Abstract
We identified 4-fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide 27 as a potent mGluR1 antagonist. The compound possessed excellent subtype selectivity and good PK profile in rats. It also demonstrated relatively potent antipsychotic-like effects in several animal models. Suitable for development as a PET tracer, compound 27 would have great potential for elucidation of mGluR1 functions in human.
MeSH terms
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Animals
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Antipsychotic Agents / chemistry
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Antipsychotic Agents / pharmacokinetics*
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Antipsychotic Agents / pharmacology*
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Antipsychotic Agents / therapeutic use
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Benzamides / chemistry
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Benzamides / pharmacokinetics*
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Benzamides / pharmacology*
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Benzamides / therapeutic use
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Humans
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Mice
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Rats
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Receptors, Metabotropic Glutamate / antagonists & inhibitors*
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Receptors, Metabotropic Glutamate / metabolism*
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Structure-Activity Relationship
Substances
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Antipsychotic Agents
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Benzamides
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Receptors, Metabotropic Glutamate
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metabotropic glutamate receptor type 1
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N-methylbenzamide