4.5 Article

1-(2-aminoethyl)-3-(arylsulfonyl)-1H-indoles as novel 5-HT6 receptor ligands

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 14, Issue 22, Pages 5499-5502

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2004.09.003

Keywords

serotonin 5-HT6 indoles GPCR

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Novel 1-(2-aminoethyl)-3-(arylsulfonyl)-1H-indoles were prepared. Binding assays indicated they are 5-HT6 receptor ligands, among which N,N-dimethyl-N-{2-[3-(1-naphthylsulfonyl)-1H-indol-1-yl]ethyl}amine 8t and N-methyl-N-{2-[3-(1-naphthylsulfonyl)-1H-indol-1-yl]ethyl}amine 8u showed high affinity for 5-HT6 receptors with K-i = 3.7 and 5.7nM, respectively. (C) 2004 Elsevier Ltd. All rights reserved.

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