IndraLab

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Lidocaine inhibits HCN1. 9 / 9
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"Thus, inhibition of HCN1 by lidocaine likely contributes to its analgesic effects, and it will be important to determine the extent to which lidocaine inhibition of HCN1 contributes to this drug 's in vivo actions and how inhibition is impacted by voltage and current."
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"Thus, we currently favor the view that uncharged lidocaine diffuses through the plasma membrane, becomes re-protonated inside the cell and inhibits the HCN1 channel from the inside."
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"However, lidocaine inhibits three of the four mammalian HCN isoforms (HCN1 as well as HCN2 and HCN4), all of which are found in neurons and cardiomyocytes 11."
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"On the other hand, the local anesthetic lidocaine ( xref ) inhibits HCN1, HCN2, and HCN4 subunits, as well as heteromeric HCN1–HCN2 channels acting in a dose-dependent manner over a concentration range relevant for systemic use [ xref ]."
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"Lidocaine inhibited HCN1, HCN2, HCN1-HCN2, and HCN4 channel currents at 100 muM in both oocytes and/or HEK 293 cells; it caused a decrease in both tonic and maximal current (~ 30-50% inhibition) and slowed current activation kinetics for all subunits."
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"Thus, inhibition of HCN1 by lidocaine likely contributes to its analgesic effects, and it will be important to determine the extent to which lidocaine inhibition of HCN1 contributes to this drug’s in vivo actions and how inhibition is impacted by voltage and current."
28455536
sparser
"Lidocaine inhibited HCN1, HCN2, HCN1-HCN2, and HCN4 channel currents at 100 μM in both oocytes and/or HEK 293 cells; it caused a decrease in both tonic and maximal current (∼30-50% inhibition) and slowed current activation kinetics for all subunits."
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"We show that lidocaine inhibition of HCN1 mediated I h is near complete within one minute of exposure, is reversible, and involves a mechanism which is antagonized by hyperpolarizing voltages and current flow."
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"Here, we focus on lidocaine inhibition of the HCN1 isoform, which has been found throughout the brain and in the conduction system of the heart 22 and has been shown in HCN1-knockout mice to contribute to the electrical and cellular activity of different types of cells, including sinoatrial node pacemaker myocytes 23, somatosensory neurons 24, cortical neurons 25, cerebellar Purkinje neurons 26, and hippocampal neurons 27."
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