INVIVO F-19 NUCLEAR-MAGNETIC-RESONANCE OF A MONOFLUORINATED NEUROLEPTIC IN THE RAT

In vivo F-19 NMR measurements of the fluorinated neuroleptic melperone [4'-fluoro-4-(4-methylpiperidino)-butyrophenone hydrochloride] in the rat brain were performed using a geometrically optimized surface coil at 4.7 T. It was possible for the first time to detect a signal of a monofluorinated neuroleptic drug with a time resolution of 30 min after i.p. application. The kinetic time course of the investigated neuroleptic melperone was recorded over 6 h and showed that the half-life in the rat brain is 4.3 h. The total amount of drug and its metabolites in the brain was estimated to be 50 mum. the chemical shift of the F-19 NMR signal shows the same upfield shift relative to that in aqueous solution as has been reported for trifluorinated neuroleptic drugs.