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Neurobiology of Amino Acids, Peptides and Trophic Factors pp 63–77Cite as

Pharmacology of Excitatory Amino Acid Antagonists and their Possible Therapeutic Use in Neurological Disease

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Part of the book series: Topics in the Neurosciences ((TINS,volume 8))

Abstract

Excitatory amino acid antagonists arc of two main types: 1) structural analogues of dicarboxylic amino acids that compete with glutamate or other agonists at the receptor site and 2) lipophilic compounds, without acidic groups, that block the excitatory action of agonists by a noncompetitive mechanism. The postsynaptic receptors at which amino acids exert an excitatory action can be classified according to their preferred agonists as kainate-, quisqualate-, and N-methyl-D-aspartate-preferring receptors [1, 2]. Referring to these receptor subtypes as kainate, quisqualate, and NMDA receptors is a convenient shorthand; it implies nothing about the nature of the endogenous neurotransmitters. Glutamate is a highly effective agonist at all three receptor subtypes. Aspartate acts preferentially on the NMDA receptor in spinal cord neurons [3]. The sulphur-containing analogues of glutamate and aspartate interact with quisqualate and NMDA receptors but not with kainate receptors [4].

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Meldrum, B.S. (1988). Pharmacology of Excitatory Amino Acid Antagonists and their Possible Therapeutic Use in Neurological Disease. In: Ferrendelli, J.A., Collins, R.C., Johnson, E.M. (eds) Neurobiology of Amino Acids, Peptides and Trophic Factors. Topics in the Neurosciences, vol 8. Springer, Boston, MA. https://doi.org/10.1007/978-1-4613-1721-0_5

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