High-affinity fluorescent ligands for the 5-HT3 receptor

被引：17
|
作者：
Simonin, Jonathan [1 ]
Vernekar, Sanjeev Kumar V. [2 ]
Thompson, Andrew J. [3 ]
Hothersall, J. Daniel [4 ]
Connolly, Christopher N. [4 ]
Lummis, Sarah C. R. [3 ]
Lochner, Martin [1 ]
机构：
[1] Univ Bern, Dept Chem & Biochem, CH-3012 Bern, Switzerland
[2] Univ Minnesota, Ctr Drug Design, Minneapolis, MN 55455 USA
[3] Univ Cambridge, Dept Biochem, Cambridge CB2 1QW, England
[4] Univ Dundee, Ninewells Med Sch, Med Res Inst, Ctr Neurosci, Dundee DD1 9SY, Scotland
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 02期
基金：
瑞士国家科学基金会; 英国工程与自然科学研究理事会; 英国惠康基金;
关键词：
5-HT3; receptor; Cys-loop ligand-gated ion channels; Fluorescent ligands; Radioligand binding; In vivo imaging; ANTAGONISTS;
D O I：
10.1016/j.bmcl.2011.11.097
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The synthesis, photophysical and biological characterization of a small library of fluorescent 5-HT3 receptor ligands is described. Several of these novel granisetron conjugates have high quantum yields and show high affinity for the human 5-HT(3)AR. (C) 2011 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1151 / 1155
页数：5
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