Parthenolide acts as a cocaine antagonist in the human dopamine transporter

2025/06/24 by Oné R. Pagán
Medicine · #Epilepsy research and treatment #Pharmacological Effects and Toxicity Studies

paper · doi:10.17912/micropub.biology.001720

openalex publication_date 2025/06/24 · openalex created_date 2025/10/10 · openalex updated_date 2026/07/01

Abstract

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.

Citations

• Advances in chemistry and bioactivity of parthenolide

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