• neurons
  • Various neurotransmitters excite neurons by suppressing a ubiquitous, voltage-dependent, noninactivating K + conductance called the M-conductance (g M ). In bullfrog sympathetic ganglion neurons the suppression of g M by the P2Y agonist ATP involves phospholipase C (PLC). (jneurosci.org)
  • Various pharmaceutical companies developed synthetic molecules activating these channels in order to prevent excessive neurotoxic calcium entry in neurons . (epfl.ch)
  • basolateral
  • 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)
  • The purpose of the study was to examine the interaction of XE991 with other types of K + channel, especially those in the basolateral membranes of murine epithelia. (aspetjournals.org)
  • XE991 inhibited the chloride secretory current in colonic epithelia by an interaction with basolateral K + channels when forskolin was used as the stimulus. (aspetjournals.org)
  • 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)
  • Na(V)1.4) encodes Nav1.4, a member of the sodium channel alpha subunit gene family. (epfl.ch)
  • residues
  • Several charged residues of the VSD, in particular four arginine residues located regularly at every third position on the S4 segment, are known to move across the transmembrane field and contribute to the gating charge. (wikipedia.org)
  • KCNQ1
  • 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)
  • Presumably, if the activity of XE991 had been enhanced when KCNQ1 channels were expressed with KCNE1, the potential to cause long QT syndrome would have increased. (aspetjournals.org)
  • Although the colonic tissue showed the presence of both KCNQ1 and KCNE3 mRNA, the airway epithelium also showed, uniquely, the presence of mRNA for KCNQ2. (aspetjournals.org)
  • 2000
  • The skeletal muscle a subunit functions as ion-conducting channel and consists of large polypeptides (1700-2000 amino acids) that fold into four highly homologous somains (repeats I-IV) containing six transmembrane segments each (S1-S6). (epfl.ch)
  • activation
  • BMS-204352 (BMS) was developed as a neuroprotective drug for disease conditions such as ischemic stroke and it has been shown to have a protective effect, due to activation of big-conductance calcium-activating potassium (BKCa) channels (Gribkoff et al. (epfl.ch)
  • Activation or inhibition of K + channels in epithelia, particularly those secreting chloride, has potentially useful therapeutic applications in diseases as diverse as cystic fibrosis, where chloride secretion is deficient, and secretory diarrhea, where it is in excess. (aspetjournals.org)
  • receptor
  • Ranolazine block of open Na+ channels is via the conserved local anesthetic receptor albeit with a relatively slow on-rate. (epfl.ch)
  • cell
  • Nav1.4 channels are located in the sarcolemma and T-tubular membranes, with a high density near the endplate of the muscle cell. (epfl.ch)
  • Current
  • This charge transfer is measured as a transient capacitive current that precedes opening of the channel. (wikipedia.org)
  • Our study was also aimed at extending our current knowledge on the in situ vascular pharmacology of DPO-1 and XE991 regarding K V 1.5 and BK Ca channels, in helping to identify the nature of K + channels that could contribute to PVAT-mediated relaxation. (frontiersin.org)
  • The cognitive enhancer XE991 interacts with K + channels consisting of KCNQ2 and KCNQ3 heteromultimers to block the M-current. (aspetjournals.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)
  • The known specificity of these drugs strongly suggested that this 4-AP and TEA-sensitive conductance is mediated by Kv3 potassium channels. (50webs.com)
  • diseases
  • The fruits of these collaborations include recognition that diseases caused by ion channel dysfunction may have genetic and autoimmune aetiologies. (bmj.com)
  • regulation
  • In this study, we tested whether K V 1.5 channels are involved in the control of mesenteric arterial tone and its regulation by PVAT. (frontiersin.org)
  • Over the past decade, various potassium (K + ) channels have been implicated as important players in the regulation of arterial vascular tone and its control by perivascular adipose tissue (PVAT). (frontiersin.org)
  • KCNE1
  • mRNA for both these components of the cAMP-sensitive K + channels were found in high abundance in the colon, whereas KCNE1 was barely detectable. (aspetjournals.org)
  • targets
  • BK channels are pharmacological targets for the treatment of stroke. (epfl.ch)
  • Because EBIO also activates Ca 2+ -sensitive K + channels, whereas forskolin activates only cAMP-sensitive K + channels, it is concluded that the latter are the targets for XE991. (aspetjournals.org)
  • tonic
  • 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)
  • sensitive
  • However, until now the in vivo pharmacology of the involved vascular K V channels with regard to XE991 remains undetermined, since XE991 effects may involve Ca 2+ activated BK Ca channels and/or voltage-dependent K V 1.5 channels sensitive to diphenyl phosphine oxide-1 (DPO-1). (frontiersin.org)
  • BK Ca channels and/or DPO-1 sensitive K V 1.5 channels in VSMCs are not the downstream mediators of the XE991 effects on PVAT-dependent arterial vasorelaxation. (frontiersin.org)