Issue: Nicotinic cholinergic receptors exist in multiple forms in the brain and may be important in mediating diverse cognitive functions such as memory and attention.
This is the first of a 2-part series on
nicotinic cholinergic receptors. Here we will discuss how
recent advances in the understanding of nicotinic
cholinergic receptors1,2 have elucidated their
molecular structures. In the second
part, we will present our current understanding of
the psychopharmacologic functions of nicotinic
cholinergic receptors. These developments form the basis
for novel treatment strategies for cognitive
disturbances, particularly those associated with
Alzheimer's disease or schizophrenia, which will be
discussed in a future Brainstorms. Organization of the Nicotinic ReceptorNicotinic receptors belong to the superfamily of receptors called ligand-gated ion channels. One of the best known members of this family is the gamma-aminobutyric acid (GABA)-benzodiazepine-chloride channel complex. These types of receptors are composed of 5 subunits that together create a central ion channel (Figure 1), which allows for the passage of calcium into the cell (Figure 2). |
SummaryThe structure of nicotinic receptors has been elucidated. How these structures lead to specific functions will be discussed in part 2.
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References1. Halladay MW, Dart MJ, Lynch JK. Neuronal nicotinic acetylcholine receptors as targets for drug discovery. J Med Chem 1997;40:4169-4194 |
2. Picciotto MR, Caldarone BJ, King SL,
et al. Nicotinic receptors in the brain: links between
molecular biology and behavior. Neuropsychopharmacology
2000;22:451-465 3. Maelicke A, Albuquerque EX. New approach to drug therapy in Alzheimer's dementia. Drug Discovery Today 1996;2:53-59 |
4. Albuquerque EX, Alkondon M, Pereira EFR, et al. Properties of neuronal nicotinic acetylcholine receptors: pharmacological characterization and modulation of synaptic function, J Pharmacol Exp Ther 1997;280:1117-1136 |
