• inhibition
  • We therefore recorded lidocaine inhibition of voltage-clamped, tetrodotoxin-sensitive Na currents in mouse Purkinje neurons, which express a native blocking protein, and in mouse hippocampal CA3 pyramidal neurons with and without a peptide from the cytoplasmic tail of Na V β4 (the β4 peptide), which mimics endogenous open-channel block. (jneurosci.org)
  • Inhibition of Na currents by lidocaine was diminished by either the β4 peptide or the native blocking protein. (jneurosci.org)
  • We therefore examined the influence of a resurgent current-inducing blocker on lidocaine inhibition, in CA3 cells with the β4 peptide, and in Purkinje cells, which have a native open-channel blocking protein. (jneurosci.org)
  • Despite no significant difference in steady-state gating parameters between V232I+L1308F and wild-type sodium currents at baseline, use-dependent inhibition of I Na by lidocaine was more pronounced in V232I+L1308F versus wild-type (73.0±0.1% versus 18.23±0.04% at 10 μmol/L measured at 10 Hz, respectively). (ahajournals.org)
  • The inhibitory effect of α-asarone persisted in the presence of ionotropic glutamate receptor blockers but was eliminated after adding a GABA A receptor blocker, suggesting that GABA A receptors mediated the inhibition of MCs by α-asarone. (frontiersin.org)
  • At the cellular level, formation of new channels, up and down regulation of certain receptors, and altered local or descending inhibition represent some of the biological mechanisms that can lead to a hyperexcitable state, known as chronic pain. (eddoctor24h.com)
  • inhibit
  • It also suggests that α-asarone could benefit patients with cough possibly through inhibiting a Na + channel subtype to inhibit peripheral and/or central sensitization of cough reflexes. (frontiersin.org)
  • drug
  • To control channel states during drug exposure, lidocaine was applied with rapid-solution exchange techniques during steps to specific voltages. (jneurosci.org)
  • 4 This study presents a rare case of lidocaine-induced BrS phenotype with a unique novel double mutation of SCN5A capable of altering the drug-receptor interaction so as to confer on lidocaine profound use-dependent sodium channel-blocking characteristics. (ahajournals.org)
  • cells
  • In constant 100 μ m lidocaine, current-clamped Purkinje cells continued to fire spontaneously. (jneurosci.org)
  • The effects of α-asarone on a defined Na v 1.2 were characterized using transfected cells that stably expressed the Na v 1.2 channel isoform. (frontiersin.org)
  • The activation of protein kinase C completely suppresses the opening BK channels in intact rat anterior pituitary cells in physiological saline. (epfl.ch)
  • Adrenal glucocorticoids Adrenal glucocorticoids regulate adaptation mechanisms to environmental challenges ( ) and can modify the electrical excitability of BK channels in human embryonic kidney cells. (epfl.ch)
  • proteins
  • There is evidence of changes in BK channel activity by phosphorylation and/or interaction by G proteins, by mechanical stretch, and by various endothelium-derived vasoactive substances . (epfl.ch)
  • human
  • This finding indicated that channel dysfunction could lead to human disorders in which pain is a prominent symptom. (jci.org)
  • control
  • The voltage and metal sensors all control the opening of the same ionic pore in response to various physiological signals . (epfl.ch)
  • type
  • Moreover, each type of neuronal BK channels are differentially sensitive to PKA-dependent phosphorylation. (epfl.ch)