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XB-ART-6071
Bioorg Med Chem 2003 Jan 17;112:171-83. doi: 10.1016/s0968-0896(02)00424-8.
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Synthesis and pharmacological characterisation of 2,4-dicarboxy-pyrroles as selective non-competitive mGluR1 antagonists.

Micheli F , Fabio RD , Cavanni P , Rimland JM , Capelli AM , Chiamulera C , Corsi M , Corti C , Donati D , Feriani A , Ferraguti F , Maffeis M , Missio A , Ratti E , Paio A , Pachera R , Quartaroli M , Reggiani A , Sabbatini FM , Trist DG , Ugolini A , Vitulli G .


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Metabotropic glutamate receptors (mGluRs) are an unusual family of G-protein coupled receptor (GPCR), and are characterised by a large extracellular N-terminal domain that contains the glutamate binding site. We have identified a new class of non-competitive metabotropic glutamate receptor 1 (mGluR1) antagonists, 2,4-dicarboxy-pyrroles which are endowed with nanomolar potency. They interact within the 7 transmembrane (7TM) domain of the receptor and show antinociceptive properties when tested in a number of different animal models.

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Species referenced: Xenopus laevis
Genes referenced: grm1