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

The uptake of norsalsolinol, a neurotoxin candidate causing parkinsonism-li ke 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 ve locity of 55.6 +/- 7.0 pmol/min per mg protein; norsalsolinol uptake was de pendent on the presence of extracellular Na+. The uptake of norsalsolinol w as sensitive to two dopamine transporter inhibitors, GBR-12909 and reserpin e, but was less sensitive to desipramine, a noradrenaline transporter inhib itor. Dopamine competitively inhibited norsalsolinol uptake into PC12 cells with a K-i value of 271.2 +/- 61.6 muM. These results suggest that norsals olinol is taken up into PC12 cells mainly by the dopamine transporter.