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

Abstract.

The uptake of norsalsolinol, a neurotoxin candidate causing parkinsonism-like symptoms, was studied in PC12 cells. The compound was actively taken up by the PC12 cells, with a K _m value of 176.2±9.1 µM 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 µM. These results suggest that norsalsolinol is taken up into PC12 cells mainly by the dopamine transporter.