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. 2011 Mar;79(3):411–419. doi: 10.1124/mol.110.069492

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Copyright © 2011 The American Society for Pharmacology and Experimental Therapeutics

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Fig. 8. — Insertion of a tryptophan in the back pathway reduces drug entry and exit. A, outside, mean peak currents ± S.E.M., recorded with 20 μM D575 in the bath, in WT (□, n = 3) and L1825W channels (■, n = 6). Currents were normalized to the first pulse of the train and mean control values were subtracted. Insets, representative currents elicited by repetitive depolarizations from −110 to −10 mV with an interpulse interval of 100 ms in a cell expressing L1825W, recorded with 20 μM D575 in the bath. τ Values from exponential fits show no change with voltage. B, inside: i, mean peak currents ± S.E.M., recorded with 200 μM D575 included in the pipette, in WT (□, n = 3) and L1825W channels (■, n = 4). Currents were normalized to the first pulse of the train, and mean control values were subtracted. Inset, representative currents elicited by repetitive depolarizations from −110 to −10 mV with an interpulse interval of 100 ms in a cell expressing L1825W, recorded with 200 μM D575 in the pipette. ii, τ values from exponential fits show voltage-dependence for D575 in both WT (□) and L1825W channels (■). iii, comparing the extent of block obtained with 200 μM D575 in WT () and L1825W channels (□) shows some voltage-dependence in each case, with much greater block obtained in L1825W channels at the same drug concentration.

Inline graphic — Insertion of a tryptophan in the back pathway reduces drug entry and exit. A, outside, mean peak currents ± S.E.M., recorded with 20 μM D575 in the bath, in WT (□, n = 3) and L1825W channels (■, n = 6). Currents were normalized to the first pulse of the train and mean control values were subtracted. Insets, representative currents elicited by repetitive depolarizations from −110 to −10 mV with an interpulse interval of 100 ms in a cell expressing L1825W, recorded with 20 μM D575 in the bath. τ Values from exponential fits show no change with voltage. B, inside: i, mean peak currents ± S.E.M., recorded with 200 μM D575 included in the pipette, in WT (□, n = 3) and L1825W channels (■, n = 4). Currents were normalized to the first pulse of the train, and mean control values were subtracted. Inset, representative currents elicited by repetitive depolarizations from −110 to −10 mV with an interpulse interval of 100 ms in a cell expressing L1825W, recorded with 200 μM D575 in the pipette. ii, τ values from exponential fits show voltage-dependence for D575 in both WT (□) and L1825W channels (■). iii, comparing the extent of block obtained with 200 μM D575 in WT () and L1825W channels (□) shows some voltage-dependence in each case, with much greater block obtained in L1825W channels at the same drug concentration.

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