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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Isoxazole Ionotropic Glutamate Neurotransmitters

Author(s): David J. Burkhart and N. R. Natale

Volume 12 , Issue 5 , 2005

Page: [617 - 627] Pages: 11

DOI: 10.2174/0929867310504050617

Price: $65


Analogs of the excitatory neurotransmitter glutamate are potential medicinal agents for a wide variety of neurological disorders. The isoxazole glutamate derivatives represent an important class of compounds because of their receptor specificity and binding affinity. Since the discovery of (S)-2-amino-3-(3- hydroxy-5-methyl-4-isoxazolyl) propionic acid (AMPA) in 1980, numerous analogs built around the isoxazole scaffold have shown remarkable selectivity for specific ionotropic glutamate receptors, but strong side effects in human clinical trials have shown the need for improvement. Trends revealed by structure activity relationship and crystallographic studies indicate the role of stereochemistry may be important in uncovering the prerequisite selectivity, which would give rise to effective therapeutics for neurological dysfunction of the glutamate receptor.

Keywords: central nervous system, heterogeneous ionotropic glutamate receptors, ampa, kainic acid, transmembrane domains

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