New probes of the agonist binding site of metabotropic glutamate receptors

A S Bessis; J Bolte; J P Pin; F Acher

doi:10.1016/s0960-894x(01)00158-5

New probes of the agonist binding site of metabotropic glutamate receptors

Bioorg Med Chem Lett. 2001 Jun 18;11(12):1569-72. doi: 10.1016/s0960-894x(01)00158-5.

Authors

A S Bessis¹, J Bolte, J P Pin, F Acher

Affiliation

¹ Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques, UMR8601-CNRS, Université René Descartes, 45 rue des Saints-Pères, 75270 Paris Cedex 06, France.

PMID: 11412983
DOI: 10.1016/s0960-894x(01)00158-5

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Binding Sites
Cell Line
Dose-Response Relationship, Drug
Excitatory Amino Acid Agonists / pharmacology*
Glutamates / pharmacology
Humans
Models, Molecular
Molecular Probes
Protein Binding
Protein Isoforms / chemistry
Protein Isoforms / metabolism
Rats
Receptors, Metabotropic Glutamate / chemistry*
Receptors, Metabotropic Glutamate / metabolism*
Stereoisomerism
Transfection

Substances

Excitatory Amino Acid Agonists
Glutamates
Molecular Probes
Protein Isoforms
Receptors, Metabotropic Glutamate
metabotropic glutamate receptor 2
metabotropic glutamate receptor 8
metabotropic glutamate receptor type 1
hydroxyglutamic acid