Galantamine is an
allosterically potentiating ligand
of the human alpha4/beta2 nAChR.
Samochocki M, Zerlin M, Jostock R, Groot Kormelink PJ,
Luyten WH, Albuquerque EX, Maelicke A.
Laboratory of Molecular Neurobiology,
Institute of
Physiological Chemistry and Pathobiochemistry, Johannes-Gutenberg University
Medical School, Mainz/Germany.
Acta Neurol Scand Suppl 2000;176:68-73
Abstract
-
Galantamine (Reminyl) 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 alpha4/beta2 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
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