• KCNQ1
  • Blocks K V 7.2+7.3 (KCNQ2+3) / M-currents (IC 50 = 0.6 - 0.98 μ M) and K V 7.1 (KCNQ1) homomeric channels (IC 50 = 0.75 μ M) but is less potent against K V 7.1/minK channels (IC 50 = 11.1 μ M). Augments hippocampal ACh release and is a cognitive enhancer following oral administration in vivo . (tocris.com)
  • In addition, KCNE2 forms reciprocally regulating tripartite complexes in the choroid plexus epithelium with the KCNQ1 α subunit and the sodium-dependent myo-inositol transporter, SMIT1. (wikipedia.org)
  • In these cells, KCNQ1-KCNE2 K+ channels, which are constitutively active, provide a conduit to return K+ ions back to the stomach lumen. (wikipedia.org)
  • While KCNQ1 channels are inhibited by low extracellular pH, KCNQ1-KCNE2 channels activity is augmented by extracellular protons, an ideal characteristic for their role in parietal cells. (wikipedia.org)
  • KCNE2 forms constitutively active K+ channels with KCNQ1 in the basolateral membrane of thyroid epithelial cells. (wikipedia.org)
  • KCNQ1-KCNE2 is required for optimal iodide uptake into the thyroid by the basolateral sodium iodide symporter (NIS). (wikipedia.org)
  • KCNQ3
  • Disruption of calmodulin binding to KCNQ2 also impairs enrichment of heteromeric KCNQ2/KCNQ3 channels at the axonal surface by blocking their trafficking from the endoplasmic reticulum to the axon. (nih.gov)
  • currents
  • Calcium accumulation during triggering stimuli appears to attenuate ERG currents, leading to membrane potential depolarization and increased input resistance, two critical elements generating persistent firing. (jneurosci.org)
  • Our results suggest that a reduction in the currents normally mediated by Ether-a-go-go-Related Gene (ERG) K + channels contributes to persistent firing in neocortical pyramidal cells. (jneurosci.org)
  • blockers
  • Three chemically diverse ERG channel blockers (terfenadine, ErgToxin-1, and E-4031) abolished persistent firing and the underlying increase in input resistance in deep pyramidal cells in temporal and prefrontal association neocortex. (jneurosci.org)
  • hERG
  • New compounds such as the HERG channel activator (3 R ,4 R )-4-[3-(6-methoxy-quinolin-4-yl)-3-oxo-propyl]-1-[3-(2,3,5-trifluoro-phenyl)-prop-2-ynyl]-piperidine-3-carboxylic acid (RPR260243) will enable us to increase our understanding in cation channel modulation and to test the concept of channel activation as a clinically relevant principle in treatment of channelopathies. (aspetjournals.org)
  • influx
  • In ventricular myocytes, excitation-contraction (EC) coupling occurs via a Ca 2+ induced Ca 2+ release mechanism such that the depolarization created by an action potential (AP) triggers Ca 2+ influx through voltage-dependent L-type Ca 2+ channels (i.e. (washington.edu)
  • Using electrophysiological, and optical approaches, we have found that an allosteric interaction between the C-terminal domains of voltage-gated Ca V 1.2 channels induces an increase in the open probability of the channels that amplifies Ca 2+ influx during the AP and contributes to reproducible EC-coupling. (washington.edu)
  • Suppression of Ca 2+ influx through voltage-activated Ca 2+ channels by 200 μM Cd 2+ resulted mainly in moderate increase of steady-state firing frequency and increase of single AP repolarization rate, however, without abolishing the basic pattern of tonic firing. (50webs.com)
  • gene
  • Abnormalities of ion channel function are responsible for a variety of non-neurological disorders including Bartter syndrome, X linked nephrolithiasis, neonatal hyperinsulinism, long QT syndromes, and most notably defects in function of the CFTR chloride channel gene causing cystic fibrosis. (bmj.com)
  • Such genetic methods allowed the genetic identification of the "Shaker" K+ channel gene in Drosophila before ion channel gene sequences were well known. (wikipedia.org)
  • We found multiple lines of evidence suggesting that a component of the underlying hyperexcitability associated with persistent firing reflects a reduction in the standing (leak) K + current mediated by Ether-a-go-go-Related Gene (ERG) channels. (jneurosci.org)
  • cation channel
  • Shortage in cation channel activators prevents testing of efficiency of activators in a variety of indications. (aspetjournals.org)
  • This shortage might result from the relative incapability of modern drug screening methods, but increasing knowledge about cation channel activator binding and action might enable us in the future to use in silico-guided drug design of channel modulators. (aspetjournals.org)
  • mechanism
  • The mechanism that permits coordinated opening of multiple Ca v 1.2 channels during EC-coupling, however, has not yet been elucidated. (washington.edu)
  • Current
  • The current generated by this channel is inhibited by M1 muscarinic acetylcholine receptors and is activated by retigabine, a novel anti-convulsant drug. (bertin-bioreagent.com)
  • diseases
  • The fruits of these collaborations include recognition that diseases caused by ion channel dysfunction may have genetic and autoimmune aetiologies. (bmj.com)
  • activation
  • In addition, the most common treatments for asthma, β-adrenergic agonists, apparently confer much of their effects through activation of large conductance Ca 2+ -activated (BK-type) K + channels ( Kotlikoff and Kamm, 1996 ). (frontiersin.org)
  • conductance
  • It was found that potassium conductance highly sensitive to external TEA (1 mM ) or 4-aminopyridine (4-AP, 200 μM) is responsible for fast repolarization and afterhyperpolarization of a single AP, providing the cells with the ability for high-frequency firing. (50webs.com)
  • Potassium conductance sensitive to α- dendrotoxin (α-DTX, 100 nM ) did not play such a role. (50webs.com)