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., et al.. - 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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