Serial [18F]N-methylspiroperidol PET studies to measure changes in antipsychotic drug D-2 receptor occupancy in schizophrenic patients

M. Smith, A. P. Wolf, J. D. Brodie, C. D. Arnett, F. Barouche, C. Y. Shiue, J. S. Fowler, J. A.G. Russell, R. R. MacGregor, A. Wolkin, B. Angrist, J. Rotrosen, E. Peselow

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Abstract

An indirect approach to the relationship among drug dose, plasma level, and the competition between a labeled neuroleptic drug [18F]N-methylspiroperidol (18F-NMS) for binding sites in striatal tissue in normal and schizophrenic subjects is described. The slope of the line plotting the ratio of activity in the striatum (As) to activity in the cerebellum (Ac) versus time up to 5 hr postinjection of 18F-NMS is taken as a marker of site occupancy. An inverse relation between labeled competitor uptake and drug plasma level has been demonstrated for the classes of antipsychotic drug studied. Striatal uptake studies showed a progressive increase in all subjects following drug withdrawal up to 156 hr postwithdrawal. Uptake and clearance of 18F-NMS in cerebellar tissue was not appreciably affected by antipsychotic medication or drug withdrawal.

Original languageEnglish
Pages (from-to)653-663
Number of pages11
JournalBiological Psychiatry
Volume23
Issue number7
DOIs
StatePublished - 1 Apr 1988
Externally publishedYes

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