期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 14, 页码 3844-3847出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.06.064
关键词
5-HT2C receptor antagonists; GPCR; depression; anxiety
A novel series of 1H-indole-3-carboxylic acid pyridine-3-ylamides were synthesized and identified to show high affinity and selectivity for 5-HT2C receptor. Among them, 1H-indole-3-carboxylic acid[6-(2chloro-pyridin-3-yloxy)-pyridin-3-yl]-amide (15k) exhibits the highest affinity (IC50 = 0.5 nM) with an excellent selectivity (>2000 times) over other serotonin (5-HT1A, 5-HT2A, and 5-HT6) and dopamine (D-2-D-4) receptors. (C) 2008 Elsevier Ltd. All rights reserved.
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