Abstract
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-([1,1,1-3H]methyl)-2-(4-{[3-(1-pyrrolidinyl)propyl]oxy} phenyl)-4(3H)-quinazolinone ([3H]1) as a potent and selective radioligand for histamine H3 receptors. Radioligand [3H]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 [3H]1 as a selective histamine H3 receptor radioligand for ex-vivo receptor occupancy assays.
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