Title:Progress in the Search for New Dopamine Transporter Inhibitors
VOLUME: 22 ISSUE: 28
Author(s):Beata Gryzlo, Paula Zareba, Katarzyna Malawska, Anna Jakubowska and Katarzyna Kulig
Affiliation:Department of Physicochemical Drug Analysis, Department of Pharmaceutical Chemistry, Jagiellonian University Medical College, Medyczna 9, 30-688 Krakow, Poland.
Keywords:ADHD, cocaine abuse, depression, dopamine transporter inhibitor, monoamine transporter inhibitor,
tropane derivatives.
Abstract:In the present review, we provide a comprehensive summary of recent pharmacological
studies on dopamine transporter (DAT) inhibitors, which are potential treatments
for neurodegenerative and psychiatric disorders. Extensive structure-activity relationship
studies have identified numerous tropane-based ligands with high affinity and selectivity for
the DAT or with high affinity to the DAT and other monoamine transporters (dual and triple
monoamine reuptake inhibitors). The review covers advances in the field in past fifteen
years. Among the described compounds, many appear to be promising drug candidates, while other may serve
as valuable tools for research or as prototypes for new classes of selective DAT inhibitors. Special attention is
being paid to separation of the DAT inhibition from NET and SERT inhibition.
