Abstract
We report herein the synthesis of the tritium labeled isotopomer of 1 and its use as a radioligand to label mGlu8 receptors in rat forebrain membranes as well as cloned human recombinant mGlu receptors. [(3)H]-1 was synthesized by the NaBT(4) reduction of an activated analog of 5. [(3)H]-1 bound appreciably to recombinant human mGlu2, mGlu3 and mGlu8 receptors and to rat forebrain membranes and was displaced by L-glutamate and L-(+)-2 amino-4-phosphonobutyric acid. The results indicate that [(3)H]-1 should be a useful ligand for the study of mGluR2, 3, and 8 receptors in cloned cell lines and possibly brain tissue.
MeSH terms
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Aminobutyrates / pharmacology
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Animals
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Brain / drug effects*
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Brain / metabolism
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Cell Line
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Cell Membrane / metabolism
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Cyclopropanes / chemistry*
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Cyclopropanes / pharmacology
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Glutamic Acid / pharmacology
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Glycine / analogs & derivatives*
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Glycine / chemistry*
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Glycine / pharmacology
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Humans
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Isotope Labeling / methods*
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Ligands
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Rats
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Receptors, Metabotropic Glutamate / metabolism*
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Tritium*
Substances
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(2S,1'S,2'R,3'R)-2(2'-carboxy-3'-hydroxymethylcyclopropyl)glycine-(3H)
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Aminobutyrates
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Cyclopropanes
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Ligands
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Receptors, Metabotropic Glutamate
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metabotropic glutamate receptor 2
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metabotropic glutamate receptor 3
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Tritium
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Glutamic Acid
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2-amino-4-phosphonobutyric acid
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Glycine