A highly selective agonist for the metabotropic glutamate receptor mGluR2

Simon D. Nielsen, Marica Fulco, Michaela Serpi, Birgitte Nielsen, Maria B. Hansen, Kasper L. Hansen, Christian Thomsen, Robb Brodbeck, Hans Bräuner-Osborne, Roberto Pellicciari, Per Ola Norrby, Jeremy R. Greenwood, Rasmus P. Clausen

Research output: Contribution to journalArticlepeer-review

Abstract

The three conformationally restricted cyclopropyl glutamate analogues (3, 4, 5) were synthesised and their affinity for ionotropic and activity at metabotropic glutamate receptors were probed. Compound 4 turned out to be a highly selective agonist at the metabotropic glutamate receptor mGluR2 with at least two orders of magnitude selectivity in potency compared to the very homologous mGluR3 as well as mGluR1, 4, 5, 7. We also tried to synthesise the two epimers of 6, but the two compounds underwent fast epimerisation in H 2O. Furthermore, two cyclopropyl arginine analogues (7, 8) were synthesised and characterised pharmacologically at GPRC6A.

Original languageEnglish
Pages (from-to)1120-1124
Number of pages5
JournalMedChemComm
Volume2
Issue number11
DOIs
StatePublished - Nov 2011

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