Elevation of amphetamine levels in rat brain after administration of the choline acetyltransferase inhibitor 4-(1-Naphthylvinyl) pyridine (NVP).

Following amphetamine administration both NVP and SKF-525A cause elevations in whole brain levels of amphetamine compared with saline treated controls. NVP was found to be about 3 times more active than SKF-525A; significant effects were obtained after doses of 0.625mg/kg and above. NVP also inhibited brain choline acetyltransferase in vitro (I50 of 4.0 x 10-5 M). Following the administration of NVP (20-200 MG/KG, I.P), there was a dose-dependent inhibition of this enzyme in brain. These results suggest that potentiation of the behavioral effects of amphetamine by NVP, which occur after doses of 5 mg/kg of NVP, are probably related to its inhibitory effects on amphetamine metabolism.