Abstract

Excitatory amino acids such as L-glutamate are the major excitatory neurotransmitters within the mammalian central nervous system. With advances in drug development and molecular neurobiology, the pharmacology of the individual glutamate receptors and their subunits is now being more fully delineated. Described here are the characteristics of heteromeric N-methyl-D-aspartate receptors, including the actions of various selective drugs. Agents such as cyclothiazide, GYKI 52466 and novel competitive antagonists have resulted in a better understanding of the pharmacology of the α-amino-3-hydroxy-5-methylisoxazole-4-propionate subtype of glutamate receptor. Metabotropic glutamate receptors are directly coupled to second messenger systems and their pharmacological characteristics and an analysis of their link to phospholipase C are reported. Pharmacotherapy using drugs directed at glutamatergic transmission is now a very real possibility.

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