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.
D000818:Animals; D001921:Brain / Q000201:enzymology / Q000378:metabolism; D001923:Brain Chemistry / Q000187:drug effects*; D002795:Choline O-Acetyltransferase / Q000037:antagonists & inhibitors; D003913:Dextroamphetamine / Q000032:analysis / Q000378:metabolism*; D008297:Male; D009286:Naphthylvinylpyridine / Q000494:pharmacology*; D011335:Proadifen / Q000494:pharmacology; D011725:Pyridines / Q000494:pharmacology*; D051381:Rats
D011725:Pyridines; D009286:Naphthylvinylpyridine; D011335:Proadifen; D002795:Choline O-Acetyltransferase; D003913:Dextroamphetamine