Synthesis and pharmacological characterisation of 2, 4-dicarboxy-pyrroles as selective non-competitive mGluR1 antagonists

F Micheli, R Di Fabio, P Cavanni, JM Rimland…

Index: Micheli, Fabrizio; Fabio, Romano Di; Cavanni, Paolo; Rimland, Joseph M; Capelli, Anna Maria; Chiamulera, Cristiano; Corsi, Mauro; Corti, Corrado; Donati, Daniele; Feriani, Aldo; Ferraguti, Francesco; Maffeis, Micaela; Missio, Andrea; Ratti, Emiliangelo; Paio, Alfredo; Pachera, Roberta; Quartaroli, Mauro; Reggiani, Angelo; Sabbatini, Fabio Maria; Trist, David G; Ugolini, Annarosa; Vitulli, Giovanni Bioorganic and medicinal chemistry, 2003 , vol. 11, # 2 p. 171 - 183

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Citation Number: 37

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) ...