latrepirdine

Latrepirdine is a small molecule, gamma-carboline derivative originally developed and marketed in Russia as an oral antihistamine (H1 receptor antagonist) under the brand name Dimebon since 1983. It was later investigated for neuroprotective properties and potential use in treating neurodegenerative diseases such as Alzheimer's disease and Huntington's disease. Latrepirdine acts through multiple mechanisms, including inhibition of histamine H1 and H2 receptors, antagonism of several serotonin receptors (notably 5-HT2C, 5-HT5A, 5-HT6), inhibition of α1A-, α1B-, α1D-, and α2A-adrenoceptors, modulation of NMDA glutamate receptors, L-type calcium channel blockade, acetylcholinesterase inhibition, butyrylcholinesterase inhibition, mitochondrial permeability transition pore modulation (neuroprotection), and possible effects on dopamine receptors. Despite promising early results in phase II trials for Alzheimer's disease and Huntington's disease suggesting cognitive enhancement or neuroprotection, subsequent phase III trials failed to demonstrate efficacy for these indications. As a result, major development efforts were discontinued[1][2][3][5][6].

Brand names

Dimebon

Other names

dimebolinlatrepirdine