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Synthesis and characterization of 8-ethynyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: new potent non-competitive metabotropic glutamate receptor 2/3 antagonists. Part 1 |
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| Authors: | Woltering Thomas J Adam Geo Alanine Alexander Wichmann Jürgen Knoflach Frédéric Mutel Vincent Gatti Silvia |
| Institution: | aF. Hoffmann-La Roche Ltd, Pharma Discovery Chemistry, CNS CH-4070 Basel, Switzerland bF. Hoffmann-La Roche Ltd, Pharma Research, CNS CH-4070 Basel, Switzerland |
| Abstract: | A series of 1,3-dihydrobenzob]1,4]diazepin-2-one derivatives was evaluated as non-competitive mGluR2/3 antagonists. Attachment of an 8-(2-aryl)-ethynyl-moiety produced compounds inhibiting the binding of 3H]-LY354740 to rat mGluR2 with low nanomolar affinity and consistent functional effect at both mGluR2 and mGluR3. |
| Keywords: | Metabotrophic glutamate receptors mGluR2 LY354740 1 3-Dihydro-benzo[b][1 4]diazepin-2-one mGluR2/3 antagonists Non-competitive antagonists |
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