期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 15, 页码 4075-4078出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.06.025
关键词
Histamine H-3 receptors; Inverse agonist; Radioligand; Receptor occupancy
Radioligands are powerful tools for examining the pharmacological profiles of chemical leads and thus facilitate drug discovery. In this study, we identified and characterized 3-([1,1,1-H-3]methyl)-2-(4-{[3-(1-pyrrolidinyl)propyl]oxy} phenyl)-4(3H)-quinazolinone ([H-3]1) as a potent and selective radioligand for histamine H-3 receptors. Radioligand [H-3]1 exhibited appreciable specific signal in brain slices prepared from wild-type mice but not from histamine H-3 receptor-deficient mice, demonstrating the specificity and utility of [H-3]1 as a selective histamine H-3 receptor radioligand for ex-vivo receptor occupancy assays. (C) 2009 Elsevier Ltd. All rights reserved.
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