Nootropic Drugs Positively Modulate α-Amino-3-Hydroxy-5-Methyl-4-Isoxazolepropionic Acid-Sensitive Glutamate Receptors in Neuronal Cultures
Article first published online: 5 OCT 2006
Journal of Neurochemistry
Volume 58, Issue 4, pages 1199–1204, April 1992
How to Cite
Copani, A., Genazzani, A. A., Aleppo, G., Casabona, G., Canonico, P. L., Scapagnini, U. and Nicoletti, F. (1992), Nootropic Drugs Positively Modulate α-Amino-3-Hydroxy-5-Methyl-4-Isoxazolepropionic Acid-Sensitive Glutamate Receptors in Neuronal Cultures. Journal of Neurochemistry, 58: 1199–1204. doi: 10.1111/j.1471-4159.1992.tb11329.x
- Issue published online: 5 OCT 2006
- Article first published online: 5 OCT 2006
- Received March 5, 1991; revised manuscript received June 23, 1991; accepted July 31, 1991.
- Nootropic drugs;
- α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid;
- 45Ca2+ influx;
- α-[3H]amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid binding
Abstract: Micromolar concentrations of piracetam, aniracetam, and oxiracetam enhanced α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)-stimulated 45Ca2+ influx in primary cultures of cerebellar granule cells. Nootropic drugs increased the efficacy but not the potency of AMPA and their action persisted in the presence of the voltage-sensitive calcium channel blocker nifedipine. Potentiation by oxiracetam was specific for AMPA receptor-mediated signal transduction, as the drug changed neither the stimulation of 45Ca2+ influx by kainate or N-methyl-d-aspartate nor the activation of inositol phospholipid hydrolysis elicited by quisqualate or (±)-1-aminocyclopentane-trans-1,3-dicarboxylic acid. Piracetam, aniracetam, and oxiracetam increased the maximal density of the specific binding sites for [3H]AMPA in synaptic membranes from rat cerebral cortex. Taken collectively, these results support the view that nootropic drugs act as positive modulators of AMPA-sensitive glutamate receptors in neurons.