Abstract
A series of des-keto lobeline analogs has been synthesized and evaluated for their ability to inhibit the dopamine transporter (DAT) and serotonin transporter (SERT) function and for their affinity for the synaptic vesicle monoamine transporter (VMAT2), as well as for α4β2 ∗ and α7 ∗ neuronal nicotinic acetylcholine receptors (nAChRs). The enantiomers 8 R-hydroxylobel-9-ene ( 3a) and 10 S-hydroxylobel-7-ene ( 3c) exhibited high potency and selectivity at SERT and DAT, respectively.
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