4-(2-Aminoethoxy)-N-(phenylsulfonyl)indoles as novel 5-HT6 receptor ligands |
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| Authors: | Zhou Ping Yan Yinfa Bernotas Ronald Harrison Boyd L Huryn Donna Robichaud Albert J Zhang Guo Ming Smith Deborah L Schechter Lee E |
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| Institution: | Chemical and Screening Science and Neuroscience Discovery Research, Wyeth Research, CN 8000, Princeton, NJ 08543-8000, USA. zhoup@wyeth.com |
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| Abstract: | The preparation of a novel class of 4-(2-aminoethoxy)-N-(phenylsulfonyl)indoles which exhibit high affinity towards the 5-HT6 receptor is reported here. Among these compounds, 4-(2-methylaminoethoxy)-N-(phenylsulfonyl)indole 5g showed superior affinity (Ki = 1 nM) towards the 5-HT6 receptor as well as excellent selectivity (> 2000-fold) against the closely related subtype 5-HT7 receptor. |
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