19F nuclear magnetic resonance spectroscopy of neuroleptics: the first in vivo pharmacokinetics of trifluoperazine in the rat brain and the first in vivo spectrum of fluphenazine in the human brain.

ABSTRACT

In vivo 19F nuclear magnetic resonance (19F-NMR) spectroscopy measurements of trifluorinated neuroleptics (fluphenazine--FL and trifluoperazine--TFP) were made in rat brain as well as in human brain. Animal studies were performed at 4.7 Tesla. Using rats that have been treated with FL over a period of 3 weeks, a NMR signal could be detected within 8-15 min. Following a single intravenous injection of TFP, brain levels could be monitored with a time resolution of 30 min. The first 19F-NMR examination of a patient was made at 3.0 Tesla 1 day after injection of FL decanoate (37.5 mg) in the course of which a signal could be detected within 30 min. It is expected that 19F-NMR will become an important tool in psychopharmacological research.