Fluorine-18 labelled substituted benzazepines as potential radiotracers for imaging dopamine D1 receptors by positron emission tomography Academic Article uri icon

abstract

  • High affinity and selective fluorinated derivatives of 7-chloro-8-hydroxy-3-methyl-1-(3'-aminophenyl)-2,3,4,5-tetrahydro-1H-3- benzazepine (SCH 38548) for dopamine D1 receptors have been prepared. The derivatives exhibit subnanomolar to nanomolar affinities for dopamine D1 receptors and micromolar to millimolar affinities for dopamine D2 and 5-HT2 receptors. Biodistribution of N-(3-[18F]fluoropropyl)SCH 38548 in rats showed specific uptake and retention (0.64% injected dose/g at 30 min) of the radiotracer in the striata with striata to cerebellum ratios reaching 12 at 2 h post-injection. Preliminary positron emission tomography scans in rhesus monkeys indicate selective uptake of the radiotracer in the striata.

publication date

  • October 1993