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Updated: Aug 30, 2026

A Plate-Based Assay for the Measurement of Endogenous Monoamine Release in Acute Brain Slices
Published on: August 11, 2021
Dopamine transporter as target for drug development of cocaine dependence medications
Aloke K Dutta1, Shijun Zhang, Rohit Kolhatkar
1Department of Pharmaceutical Sciences, Applebaum College of Pharmacy and Health Science, Wayne State University, 3128 Applebaun Hall, Detroit, MI 48202, USA. adutta@wayne.edu
Abstract:
Because much evidence implicates the dopamine transporter in the reinforcing effects of cocaine, development of potential medications for cocaine dependence has included the dopamine transporter as a target. The present overview covers progress in the drug development area regarding several classes of dopamine uptake inhibitors, with an emphasis on structure-activity relationships that enhance potency and selectivity at transporters for dopamine compared with those for serotonin or norepinephrine. The following categories of compounds are covered: tropane, benztropine, 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR), methylphenidate, mazindol, and phencyclidine analogs. Activity at transporters as well as on behavior is highlighted.
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