Glutamate receptors ionotropic, agonists

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). 

There are three types of ionotropic glutamate receptors NMDA, a-amino-3-hydroxy-5-methyl-4-isoxazoleproprionic acid (AMPA), and kainate receptors (Fig. 1). Each is principally activated by the agonist bearing its name and is permeable to cationic flux hence, their activation results in membrane depolarization. Ionotropic glutamate receptors were originally classified based on three selective, synthetic agonists quisqualate, kainate and NMDA. After the discovery of metabotropic receptors, it became clear that quisqualate also interacts with them. Since that time, quisqualate-sensitive ionotropic receptors have been classified by the more selective agonist AMPA. 

The amino acid L-glutamate is the main excitatory neurotransmitter of the central nervous system (Fonnum, 1984). Glutamate exerts its excitatory effects either by activation of several G-protein-coupled metabotropic glutamate receptors or by induction of ion fluxes by different classes of ionotropic receptors. The NMDA receptor is one of those glutamate-gated ion channels which got its name from its selective artificial agonist NMDA (N-methyl-D-aspartate) and which controls slow but persistent ion fluxes of Na+, K+, and Ca2+ across the cell membrane. 

Figure 30-24 Chemical structures of some agonists of ionotropic glutamate receptors (iGluR).

Glutamate ionotropic receptors - agonists Important agents include the plant agents ibotenic acid, acromelic acid and BMAA (P-W-oxalylamino-L-alanine), and also domoicacid (amnesic shellfish poison). See GLUTAMATE RECEPTOR AGONISTS. 

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