Regional distribution and kinetics of haloperidol binding in human brain: A pet study with [18F]haloperidol

David J. Schlyer, Nora D. Volkow, Joanna S. Fowler, Alfred P. Wolf, Chyng‐Yann ‐Y Shiue, Stephen L. Dewey, Bernard Bendriem, Jean Logan, Robert Raulli, Robert Hitzemann, Jonathan Brodie, Abass A. Alavi, Robert R. MacGregor

Research output: Contribution to journalArticle

41 Scopus citations

Abstract

The regional distribution and the kinetics of haloperidol uptake in human brain were examined using [18F]haloperidol and PET in 9 controls and 5 schizophrenics while on haloperidol medication and after haloperidol washout. The regional distribution of [18F]N‐methylspiroperidol, a tracer for D2 receptors, was measured in 1 normal subject for comparison. The uptake of [18F]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 D2 receptors. In normals, the cerebellum, basal ganglia, and thalamus showed a greater concentration than the cortex, and there was minimal clearance of 18F 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 [18F]haloperidol from brain and a higher concentration of [18F]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 D2 receptors and to sigma receptors. © 1992 Wiley‐Liss, Inc.

Original languageEnglish (US)
Pages (from-to)10-19
Number of pages10
JournalSynapse
Volume11
Issue number1
DOIs
StatePublished - May 1992

Keywords

  • Dopamine receptors
  • Neuroleptics
  • Schizophrenia
  • Sigma receptors

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience

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    Schlyer, D. J., Volkow, N. D., Fowler, J. S., Wolf, A. P., Shiue, CY. Y., Dewey, S. L., Bendriem, B., Logan, J., Raulli, R., Hitzemann, R., Brodie, J., Alavi, A. A., & MacGregor, R. R. (1992). Regional distribution and kinetics of haloperidol binding in human brain: A pet study with [18F]haloperidol. Synapse, 11(1), 10-19. https://doi.org/10.1002/syn.890110103