Agonists and antagonists for group III metabotropic glutamate receptors 6, 7 and 8.
Metabotropic glutamate receptors (mGluRs) have been implicated in a variety of neurological and psychiatric disorders. This article describes recent progress in the development of agonists and antagonists for mGluR 6, 7, and 8. All of them are conformationally constrained or substituted amino acids, and they act at N-terminal extracellular glutamate binding site. These ligands serve as valuable tools for studying physiological and pathological roles of mGluRs. However, their therapeutic potential may be restricted by their poor CNS penetration and lack of selectivity for individual receptors.
Yang
Zhi-Qiang
ZQ
Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., PO Box 4, West Point, PA 19486 USA. zhiqiang-yang@merck.com
D000818:Animals; D015195:Drug Design; D018690:Excitatory Amino Acid Agonists / Q000494:pharmacology; D018691:Excitatory Amino Acid Antagonists / Q000494:pharmacology; D006801:Humans; D018094:Receptors, Metabotropic Glutamate / Q000819:agonists* / Q000037:antagonists & inhibitors*
D018690:Excitatory Amino Acid Agonists; D018691:Excitatory Amino Acid Antagonists; D018094:Receptors, Metabotropic Glutamate; C113897:metabotropic glutamate receptor 6; C102719:metabotropic glutamate receptor 7; C111435:metabotropic glutamate receptor 8