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Galantamine is an allosterically potentiating ligand of the human α4/β2 nAChR

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Abstract:

Galantamine (ReminylTM) is a novel drug treatment for mild to moderate Alzheimer's disease (AD). Originally established as a reversible inhibitor of the acetylcholine-degrading enzyme acetylcholinesterase (AChE), galantamine also acts as an allosterically potentiating ligand (APL) on nicotinic acetylcholine receptors (nAChR). Having previously established this second mode of action on nAChRs from murine brain, we demonstrate here the same action of galantamine on the most abundant nAChR in the human brain, the α4/β2 subtype. This nAChR-sensitizing action is not a common property of all, or most, AChE inhibitors, as is shown by the absence of this effect for other therapeutically applied AChE inhibitors including tacrine, metrifonate, rivastigmine and donepezil. The possible benefits for therapy of AD of an APL action on nicotinic receptors is discussed.

Keywords: AChE inhibitor; APL; Alzheimer; ReminylTM; galantamine; human nAChR; α4/β2 nAChR

Document Type: Original Article

Affiliations: 1: Laboratory of Molecular Neurobiology, Institute of Physiological Chemistry and Pathobiochemistry, Johannes-Gutenberg University Medical School, D-55,099 Mainz/Germany, 2: Department of Advanced Bio-Technologies, Janssen Research Foundation, B-2340 Beerse/Belgium, 3: Department of Pharmacology and Experimental Therapeutics, University of Maryland School of Medicine, Baltimore, MD 21,201, USA

Publication date: December 1, 2000

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