Abstract
Metabotropic glutamate receptor 2 (mGluR2) has been implicated in a variety of CNS disorders, including schizophrenia. Disclosed herein is the development of a new series of allosteric potentiators of mGluR2. Structure-activity relationship studies in conjunction with pharmacokinetic data led to the discovery of indole 5, which is active in an animal model for schizophrenia.
MeSH terms
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Acetophenones / chemistry
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Acetophenones / pharmacokinetics
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Acetophenones / pharmacology*
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Allosteric Regulation / drug effects
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Animals
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Brain / drug effects
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Brain / metabolism
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Cross-Linking Reagents / chemistry
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Disease Models, Animal*
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Humans
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Ketamine / pharmacology
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Molecular Structure
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Rats
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Receptors, Metabotropic Glutamate / metabolism*
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Schizophrenia / chemically induced
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Schizophrenia / drug therapy*
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Schizophrenia / metabolism*
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Structure-Activity Relationship
Substances
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Acetophenones
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Cross-Linking Reagents
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Receptors, Metabotropic Glutamate
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metabotropic glutamate receptor 2
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Ketamine