Abstract
Glycine transporter 1 (GlyT1) represents a novel target for the treatment of schizophrenia via the potentiation of glutamatergic NMDA receptors. The discovery of 4,4-disubstituted piperidine inhibitors of GlyT1 which exhibit improved pharmacokinetic properties, including oral bioavailability, is discussed.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Dogs
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Drug Discovery / methods*
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Glycine / biosynthesis
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Glycine Plasma Membrane Transport Proteins / antagonists & inhibitors*
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Glycine Plasma Membrane Transport Proteins / metabolism
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Humans
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Mice
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Mice, Inbred DBA
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N-Methylaspartate / chemistry
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N-Methylaspartate / pharmacology
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Piperidines / administration & dosage
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Piperidines / chemical synthesis*
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Piperidines / pharmacokinetics*
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Rats
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Substrate Specificity
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Sulfonamides / chemical synthesis
Substances
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Glycine Plasma Membrane Transport Proteins
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Piperidines
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Sulfonamides
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N-Methylaspartate
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Glycine