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Galantamine


Mechanism of action:

Galantamine is an acetylcholinesterase inhibitor and also a positive allosteric modulator of nicotinic acetylcholine receptors. Galantamine reversibly inhibits acetylcholinesterase, reducing the breakdown of acetylcholine in the synaptic cleft and thereby increasing acetylcholine concentration. This enhances cholinergic activity in the central nervous system, especially in the cerebral cortex and hippocampus. Galantamine also acts as a positive allosteric modulator of α4β2 and α7 nicotinic acetylcholine receptors, enhancing the receptor response to acetylcholine without directly activating the receptors themselves. As a result, it can strengthen cholinergic neurotransmission related to cognitive functions such as memory and attention.

Reference(s):

1. Scott LJ et al. (2000). Galantamine: a review of its use in Alzheimer's disease. Drugs. 


2. Greenblatt HM et al. (1999). Structure of acetylcholinesterase complexed with (-)-galanthamine at 2.3 A resolution. FEBS Lett. 


3. Lilienfeld S et al. (2002). Galantamine—a novel cholinergic drug with a unique dual mode of action for the treatment of patients with Alzheimer's disease. CNS Drug Rev.

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