Metabotropic glutamate receptors: From the workbench to the bedside
Section snippets
Historical background
The evidence that quisqualate and glutamate stimulated inositol phosphate formation in cultured striatal neurons (Sladeczek et al., 1985) offered the first demonstration that excitatory amino acids could activate receptors other than the classical ligand-gated ion channels (named NMDA, “quisqualate” and kainate receptors at that time). In the meantime, ibotenic acid, a heterocyclic amino acid naturally occurring in the mushrooms Amanita muscaria and Amanita pantherina, was found to stimulate
Structure and activation mechanism of mGluRs
Sequence analysis of most class CG-protein coupled receptors (GPCRs), including the 8 mGlu receptor subtypes, the Ca2+-sensing receptor, the taste T1R receptors, and the basic amino acid receptor GPCR6a, revealed that these receptors have a large extracellular domain made of a Venus Fly Trap (VFT) domain similar to the periplasmic bacterial leucine/isoleucine/valine binding protein (LIVBP) linked to the first TM domain via a cysteine-rich domain (CRD) containing 9 highly conserved cysteine
mGlu1 receptor
Gene name: GRM1 (human); Grm1 (rat, mouse). Accession numbers: NP_000829 (human); NP_058707 (rat); NP_058672 (mouse). Chromosomal location: 6q24 (human); 1p13 (rat); 10A2 (mouse) (Masu et al., 1991, Kuramoto et al., 1994, Desai et al., 1995, Stephan et al., 1996).
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