New probes of the agonist binding site of metabotropic glutamate receptors.
The (2S,4R)- and (2S,4S)-4-hydroxyglutamates activate cloned mGlu(1a), mGlu(2), and mGlu(8a) receptors with different potencies. Best results were obtained with the (2S,4S) isomer being almost as potent as glutamate on mGlu(1a)R and mGlu(8a)R. Data are interpreted on the basis of the binding site model and X-ray structure.
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Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques, UMR8601-CNRS, Université René Descartes, 45 rue des Saints-Pères, 75270 Paris Cedex 06, France.
Bolte
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Pin
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JP
Acher
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D000818:Animals; D001665:Binding Sites; D002460:Cell Line; D004305:Dose-Response Relationship, Drug; D018690:Excitatory Amino Acid Agonists / Q000494:pharmacology*; D005971:Glutamates / Q000494:pharmacology; D006801:Humans; D008958:Models, Molecular; D015335:Molecular Probes; D011485:Protein Binding; D020033:Protein Isoforms / Q000737:chemistry / Q000378:metabolism; D051381:Rats; D018094:Receptors, Metabotropic Glutamate / Q000737:chemistry* / Q000378:metabolism*; D013237:Stereoisomerism; D014162:Transfection
D018690:Excitatory Amino Acid Agonists; D005971:Glutamates; D015335:Molecular Probes; D020033:Protein Isoforms; D018094:Receptors, Metabotropic Glutamate; C108822:metabotropic glutamate receptor 2; C111435:metabotropic glutamate receptor 8; C104077:metabotropic glutamate receptor type 1; C011859:hydroxyglutamic acid