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Cocaine inhibits SCN5A. 10 / 10
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"When we delivered a single conditioning pulse to +30 mV for 300 ms followed by a 100-ms interval at the holding potential and a test pulse to +30 mV, cocaine blocked a similar percentage of mu 1 chann[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"The simulation predicted steady-state cocaine block of mu 1 channels within a few millivolts at the midpoint of block, whereas steady-state cocaine block of hH1 channels was several millivolts more ne[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"We suggested that the differences in steady-state inactivation between hH1 channels and mu 1 channels may in part explain the cardiotoxic effects of cocaine.In the present study we further addressed s[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Much evidence shows an inhibition of voltage-gated Na channels by cocaine (for example, see [72,243,244]), where a tonic (TTX-resistant) Nav1.5 channel current amplitude reduction produced by cocaine (0.05 mM) is ca."
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"At intermediate voltages (-120 mV to -90 mV), however, cocaine blocked hH1 channels with much greater potency, suggesting that the modulation of receptor affinity differs at the two isoforms."
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"Although we lacked direct evidence to support our hypothesis, we suggested that cocaine blocked a larger proportion of hH1 channels than mu 1 channels at intermediate voltages because of greater stead[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"At strongly negative conditioning pulses, 30 mu M cocaine blocked ~ 10% of the resting mu 1 (1-3) hH1 (4) and mu 1 (1) hH1 (2-4) channels, which was similar to the block of resting mu 1 and hH1 channe[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"The fractional amplitudes of the fast time constants of recovery from cocaine block of mu 1 and hH1 channels were 26.3 +/- 1.4% and 27.5 +/- 1.4% (p> 0.05), respectively."
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"The time constants of recovery from 30 mu M cocaine block of mu 1 and hH1 channels were 6.5 +/- 0.4 s (n = 5) and 6.8 +/- 0.5 s (n = 6; p> 0.5), respectively."
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"We compared use dependent cocaine block of mu 1 and hH1 channels using 1 and 2 Hz stimulation rates but found no difference between the channels in the extent of use dependent block."
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