2. Academic Validation
  3. New probes of the agonist binding site of metabotropic glutamate receptors

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.
A S Bessis 1,  J Bolte,  J P Pin,  F Acher
Affiliations

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.

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