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. © 2002 Elsevier Science Ltd. All rights reserved.
Synthesis and pharmacological characterisation of 2,4-dicarboxy-pyrroles as selective non-competitive mGluR1 antagonists / Micheli, F.; Di Fabio, R.; Cavanni, P.; Rimland, J. M.; Capelli, A. M.; 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, F. M.; Trist, D. G.; Ugolini, A.; Vitulli, G.. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - 11:2(2003), pp. 171-183. [10.1016/S0968-0896(02)00424-8]
Synthesis and pharmacological characterisation of 2,4-dicarboxy-pyrroles as selective non-competitive mGluR1 antagonists
Ferraguti F.;
2003
Abstract
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. © 2002 Elsevier Science Ltd. All rights reserved.
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