Nicotinic cholinergic modulation: galantamine as a prototype.

Full Abstract

Nicotinic acetylcholine receptor pharmacology is becoming increasingly important in the clinical symptomatology of neurodegenerative diseases in general and of cognitive and behavioral aspects in particular. In addition, the concept of allosteric modulation of nicotinic acetylcholine receptors has become a research focus for the development of therapeutic agents. In this review the scientific evidence for changes in nicotinic acetylcholine receptors in Alzheimer's disease is described. Within this context, the pharmacology of galantamine, a recently approved drug for cognition enhancement in Alzheimer's disease, is reviewed along with preclinical studies of its efficacy on learning and memory. Galantamine modestly inhibits acetylcholinesterase and has an allosteric potentiating ligand effect at nicotinic receptors. The data collected in this review suggest that the unique combination of acetylcholinesterase inhibition and nicotinic acetylcholine receptor modulation offers potentially significant benefits over acetylcholinesterase inhibition alone in facilitating acetylcholine neurotransmission.

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Author information

Author/s: Woodruff-Pak, Diana S (DS); Lander, Cynthia (C); Geerts, Hugo (H);

Affiliation: Albert Einstein Healthcare Network, Korman Suite 100, 5501 Old York Road, Philadelphia, PA 19141, USA. woodrufd(-atsign-)einstein.edu.

Journal and publication information

Publication Type: Journal Article; Review

Journal: CNS drug reviews (CNS Drug Rev), published in United States. (Language: eng)

Reference: 2002-; vol 8 (issue 4) : pp 405-26

Dates: Created 2002/12/13; Completed 2003/03/25; Revised 2005/11/16;

PMID: 12481195, status: MEDLINE (last retrieval date: 11/6/2008)

Sourced from the National Library of Medicine. Abstract text and other information may be subject to copyright.

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MeSH headings (categories)

This article was linked to the MESH Headings shown below.

Acetylcholine - metabolism
Allosteric Regulation
Alzheimer Disease - drug therapy; metabolism
Animals
Cholinesterase Inhibitors - pharmacology; therapeutic use
Galantamine - pharmacology; therapeutic use
Humans

Learning - drug effects
Ligands
Memory - drug effects
Models, Animal
Models, Biological
Receptors, Nicotinic - drug effects; metabolism
Synaptic Transmission - drug effects

Associated Chemicals: Cholinesterase Inhibitors (0) ; Ligands (0) ; Receptors, Nicotinic (0) ; Galantamine (357-70-0) ; Acetylcholine (51-84-3)

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