457075-21-7

Biological Activity: Ganstigmine 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 covalently binds to the serine residue at the active site of Torpedo californica AChE, and the nitrogen atom on its moiety forms a key hydrogen bond interaction with the histidine residue (His440) at the active site, inactivating the catalytic triad. 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-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^{[1][2][3][4][5]}.