Figure 2From: Activation of TRPA1 by membrane permeable local anesthetics Lidocaine activates human TRPA1. A. Representative inward currents in HEK293t cells expressing hTRPA1 activated by 3, 10, 30 and 100 mM lidocaine. Cells were held at -60 mV and only one concentration was applied on each cell. B. Concentration-dependent activation of hTRPV1 by lidocaine. The Hill-equation was applied to calculate the EC50 value. Transmembrane domain 5 is a determinant for species different activation of TRPA1 by lidocaine C. Representative inward currents evoked by 30 mM lidocaine on mTRPA1-WT, and the chimeras mTRPA1-hTM5/6 and hTRPA1-mTM5/6. Note the lack of a resurging current for mTRPA1-hTM5/6. D. Typical experiments for lidocaine-induced block of MO-evoked inward currents on hTRPA1-WT, mTRPA1-hTM5/6, mTRPA1-WT and hTRPA1-mTM5/6. Lidocaine was co-applied with MO during the steady-state phase of MO-evoked currents and experiments were performed in a Ca2+-free extracellular solution to minimize desensitization. Note the slow onset of lidocaine-induced block for hTRPA1-WT and mTRPA1-hTM5/6 as compared to mTRPA1-WT and hTRPA1-mTM5/6. Cells were held at -60 mV.Back to article page