Fluorine-18 labelled substituted benzazepines as potential radiotracers for imaging dopamine D1 receptors by positron emission tomography.
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.
Mukherjee
J
J
Franklin McLean Institute, Department of Radiology, University of Chicago, IL 60637.
Yang
Z Y
ZY
Perry
B D
BD
D000818:Animals; D001552:Benzazepines / Q000378:metabolism*; D005462:Fluorine Radioisotopes; D008253:Macaca mulatta; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D017447:Receptors, Dopamine D1 / Q000032:analysis*; D014055:Tomography, Emission-Computed
D001552:Benzazepines; D005462:Fluorine Radioisotopes; D017447:Receptors, Dopamine D1; C051391:Sch 38548