【文章名】Development of a selective and potent radioactive ligand for histamine H-3 receptors: A compound potentially useful for receptor occupancy studies
[摘要]：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 H3 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.
