Uptake of the dopaminergic neurotoxin, norsalsolinol, into PC12 cells via dopamine transporter

The uptake of norsalsolinol, a neurotoxin candidate causing parkinsonism-like symptoms, was studied in PC 12 cells. The compound was actively taken up by the PC 12 cells, with a K-m value of 176.2 +/- 9.1 muM and a maximum velocity of 55.6 +/- 7.0 pmol/min per mg protein; norsalsolinol uptake was dependent on the presence of extracellular Na+. The uptake of norsalsolinol was sensitive to two dopamine transporter inhibitors, GBR-12909 and reserpine, but was less sensitive to desipramine, a noradrenaline transporter inhibitor. Dopamine competitively inhibited norsalsolinol uptake into PC12 cells with a K-i value of 271.2 +/- 61.6 muM. These results suggest that norsalsolinol is taken up into PC12 cells mainly by the dopamine transporter.