Abstract
The synthesis of NPTS, 6, a potent inhibitor of the type 1 glycine transporter (GlyT1) is described, as well as preparation of 6 in optically active and tritiated form for use as a radioligand for affinity displacement assay of GlyT1.
MeSH terms
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Amino Acid Transport Systems, Neutral / antagonists & inhibitors*
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Animals
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Binding, Competitive / drug effects
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Glycine Plasma Membrane Transport Proteins
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Hippocampus / drug effects
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Hippocampus / metabolism
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Humans
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In Vitro Techniques
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Kinetics
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Radiopharmaceuticals / chemical synthesis*
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Radiopharmaceuticals / pharmacology*
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Rats
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Sarcosine / analogs & derivatives
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Sarcosine / chemical synthesis*
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Sarcosine / pharmacology*
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Stereoisomerism
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Synaptic Transmission / drug effects
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Synaptosomes / drug effects
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Synaptosomes / metabolism
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Tumor Cells, Cultured
Substances
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(R)-N(3-phenyl-3-(4'-(4-toluoyl)phenoxy)-propyl)sarcosine
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Amino Acid Transport Systems, Neutral
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Glycine Plasma Membrane Transport Proteins
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Radiopharmaceuticals
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SLC6A9 protein, human
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Slc6a9 protein, rat
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Sarcosine