PET measurements of neuroreceptor occupancy by typical and atypical neuroleptics

Peter F. Goyer, Marc S. Berridge, Evan D. Morris, William E. Semple, Beth A. Compton-Toth, S. Charles Schulz, Dean F. Wong, Flora Miraldi, Herbert Y. Meltzer

Research output: Contribution to journalArticle

Abstract

The goal of this study was to use PET and 11C-N-methylspiperone (11C-NMSP) to measure the differences in relative occupancy of serotonin (5-hydroxytryptamine-2 or 5-HT(2A) and dopamine-2 (D2) neuroreceptors in subjects being treated with typical or atypical antipsychotic drugs. Methods: We used PET and single-dose 11C-NMSP to measure receptor indices and relative receptor occupancy of 5-HT(2A) receptors in frontal cortex and D2 receptors in basal ganglia in five subjects who were neuroleptic free, five subjects who were being treated with typical antipsychotic drugs and five subjects who were being treated with clozapine, an atypical antipsychotic drug. Results: Among the three groups, there were significant differences in 5-HT(2A) indices, D2 indices and the ratio of 5-HT(2A) to D2 indices. With no overlap, the 5-HT(2A) index separated all subjects who received clozapine and the D2 index separated the remaining two groups. Conclusion: Typical antipsychotic and atypical antipsychotic subjects do have differing patterns of 5-HT(2A) and D2 relative receptor occupancy when measured with a single PET scan, single 11C-NMSP radiotracer dose and no separately injected 'cold' pharmaceutical.

Original languageEnglish (US)
Pages (from-to)1122-1127
Number of pages6
JournalJournal of Nuclear Medicine
Volume37
Issue number7
StatePublished - Jul 1996

Keywords

  • PET
  • carbon-11-N-methylspiperone
  • neuroreceptor occupancy

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging

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    Goyer, P. F., Berridge, M. S., Morris, E. D., Semple, W. E., Compton-Toth, B. A., Schulz, S. C., Wong, D. F., Miraldi, F., & Meltzer, H. Y. (1996). PET measurements of neuroreceptor occupancy by typical and atypical neuroleptics. Journal of Nuclear Medicine, 37(7), 1122-1127.