Biochemical Pharmacology volume 79, issue 6, P897-907 2010 DOI: 10.1016/j.bcp.2009.10.016 View full text
Ligia Westrich, Sara Gil-Mast, Sandhya Kortagere, Eldo V. Kuzhikandathil

Abstract: The D3 but not D2 dopamine receptors exhibit a tolerance property in which agonist-induced D3 receptor response progressively decreases upon repeated agonist stimulation. We have previously shown that the D3 receptor tolerance property is not mediated by receptor internalization, persistent agonist binding or a decrease in receptor binding affinity. In this paper, we test the hypothesis that alterations in D3 receptor conformation underlie the tolerance property. Structural models of wild type and mutant human…

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