Fluorescent non-imidazole histamine H3 receptor ligands with nanomolar affinities

被引：28

作者：

Amon, M

Ligneau, X

Schwartz, JC

Stark, H ^{[1
]}

机构：

[1] Goethe Univ Frankfurt, Biozentrum, ZAFES, Inst Pharmazeut Chem, D-60431 Frankfurt, Germany

[2] Bioprojet Biotech, F-35762 St Gregoire, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 07期

关键词：

histamine; antagonist; ligand; fluorescence; H3; medicinal chemistry;

D O I：

10.1016/j.bmcl.2005.12.084

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

omega-Piperidinoalkanamine derivatives with fluorescent moieties (2-cyanoisoindol-1-yl, 7-nitrobenzofurazan-4-yl) have been synthesized starting from piperidine in three steps. The compounds display moderate to good histamine hH(3) receptor affinities with K-i values ranging from 178 to 11 nM The new compounds may act as tools for identification and understanding of the binding site on the histamine H-3 receptor. (C) 2006 Elsevier Ltd. All rights reserved.

引用

页码：1938 / 1940

页数：3

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