4-(3,4-dihydro-1H-isoquinolin-2yl)-pyridines and 4-(3,4-dihydro-1H-isoquinolin-2-yl)-quinolines as potent 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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| Institution: | Pharma Division, Discovery Chemistry, F. Hoffmann-La Roche Ltd., CH-4070 Basel, Switzerland. bernd.buttelmann@roche.com |
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| Abstract: | A series of 4-(3,4-dihydro-1H-isoquinolin-2yl)-pyridines and analogous quinolines was prepared and evaluated as NR1/2B subtype selective NMDA receptor antagonists. 2-Hydroxyalkylamino substitution combines high affinity with selectivity (vs alpha1 and M1 receptors) and activity in vivo. |
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