Glutamate receptor agonists

Glutamate receptor. agonists ( excitotoxins ) glutamate, kainate,... 

L-Glutamate acts as an excitatory neurotransmitter at many synapses in the mammalian central nervous system. Electrophysiological measurements and the use of various selective agonists and antagonists indicate that different glutamate receptors co-exist on many neurons. 

These X-ray structures provide a wealth of information about the interactions of agonists, antagonists, and allosteric modulators with the glutamate receptor subunit... 

Stereostructure-activity studies on agonists at the AMPA and kainate subtypes of ionotropic glutamate receptors. Chirality, 15, 167-179. 

Ionotropic glutamate receptors mediate fast excitatory neurotransmission in practically all areas of the central nervous system (CNS). They are also critical for both the induction and expression of synaptic plasticity, and have been implicated in diverse pathological conditions, such as epilepsy, ischemic brain damage, anxiety, and addiction. There are three subtypes of ionotropic glutamate receptors that are named after their high-affinity agonists as a-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA), N-1nethyl-D-aspartate (NMDA), and kainate (KA) receptors (1). 

Takahashi, K., Tsuchida, K., Tanabe, Y., Masayuki, M., and Nakanishi, S. (1993) Role of the large extracellular domain of metabotropic glutamate receptors in agonist selectivity determination. J. Biol. Chem. 268,19341-19345. 

Tones, M. A., Bendali, N., Flor, P. J., Knopfel, T., and Kuhn, R. (1995) The agonist selectivity of a class III metabotropic glutamate receptor, human mGluR4a, is determined by the N-terminal extracellular domain. NeuroReport 7,117-120. 

Stem-Bach, Y., Bettler, B., Hartley, M., Sheppard, P. O., O Hara, P. J., and Heinemann, S. F. (1994) Agonist selectivity of glutamate receptors is specified by two domains structurally related to bacterial amino acid-binding proteins. Neuron 13,1345-1357. 

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