Development of a selective and potent radioactive ligand for histamine H3 receptors: A compound potentially useful for receptor occupancy studies

We developed 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. [3H]1 displayed appreciable specific signal in brain slices, demonstrating the utility as a selective radioligand for histamine H3 receptor occupancy assay.