• Label-free cell phenotypic profiling decodes the composition and signaling of an endogenous ATP-sensitive potassium channel. (rndsystems.com)
  • The most common genetic cause is a change in one or both copies of a gene that instructs the building of the potassium channel (ABCC8 and KCNJ11). (wikipedia.org)
  • Researchers have now found that memantine also inhibits the ATP-sensitive potassium channel (Kir6.2 channel), improving insulin signal dysfunction in the brain . (neurosciencenews.com)
  • Evidence for the involvement of the ATP-sensitive potassium channel in a novel model of hypoxic preconditioning in dogs. (doximity.com)
  • The inward-rectifier potassium channel family (also known as 2-TM channels) include the strong inward-rectifier channels (K ir 2.x), the G-protein-activated inward-rectifier channels (K ir 3.x) and the ATP-sensitive channels (K ir 6.x), which combine with sulphonylurea receptors. (tocris.com)
  • Edwards G., Weston A.,N. Pharmacology of the potassium channel openers //Cardiovasc. (kiev.ua)
  • In addition the cloned channels are activated by the potassium channel opener, pinacidil, but are not inhibited by the sulphonylurea, glibenclamide. (elsevierpure.com)
  • Previously we have shown that the activity of one of the critical ion channels needed for maintaining GnRH neurons in a hyperpolarized state, the ATP-sensitive potassium channel (K ATP ) channel, is augmented by E2 in ovariectomized females. (elsevierpure.com)
  • K ATP channels, widely represented in metabolically active tissues, are hetero-octamers composed of four regulatory SUR subunits (SUR1, SUR2A, or SUR2B) and four ATP-sensitive pore-forming inwardly rectifying potassium channel (Kir6.x) subunits (Kir6.1 or Kir6.2) [ 20 ]. (biomedcentral.com)
  • ATP-Sensitive potassium channels: a review of their cardioprotective pharmacology. (nih.gov)
  • NO-dependent mechanisms modulate both K ATP channels and participate in the pathophysiology and pharmacology of neuropathic pain. (biomedcentral.com)
  • Memantine increased CaMKII activity in the APP23 mouse hippocampus, and memantine-induced enhancement of hippocampal long-term potentiation (LTP) and CaMKII activity was totally abolished by treatment with pinacidil, a specific opener of KATP channels. (neurosciencenews.com)
  • The largest change in membrane voltage was observed with the K-ATP opener pinacidil, which caused 24 +/- 3 mV hyperpolarization. (limkinase-signal.com)
  • K ATP channels are important regulators of secretory processes and muscle contraction, and are targets for therapeutic treatment of type II diabetes by the inhibitory sulphonylureas 2 and for hypertension by activators such as pinacidil 3 . (elsevierpure.com)
  • We conclude that K+ channels are important modulators of human lymphatic contractility. (limkinase-signal.com)
  • The present experiment examined the effects of glucose and the direct K-ATP channel modulators glibenclamide and lemakalim on spontaneous alternation performance and hippocampal ACh release. (syr.edu)
  • The results demonstrate that K-ATP channel modulators influence behavior when administered directly into the hippocampus, with channel blockers enhancing and openers impairing spontaneous alternation performance, thus supporting the hypothesis that glucose enhances memory via action at central K-ATP channels. (syr.edu)
  • That lemakalim, as well as glibenclamide and glucose, increased hippocampal ACh output suggests a dissociation between the effects of K-ATP channel modulators on behavior and hippocampal ACh release. (syr.edu)
  • Stefani, MR & Gold, PE 2001, ' Intrahippocampal infusions of K-ATP channel modulators influence spontaneous alternation performance: Relationships to acetylcholine release in the hippocampus ', Journal of Neuroscience , vol. 21, no. 2, pp. 609-614. (syr.edu)
  • In the pancreas, the Kir6.2 channel blockade increases the insulin signaling, and insulin signaling decreases the blood glucose levels," says Dr. Shigeki Moriguchi. (neurosciencenews.com)
  • In the brain, insulin signaling increases the acquisition of memory through CaM kinase II activation by Kir6.2 channel blockade. (neurosciencenews.com)
  • Abstract for "Blockade of the KATP channel Kir6.2 by memantine represents a novel mechanism relevant to Alzheimer's disease therapy" by S Moriguchi, T Ishizuka, Y Yabuki, N Shioda, Y Sasaki, H Tagashira, H Yawo, J Z Yeh, H Sakagami, T Narahashi and K Fukunaga in Molecular Psychiatry . (neurosciencenews.com)
  • and eliminated arteriolar constriction during K ATP channel blockade with glibenclamide. (umn.edu)
  • K-ATP channels appear to couple glucose metabolism and neuronal excitability, with channel blockade increasing the likelihood of neurosecretion. (syr.edu)
  • In their experiment with mice, the researchers found that memantine treatment improved impaired hippocampal long-term potentiation (LTP) and memory-related behaviors in the mice through the inhibition of KATP channel Kir6.2. (neurosciencenews.com)
  • The researchers now hope that results of their study and the parallels drawn with diabetes, will lead to new treatments for Alzheimer's disease, using the inhibition of Kir6.2 channel. (neurosciencenews.com)
  • Altogether, our studies show that memantine modulates Kir6.2 activity, and that the Kir6.2 channel is a novel target for therapeutics to improve memory impairment in Alzheimer disease patients. (neurosciencenews.com)
  • The classical type of KATP channel is an octameric (4:4) complex of two structurally unrelated subunits, Kir6.2 and SUR. (ox.ac.uk)
  • However, the mRNA expression of the K ATP channel subunits Kir6.2 and SUR1 are unchanged with in vivo E2 treatment. (elsevierpure.com)
  • Specifically, current through recombinant wild-type SUR1/Kir6.2 channels expressed in COS7 cells was activated by NO, but channels formed only from truncated isoform Kir6.2 subunits without SUR1 subunits were insensitive to NO. Further, mutagenesis of SUR1 indicated that NO-induced K ATP channel activation involves interaction of NO with residues in the NBD1 of the SUR1 subunit. (biomedcentral.com)
  • In general, K-ATP channels appeared to be constitutively open since incubation with glibenclamide increased contraction frequency in spontaneously active vessels and depolarized and initiated contractions in previously quiescent vessels. (limkinase-signal.com)
  • Findlay I. Inhibition of ATP-sensitive K+ channels in cardiac muscle by the sulfonylureadrag glibenclamide // J. Pharmacol. (kiev.ua)
  • Hamada E., Takikawa R., Ito H.,Iguchi M., Terano A., Sugimoto T., Kurachi Y.Glibenclamide specifically blocks ATP-sensitive K+ channel current in atrial myocytesof guinea pig heart // Jpn. (kiev.ua)
  • Diazoxide, an opener of ATP-sensitive potassium channels, induces pharmacological preconditioning in different types of cells. (tubitak.gov.tr)
  • However, the target of action of diazoxide is not clear enough because this substance can activate ATP-sensitive potassium channels localized in mitochondria (mitoKATP) as well as in plasma membranes (KATP channels). (tubitak.gov.tr)
  • Dunne M.J., Illot M.C., Peterson O.H. Interaction of diazoxide, tolbutamide andATP4- on nucleotide-dependent K+ channels in an insulin-secreting cell line // J. Membr.Biol. (kiev.ua)
  • E2 dose-dependently (EC 50 = 0.6 nM) enhanced the diazoxide (channel opener)-activated K ATP channel currents by 1.2- to 2.0-fold, which was antagonized by ICI 182,780. (elsevierpure.com)
  • Similar to E2, STX, a membrane estrogen receptor (ER) agonist that does not bind to ERα or ERβ, also potentiated the diazoxide-induced K ATP channel current by 1.5-fold. (elsevierpure.com)
  • Bhatnagar A., Bolli R. Modulation of KATP channels to protect the ischemic miocardium:Clinical implications // Exp. (kiev.ua)
  • Cavero I., Djellas Y.,Guillon J-M. Ischemic miocardial cell protection conferred by theopening of ATP-sensitive potassium channels // Cardiovasc. (kiev.ua)
  • K ATP channels are inhibited by intracellular ATP and are stimulated by intracellular nucleotide diphosphates 1 . (elsevierpure.com)
  • We report here that the expressed channels possess all of the essential features of native cardiac K ATP channels, including sensitivity to intracellular nucleotides. (elsevierpure.com)
  • With HyperPP fast channel inactivation, mutations are usually situated in the inner parts of transmembrane segments or in the intracellular loops affecting the docking sites for the fast inactivating particle, thus impairing fast channel inactivation leading to persistent Na + current. (medscape.com)
  • The former serves as an ATP-inhibitable pore, while SUR is a regulatory subunit endowing sensitivity to sulphonylurea and K+ channel opener drugs, and the potentiatory action of MgADP. (ox.ac.uk)
  • Cell-attached and cell-free recordings of K ATP currents in large DRG neurons from control rats (sham surgery, SS) revealed activation of K ATP channels by NO exogenously released by the NO donor SNAP, through decreased sensitivity to [ATP]i. (biomedcentral.com)
  • The influence of new fluorine-containing activators of K+ channels on the vascular tone was investigated in vitro experiments on the guinea pig aorta. (kiev.ua)
  • It was shown that new fluorine-containing activators of K+ channels - PF -5 and PF-10 - are powerful vasodilator substances and PF-5 in concentration more than 0.1 mM exerts a distort of vascular reaction on the vasoconstriction. (kiev.ua)
  • Both subunits are required to form a functional channel. (ox.ac.uk)
  • We exerted the identification of mechanisms of the action of these substances using the well-known ATP-sensitive K+ channel inhibitor - glibenclamid - and showed their dose-effect correlation. (kiev.ua)
  • Other findings indicated that the mechanisms by which NO activates K ATP channels involve direct S-nitrosylation of cysteine residues in the SUR1 subunit. (biomedcentral.com)
  • Benndorf K., Thierfelder S., Doepner B., Gebhardt C., Hirche H. Role of cardiac KATPchannels during anoxia and ischemia // News Physiol. (kiev.ua)
  • Hiraoka M., Furukawa T. Functional modulation of cardiac ATP-sensitive K+ channels. (kiev.ua)
  • In cardiac tissue, K ATP channels are central regulators of post-ischaemic cardioprotection 4,5 . (elsevierpure.com)
  • NO activates K ATP channels in large DRG neurons via direct S-nitrosylation of cysteine residues in the SUR1 subunit. (biomedcentral.com)
  • Preclinical evidence suggests that this pathway results in the opening of ATP-sensitive potassium (KATP) channels, and it has been hypothesized that opening of potassium channels might be the final common pathway in the genesis of a migraine pain [1]. (ouenhoumon.com)
  • Therefore, E2 can potentiate K ATP channel activity in GnRH neurons through a membrane ER-activated PKC-PKA signaling pathway. (elsevierpure.com)
  • All forms of familial PP show the final mechanistic pathway involving aberrant depolarization, inactivating sodium channels, and muscle fiber inexcitability. (medscape.com)
  • This channel normally regulates insulin production from the β-cell in the pancreas in response to sugar levels in the blood. (wikipedia.org)
  • A change or fault in the channel leads to uncontrolled and excessive production of insulin. (wikipedia.org)
  • Electrophysiological and pharmacological characteristics vary among K ATP channels recorded from diverse tissues suggesting extensive molecular heterogeneity 1 . (elsevierpure.com)
  • The capacity of NO to activate K ATP channels via this mechanism remains intact even after spinal nerve ligation, thus providing opportunities for selective pharmacological enhancement of K ATP current even after decrease of this current by painful-like nerve injury. (biomedcentral.com)
  • One mechanism by which administration of glucose enhances cognitive functions may be by modulating central ATP-sensitive potassium (K-ATP) channels. (syr.edu)
  • Therefore, to elucidate the cellular signaling mechanism(s) modulating the channel activity, we did whole-cell patch-clamp recording of enhanced green fluorescent protein-GnRH neurons from ovariectomized female mice to study the acute effects of E2. (elsevierpure.com)
  • Structurally, the pore-forming subunit of K ir channels is the α-subunit. (tocris.com)
  • However, baseline opening of K ATP channels and their activation induced by metabolic inhibition was suppressed by axotomy. (biomedcentral.com)
  • Furthermore, activation of K ATP channels is suppressed in DRG neurons after painful-like nerve injury. (biomedcentral.com)
  • Therefore, we investigated NO modulation of K ATP channels in control and axotomized DRG neurons. (biomedcentral.com)
  • lymphatic vessel contractility from all the major classes of K+ channels [ATP-sensitive K+ (K-ATP), Ca2+-activated K+, inward rectifier K+, and voltage-dependent K+ channels], and this was confirmed at the mRNA level. (limkinase-signal.com)
  • Ion channel dysfunction is usually well compensated with normal excitation, and additional triggers are often necessary to produce muscle inexcitability owing to sustained membrane depolarization. (medscape.com)
  • POTASSIUM channels that are ATP-sensitive (K ATP ) couple membrane potential to the metabolic status of the cell. (elsevierpure.com)
  • Because their opening is determined by the cytosolic ADP/ATP ratio, K ATP channels act as metabolic sensors, linking cytosolic energetics with cellular functions in various tissues [ 21 , 22 ]. (biomedcentral.com)
  • Contraction amplitude, Selleckchem Compound Library frequency, and baseline tension were altered depending on which channel was blocked or activated. (limkinase-signal.com)
  • The aim of this study was to investigate the contribution of distinct K+ channels to human lymphatic vessel contractility. (limkinase-signal.com)
  • Adeagbo A.S., Malik K.U. Contribution of K+ channels to arachidonik acid-inducedendothelium-dependent vasodilation in rat isolated perfused mesenteric arteries //J. Pharmacol. (kiev.ua)
  • Lymph propulsion is dependent on phasic VX-689 manufacturer contractions generated by smooth muscle cells of lymphatic vessels, and it is likely that K+ channels play a critical role in regulating contractility in this tissue. (limkinase-signal.com)
  • K V 11.1 (hERG) and K ir 6 (K ATP ) channel blocker. (tocris.com)
  • Monophosphoryl lipid A attenuates myocardial stunning in dogs: role of ATP-sensitive potassium channels. (doximity.com)
  • Komaru T., Lamping K.G., Eastham C.L., Dellsperger K.C. Role of ATP-sensitivepotassium channels in coronary microvascular autoregulatory responses // Circulat.Res. (kiev.ua)