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ID: ALA1149505

Journal: Bioorg Med Chem Lett

Title: Des-keto lobeline analogs with increased potency and selectivity at dopamine and serotonin transporters.

Authors: Zheng G, Horton DB, Deaciuc AG, Dwoskin LP, Crooks PA.

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 alpha4beta2( *) and alpha7( *) neuronal nicotinic acetylcholine receptors (nAChRs). The enantiomers 8R-hydroxylobel-9-ene (3a) and 10S-hydroxylobel-7-ene (3c) exhibited high potency and selectivity at SERT and DAT, respectively.

CiteXplore: 16905316

DOI: 10.1016/j.bmcl.2006.07.070