Common Names: cardinalflower
Researchers identified lobinaline N-oxide, a water-soluble derivative of lobinaline, an atypical dopamine transporter (DAT) inhibitor lead from Lobelia cardinalis, through "target-directed evolution" of mutant L. cardinalis cell population expressing human DAT. Lobinaline N-oxide showed promising therapeutic potential to treat Substance Use Disorder (SUD) as it prolonged dopamine peak amplitudes in the ventral striatum and produced complex changes in post-peak dopamine clearance. Target-directed evolution of plant cells has been proved useful for lead optimization in drug development.