Chemical Name: 2,3,4,5-Tetrahydro-2,8-dimethyl-5-[2-(6-methyl-3-pyridinyl)ethyl]-1H-pyrido[4,3-b]indole dihydrochloride
Biological ActivityNon-selective antihistamine that displays cognitive enhancing abilities. Also displays high affinity for 5-HT (particularly 5-HT6 and 5-HT7), α-adrenergic, dopaminergic, AMPA and NMDA receptors, and L-type calcium channels. Does not inhibit acetylcholinesterase activity. Exhibits neuroprotective activity in cellular models of Alzheimer's and Huntington's disease and preserves cognitive function following administration to AF64A lesioned rats. Protects neurons against the neurotoxic action of β-amyloid fragment; shown to enhance autophagy in yeast and reduce intracellular Aβ42 levels.
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Latrepirdine (Dimebon) enhances autophagy and reduces intracellular GFP-Aβ42 levels in yeast.
Bharadwaj et al.
J.Alzheimers Dis., 2012;32:949
Antihistamine agent dimebon as a novel neuroprotector and a cognitive enhancer.
Bachurin et al.
Dimebon is a 5-HT6 antagonist with acute cognitive enhancing activities.
Schaffhauser et al.
From anti-allergic to anti-Alzheimer's: molecular pharmacology of dimebon.
Okun et al.
Curr.Alzheimer Res., 2009;7:97
Cognition-enhancing properties of dimebon in a rat novel object recognition task are unlikely to be associated with acetylcholinesterase inhibition or N-MthD.-aspartate receptor antagonism
Giorgetti et al.
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