Current Medicinal Chemistry - Central Nervous System Agents

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New Trends in the Development of Positive Allosteric Modulators of AMPA Receptors

Author(s): E. Graindorge, P. Francotte, S. Boverie, P. de Tullio, B. Pirotte.

Abstract:

The 2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propanoic acid (AMPA) receptors, a subtype of glutamate receptors, are involved in important neuronal functions such as long-term memory. A decrease of the number and activity of these receptors seems to play a role in schizophrenia and in the impairment of cognitive function associated to Alzheimers disease. Therefore, research has been focused on the development of drugs acting on those receptors, in particular of AMPA receptors positive allosteric modulators. Although agonists have an intrinsic activity, allosteric modulators need the release of glutamate to be active. Therefore, these drugs are expected to exhibit a decreasing risk of toxicity compared to pure agonists. In this article, we review the recent advances in the design of positive allosteric modulators of AMPA receptors.

Keywords: positive allosteric modulators, ampa receptors, glutamate receptors, long-term memory, ionotropic receptors

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Article Details

VOLUME: 4
ISSUE: 2
Year: 2004
Page: [95 - 103]
Pages: 9
DOI: 10.2174/1568015043357002
Price: $58