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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