CHF2819

Ganstigmine (CHF 2819 free base) is a potent, orally active, blood-brain barrier-permeable acetylcholinesterase (AChE) inhibitor, with an IC₅₀ value of 65 nM against human AChE, 310 nM against human butyrylcholinesterase (BChE), and 5.12 μM against Torpedo californica AChE. Ganstigmine increases extracellular acetylcholine levels in the brain of rodents without altering the concentrations of other neurotransmitters, stimulates cholinergic transmission, and induces the release of soluble non-amyloidogenic amyloid precursor protein. Ganstigmine exhibits neuroprotective activity independent of cholinesterase inhibition, prevents neuronal death, alleviates β-amyloid-induced neurodegeneration, rescues cholinergic neuron loss, and reverses Scopolamine (HY-N0296)-induced amnesia and memory deficits. Ganstigmine shows cholinesterase inhibition-independent neuroprotective effects against growth factor deprivation and Aβ_25-35 toxicity. Ganstigmine can be used in research on Alzheimer's disease, cholinergic dysfunction, and neuroprotection .

Demethyl-Ganstigmine hydrochloride (Demethyl-CHF 2819) is an orally active AChE inhibitor. Demethyl-Ganstigmine hydrochloride promotes the release of sAPPα from neuroblastoma cells. Demethyl-Ganstigmine hydrochloride increases the concentration of acetylcholine in the prefrontal cortex of rats. Demethyl-Ganstigmine hydrochloride is used in research on neurological diseases such as Alzheimer's disease .