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. 2008 Jan 21;153(6):1324–1330. doi: 10.1038/sj.bjp.0707675

Figure 1.

Figure 1

Inhibition of transient receptor potential melastatin 2 (TRPM2) currents by 2-aminoethoxydiphenyl borate (2-APB) in human embryonic kidney cells (HEK293 cells) expressing TRPM2. (a) A representative trace of TRPM2 current activated by ADP-ribose (ADPR; 100 μM) and its desensitization. (bd) The known TRPM2 inhibitors—miconazole (10 μM; b), N-(p-amylcinnamoyl)anthranilic acid (ACA, 20 μM; c) and flufenamic acid (FFA, 200 μM; d)—inhibited TRPM2 currents activated by ADPR (100 μM) at room temperature. Bars indicate duration of the compound application. (e) Dose-dependent inhibition of ADPR-activated TRPM2 currents by 2-APB at room temperature. Vh=−60 mV. (f) Current–voltage relation (left) of ADPR-activated whole-cell currents before activation (right upper), during peak activation (right second upper), after inhibition by 10 μM of 2-APB (right third upper) and after inhibition by 100 μM of 2-APB (right lower). The inset on the left indicates the step-pulse protocol.