Dimebon is an activator of AMPK, a potentiator of AMPA, and an inhibitor of L-type voltage-gated Ca2+ channels, NMDA receptors, H1/2 histamine receptors, α-adrenergic receptors, and 5-HT2C/5A/6 receptors. Dimebon displays neuroprotective and cognition enhancing effects in neurodegenerative diseases. Dimebon decreases neuronal excitability and glutamate release. In animal models of autotrophic lateral sclerosis (ALS), dimebon delays the onset of symptoms and increases the lifespan. In animal models of Alzheimer’s disease, this compound regulates APP metabolism, decreasing levels of amyloid-β (Aβ). In other animal models, dimebon prevents Aβ-induced mitochondrial swelling in the brain. Dimebon also exhibits beneficial effects in animal models of Parkinson’s disease.