Regional distribution and kinetics of haloperidol binding in human brain: A PET study with ( super(18)F)haloperidol

The regional distribution and the kinetics of haloperidol uptake in human brain were examined using ( super(18)F)haloperidol and PET in 9 controls and 5 schizophrenics while on haloperidol medication and after haloperidol washout. The uptake of ( super(18)F)haloperidol in the whole brain in normals was high, and regional distribution was much more extensive than could be accounted for by the distribution of dopamine D sub(2) receptors. In normals, the cerebellum, basal ganglia, and thalamus showed a greater concentration than the cortex, and there was minimal clearance of super(18)F from the brain during the 10-hr period of the study. The results are discussed in terms of the pharmacokinetics of haloperidol in the human brain and its binding to dopamine D sub(2) receptors and to sigma receptors.