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Member of the Ampakine class of memory enhancers prolongs the single channel open time of reconstituted AMPA receptors
- Source :
- Synapse. 40:154-158
- Publication Year :
- 2001
- Publisher :
- Wiley, 2001.
-
Abstract
- Ampakines are small benzamide compounds that allosterically produce the positive modulation of AMPA receptors and improve performance on a variety of behavioral tasks. To test if the native synaptic membrane is necessary for the effects of such positive modulators, the mechanism of action of the Ampakine 1-(1,3-benzodioxol-5-ylcarbonyl)-1,2,3,6-tetrahydropyridine (CX509) was investigated in isolated rat brain AMPA receptors reconstituted in lipid bilayers. The drug increased the open time of AMPA-induced single channel current fluctuations with an EC50 of 4 μM. The action of CX509 was highly selective since it had no effect on the amplitude or close time of channel events. The open time effect had a maximum enhancement of 70-fold and the modulated currents were blocked by CNQX. It is concluded that the synaptic membrane environment is not necessary for Ampakine effects. In fact, CX509 was about 100 times more potent on the reconstituted AMPA receptors than on receptors in their native membrane. These findings indicate that centrally active Ampakines modulate specific kinetic properties of AMPA currents. They also raise the possibility that AMPA receptors are regulated by factors present in situ, thus explaining the more efficient modulatory effects of CX509 when acting on receptors removed from their synaptic location. Synapse 40:154–158, 2001. © 2001 Wiley-Liss, Inc.
- Subjects :
- Ampakine
Time Factors
Pyridines
medicine.drug_class
Synaptic Membranes
Kainate receptor
Dioxoles
AMPA receptor
Ion Channels
Cellular and Molecular Neuroscience
chemistry.chemical_compound
Piperidines
Memory
Excitatory Amino Acid Agonists
medicine
Animals
Receptors, AMPA
Long-term depression
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid
Nootropic Agents
Ion channel
Neurons
Brain
Pyrrolidinones
Rats
chemistry
Benzamides
Silent synapse
CNQX
Biophysics
Neuroscience
Ion channel linked receptors
Subcellular Fractions
Subjects
Details
- ISSN :
- 10982396 and 08874476
- Volume :
- 40
- Database :
- OpenAIRE
- Journal :
- Synapse
- Accession number :
- edsair.doi.dedup.....1a15a514b9c3eaea24f6996e63ef67fb