Radiosynthesis and quality control of [11C]TASP457 as a clinically useful PET ligand for imaging of histamine H3 receptors in human brain

Recently, 6-[(1-cyclobutylpiperidin-4-yl)oxy]- 1-(6-[11C]methoxypyridin-3-yl)-3,4-dihydroquinolin-2(1H)-one ([11C]TASP457, [11C]2) has been developed as a novel PET ligand for histamine H3 receptors in brain. [11C]2 is potentially suitable for imaging H3 receptors in rat and monkey brains, which has motivated us to perform first-in-human study of [11C]2 for qualifying H3 receptors in human brain. In this paper, we report efficient radiosynthesis of [11C]2 to obtain sufficient radioactivity and high quality for clinical application.
Source: Nuclear Medicine and Biology - Category: Nuclear Medicine Authors: Source Type: research