Which Form of Dopamine Is the Substrate for the Human Dopamine Transporter: the Cationic or the Uncharged Species?

Autor: Lijuan C. Wang, Maarten E.A. Reith, Janet L. Berfield
Rok vydání: 1999
Předmět:
Zdroj: Journal of Biological Chemistry. 274:4876-4882
ISSN: 0021-9258
DOI: 10.1074/jbc.274.8.4876
Popis: The question of which is the active form of dopamine for the neuronal dopamine transporter is addressed in HEK-293 cells expressing the human dopamine transporter. The Km value for [3H]dopamine uptake fell sharply when the pH was increased from 6.0 to 7.4 and then changed less between pH 7.4 and 8.2. The KI for dopamine in inhibiting the cocaine analog [3H]2beta-carbomethoxy-3beta-(4-fluorophenyl)tropane binding displayed an identical pH dependence, suggesting that changes in uptake result from changes in dopamine recognition. Dopamine can exist in the anionic, neutral, cationic, or zwitterionic form, and the contribution of each form was calculated. The contribution of the anion is extremely low (
Databáze: OpenAIRE