Abstract
This article describes recent medicinal chemistry progress toward selective potentiators of the metabotropic glutamate receptor 2 (mGluR2). Groups at Lilly and Merck have identified new classes of potentiators that exhibit selectivity for mGluR2 over the seven other subtypes of mGluRs. Structure-activity relationships as well as pharmacokinetic properties and in vivo activity are reviewed.
MeSH terms
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Allosteric Regulation
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Animals
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Drug Design
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Excitatory Amino Acid Agonists / pharmacokinetics*
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Excitatory Amino Acid Agonists / pharmacology*
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Humans
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Receptors, Metabotropic Glutamate / agonists*
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Receptors, Metabotropic Glutamate / metabolism
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Structure-Activity Relationship
Substances
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Excitatory Amino Acid Agonists
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Receptors, Metabotropic Glutamate
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metabotropic glutamate receptor 2