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Bisnorcymserine is an orally available small molecule inhibitor of butyrylcholinesterase (BChE), developed primarily for the treatment of dementia and investigated in Alzheimer's disease. It acts as a reversible inhibitor of BChE by binding non-covalently to the enzyme's active site. The leaving group, bisnoreseroline, interacts with key residues (Ser200 and His440) within the catalytic triad and stacks with Trp84 at the bottom of the gorge in BChE. This disrupts normal enzymatic activity and may help improve brain function by modulating cholinergic neurotransmission. Bisnorcymserine has also been described as an amyloid beta-protein precursor inhibitor[2][7][9]. The drug was originally developed by researchers at the National Institute on Aging/NIH and later advanced by Annovis Bio.
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