In vivo evaluation of [123I]-8-[4-[2-(5-Iodothienyl)]-4-oxobutyl]-3-methyl-1-phenyl-1, 3, 8-triazaspiro [4.5] decan-4-one as a potential dopamine D2 receptor radioligand … (original) (raw)

The compound [123I]-8-[4-[2-(5-Iodothienyl)]-4-oxobutyl]-3-methyl-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one has been synthesized as a potential selective ligand for dopamine D2 receptors. In vivo studies in male Wistar rats showed moderate brain uptake and a maximum striatum-to-cerebellum ratio of 2.6 at 20 minutes post-injection. However, rapid clearance from the brain and moderate ratios suggest limited effectiveness compared to existing clinical radioligands, emphasizing the need for further development.