Parthenolide acts as a cocaine antagonist in the human dopamine transporter.

In this work, I describe the effects of parthenolide, a naturally occurring sesquiterpene lactone, on radiolabeled cocaine binding and on radiolabeled dopamine uptake in the human dopamine transporter expressed on HEK-293 cells (HEK/DAT cells). Parthenolide displaces radiolabeled cocaine in a concentration-dependent manner and does not display any significant inhibition of radiolabeled dopamine uptake. Further, parthenolide seems to alleviate the inhibition of dopamine uptake by 5 μM unlabeled cocaine at sub-toxic parthenolide concentrations.