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Regional distribution and kinetics of haloperidol binding in human brain: A pet study with [ 18 F]haloperidol
Author(s) -
Schlyer David J.,
Volkow Nora D.,
Fowler Joanna S.,
Wolf Alfred P.,
Shiue ChyngYann,
Dewey Stephen L.,
Bendriem Bernard,
Logan Jean,
Raulli Robert,
Hitzemann Robert,
Brodie Jonathan,
Alavi Abass A.,
MacGregor Robert R.
Publication year - 1992
Publication title -
synapse
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.809
H-Index - 106
eISSN - 1098-2396
pISSN - 0887-4476
DOI - 10.1002/syn.890110103
Subject(s) - haloperidol , basal ganglia , human brain , chemistry , distribution (mathematics) , pharmacokinetics , pharmacology , dopamine receptor , endocrinology , medicine , receptor , dopamine , central nervous system , psychology , neuroscience , biochemistry , mathematical analysis , mathematics
Abstract The regional distribution and the kinetics of haloperidol uptake in human brain were examined using [ 18 F]haloperidol and PET in 9 controls and 5 schizophrenics while on haloperidol medication and after haloperidol washout. The regional distribution of [ 18 F]N‐methylspiroperidol, a tracer for D 2 receptors, was measured in 1 normal subject for comparison. The uptake of [ 18 F]haloperidol in the whole brain in normals was high (6.6% of the injected dose at 2 hr), and regional distribution was much more extensive than could be accounted for by the distribution of dopamine D 2 receptors. In normals, the cerebellum, basal ganglia, and thalamus showed a greater concentration than the cortex, and there was minimal clearance of 18 F from the brain during the 10‐hr period of the study. Medicated schizophrenics showed a total brain uptake of 4.0% and had a significant clearance of [ 18 F]haloperidol from brain and a higher concentration of [ 18 F]haloperidol in plasma. After withdrawal from medication. These results are discussed in terms of the pharmacokinetics of haloperidol in the human brain and its binding to dopamine D 2 receptors and to sigma receptors. © 1992 Wiley‐Liss, Inc.