2001
DOI: 10.1345/aph.1a092
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Galantamine: A New Alzheimer Drug with a Past Life

Abstract: Galantamine is a useful agent for the treatment of Alzheimer disease and for the reversal of neuromuscular blockade. It acts as both an acetylcholinesterase inhibitor and a nicotinic receptor agonist.

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Cited by 33 publications
(13 citation statements)
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“…Given the important role that P-gp plays in protecting the brain from entry of these drugs, the design of such dimeric agents would be useful for blocking the efflux of neurodegenerative disease drugs at the BBB. We chose galantamine, an approved symptomatic therapy for Alzheimer’s disease [23], as a viable compound for dimerization as it has a secondary alcohol that may act as a point of attachment to a crosslinking agent. Although galantamine has not been reported to be a substrate of P-gp, it has a structure that is very similar to the known P-gp substrate morphine [24].…”
Section: Resultsmentioning
confidence: 99%
“…Given the important role that P-gp plays in protecting the brain from entry of these drugs, the design of such dimeric agents would be useful for blocking the efflux of neurodegenerative disease drugs at the BBB. We chose galantamine, an approved symptomatic therapy for Alzheimer’s disease [23], as a viable compound for dimerization as it has a secondary alcohol that may act as a point of attachment to a crosslinking agent. Although galantamine has not been reported to be a substrate of P-gp, it has a structure that is very similar to the known P-gp substrate morphine [24].…”
Section: Resultsmentioning
confidence: 99%
“…These alkaloids may interfere or compete with the action of serotonin in the brain. [37] Ergot alkaloids have marked effects on blood flow, which was originally thought to be the main mechanism of action. Tropane alkaloids like atropine, hyoscyamine and scopolamine from Datura affect the spinal cord and CNS.…”
Section: Alkaloidsmentioning
confidence: 99%
“…Galantamine (3) is licensed in Europe for AD treatment and was well tolerated and significantly improved cognitive function when administered to AD patients, in multi-centre randomized controlled trials (Wilcock et al, 2000;Wilkinson and Murray, 2001). Galantamine (3) is also reported to stimulate nicotinic receptors (Pearson, 2001;Woodruff-Pak et al, 2001), which may also enhance cholinergic function and memory. This additional activity suggests that galantamine (3) may have therapeutic advantages over other AChE inhibitors.…”
Section: Inhibitors Of Acetylcholinesterase: Alkaloidsmentioning
confidence: 99%