2-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines as a novel class of NR1/2B subtype selective NMDA receptor antagonists |
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| Authors: | Büttelmann Bernd Alanine Alexander Bourson Anne Gill Ramanjit Heitz Marie-Paule Mutel Vincent Pinard Emmanuel Trube Gerhard Wyler René |
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| Affiliation: | Pharma Division, Discovery Chemistry, F. Hoffmann-La Roche Ltd., CH-4070 Basel, Switzerland. bernd.buettelmann@roche.com |
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| Abstract: | Recently, we disclosed 4-aminoquinolines as structurally novel NR1/2B subtype selective NMDA receptor antagonists. We would now like to report our findings on structurally related pyridine analogues. The SAR developed in this series resulted in the discovery of high affinity antagonists which are selective (vs alpha1 and M1 receptors) and active in vivo. |
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