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Figure 1. VU573 inhibits mGluR8-activated Kir3.1/3.2 channel activity in thallium flux assays. (A) Representative FluoZin-2 fluorescence traces recorded from HEK-293 cells stably expressing mGluR8 and Kir3.1/3.2 before and after co-application of thallium and different doses of glutamate (shaded box). From an 11-point glutamate concentration–response curve (not shown), the glutamate concentration evoking approximately 80% (EC80) of the maximal response (ECmax) was determined and used for subsequent experiments. (B) Representative traces for changes of Tl+-induced FluoZin-2 fluorescence following 20 min pre-treatment of cells with the indicated concentrations of VU573 and subsequent thallium and glutamate-EC80 addition (shaded box). (C) Mean ± SEM concentration–response curve for VU573-dependent inhibition of Kir3.1/3.2 (n = 3). The chemical structure of VU573 is shown in the inset. (D) Representative FluoZin-2 fluorescence traces recorded from monoclonal Kir1.1-S44D expressing cells cultured overnight in absence (−Tet) or presence (+Tet) of Tetracycline. (E) Representative traces for changes of Tl+-induced FluoZin-2 fluorescence following pre-treatment of cells with the indicated concentrations of VU573 and then exposed to thallium (shaded box). (F) Mean ± SEM concentration–response curve for VU573-dependent inhibition of Kir1.1-S44D (n = 3). Image published in: Raphemot R et al. (2011) Copyright © 2011 Raphemot, Lonergan, Nguyen, Utley, Lewis, Kadakia, Weaver, Gogliotti, Hopkins, Lindsley and Denton. Creative Commons Attribution-NonCommercial license Larger Image Printer Friendly View

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