The functioning neuronal transporter for dopamine: kinetic mechanisms and effects of amphetamines, cocaine and methylphenidate

Part of the Progress in Drug Research book series (PDR, volume 59)


The dopamine transporter (DAT) is a transmembrane spanning protein that catalyzes the transport of dopamine across the neuronal membrane to concentrate the neurotransmitter inside the cell. Although the uptake of dopamine has been studied since the 1960s, more recent advances in knowledge of the protein itself and in making kinetically resolved measurements of its action have led to more insights into its mechanism and pharmacology. The literature of the kinetics of transporters and kinetic measurements of DAT activity is reviewed to provide an overview of the multisubstrate mechanism of DAT activity, its pharmacology with regard to amphetamine, cocaine and methylphenidate, and correlations of DAT activity with some behavioral outputs.

Key words

Amphetamine benztropine cocaethylene cocaine cocaine self-administration dopamine dopamine transporter GBR-12909 locomotor activity mazindol methylphenidate nomifensine rotating disk electrode voltammetry transporter kinetics m-tyramine 


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© Springer Basel AG 2002

Authors and Affiliations

  1. 1.Department of Chemistry, School of Molecular Biosciences, and Programs in Pharmacology/Toxicology and NeuroscienceWashington State UniversityPullmanUSA

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