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AMPA Antagonists: From bench to bedside.

Mattes, Henri, Carcache, David, Kalkman, Hans O. and Koller, Manuel (2010) AMPA Antagonists: From bench to bedside. Journal of Medicinal Chemistry.


AMPA receptors mediate most of the excitatory neurotransmission in the mammalian central nervous system. They also play a key role in synaptic plasticity in the CNS and in memory processes. They may thereby have utility in a number of CNS disorders. In recent years several classes of AMPA receptor antagonists, both competitive and non-competitive, have been reported in the literature. Compounds that present a number of advantages in terms of potency, selectivity and pharmacokinetic properties are currently undergoing clinical evaluation. First successful clinical results in the treatment of epilepsy, the treatment of migraine, as analgesics as well as for the treatment of hyperalgesia and allodynia, have been reported. In the near future, the most important applications for the AMPA receptor antagonists will probably be as neuroprotectant in various neurodegenerative diseases. The present perspective covers recent history of competitive and non-competitive AMPA receptor antagonists design, clinical results obtained with these compounds and emerging therapeutic opportunities.

Item Type: Article
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Additional Information: archiving not formally supported by this publisher
Keywords: Glutamate , AMPA, antagonist, ionotropic, receptors, schizophrenia, epilepsy, cytoprotection, pain, migraine, neuroprotection
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Date Deposited: 13 Oct 2015 13:17
Last Modified: 13 Oct 2015 13:17


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