A COMPARISON OF THE INHIBITION OF THE HUMAN DOPAMINE TRANSPORTER EXPRESSED IN HEK CELLS BY THE WAKE PROMOTING DRUG MODAFINIL AND A STRUCTURAL ANALOG

Matthew Kahlscheuer1,  Amber Schuh1,  Jamie Wieting*1,  Amanda McGovern1,  Jonathon Russel1,  Cynthia Ochsner2

St. Norbert College1, Chemistry, De Pere, WI 54115
St Norbert College2, Chemistry, De Pere, WI 54115

ochsce@snc.edu

Abstract

Rotating disk electrode voltammetry was used to measure the time-resolved transport of dopamine into human embryonic kidney (HEK) cells stably expressing the human dopamine transporter (hDAT). Dopamine transport was first order with a Km and Vmax of 1.2 micromolar DA and 20.2 pmol DA/sec/104cells respectively. Modafinil, a drug used to treat narcolepsy, was determined to inhibit the human dopamine transporter in a competitive fashion. Interestingly, a close structural analog was found to be an uncompetitive inhibitor of the transporter.

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