neurodegener. 2008 oct 21;3:15.
[4]. lermontova nn, redkozubov ae, shevtsova ef, et al. dimebon and tacrine inhibit neurotoxic action of beta-amyloid in culture and block l-type ca(2+) channels. bull exp biol med. 2001 nov;132(5):1079-83.
[5]. bachurin s, bukatina e, lermontova n, et al. antihistamine agent dimebon as a novel neuroprotector and a cognition enhancer. ann n y acad sci. 2001 jun;939:425-35.
