New probes of the agonist binding site of metabotropic glutamate receptors

The (2S,4R)- and (2S,4S)-4-hydroxyglutamates activate cloned mGlu1a, mGlu2, and mGlu8a receptors with different potencies. Best results were obtained with the (2S,4S) isomer being almost as potent as glutamate on mGlu1aR and mGlu8aR. Data are interpreted on the basis of the binding site model and X-ray structure