Katp channels. Medical search

Heteromultimers of Kir6 channels (the pore portion) and sulfonylurea receptor (the regulatory portion) which affect function of the HEART; PANCREATIC BETA CELLS; and KIDNEY COLLECTING DUCTS. KATP channel blockers include GLIBENCLAMIDE and mitiglinide whereas openers include CROMAKALIM and minoxidil sulfate.

Potassium channels where the flow of K+ ions into the cell is greater than the outward flow.

ATP-BINDING CASSETTE PROTEINS that are highly conserved and widely expressed in nature. They form an integral part of the ATP-sensitive potassium channel complex which has two intracellular nucleotide folds that bind to sulfonylureas and their analogs.

Gated, ion-selective glycoproteins that traverse membranes. The stimulus for ION CHANNEL GATING can be due to a variety of stimuli such as LIGANDS, a TRANSMEMBRANE POTENTIAL DIFFERENCE, mechanical deformation or through INTRACELLULAR SIGNALING PEPTIDES AND PROTEINS.

An antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide.

Cell membrane glycoproteins that are selectively permeable to potassium ions. At least eight major groups of K channels exist and they are made up of dozens of different subunits.

A class of drugs that act by inhibition of potassium efflux through cell membranes. Blockade of potassium channels prolongs the duration of ACTION POTENTIALS. They are used as ANTI-ARRHYTHMIA AGENTS and VASODILATOR AGENTS.

Voltage-dependent cell membrane glycoproteins selectively permeable to calcium ions. They are categorized as L-, T-, N-, P-, Q-, and R-types based on the activation and inactivation kinetics, ion specificity, and sensitivity to drugs and toxins. The L- and T-types are present throughout the cardiovascular and central nervous systems and the N-, P-, Q-, & R-types are located in neuronal tissue.

Proteins that bind specific drugs with high affinity and trigger intracellular changes influencing the behavior of cells. Drug receptors are generally thought to be receptors for some endogenous substance not otherwise specified.

10-carbon saturated monocarboxylic acids.

Organic compounds containing both the hydroxyl and carboxyl radicals.

The opening and closing of ion channels due to a stimulus. The stimulus can be a change in membrane potential (voltage-gated), drugs or chemical transmitters (ligand-gated), or a mechanical deformation. Gating is thought to involve conformational changes of the ion channel which alters selective permeability.

An adenine nucleotide containing three phosphate groups esterified to the sugar moiety. In addition to its crucial roles in metabolism adenosine triphosphate is a neurotransmitter.

A potassium-channel opening vasodilator that has been investigated in the management of hypertension. It has also been tried in patients with asthma. (Martindale, The Extra Pharmacopoeia, 30th ed, p352)

A benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group.

A guanidine that opens POTASSIUM CHANNELS producing direct peripheral vasodilatation of the ARTERIOLES. It reduces BLOOD PRESSURE and peripheral resistance and produces fluid retention. (Martindale The Extra Pharmacopoeia, 31st ed)

A family of MEMBRANE TRANSPORT PROTEINS that require ATP hydrolysis for the transport of substrates across membranes. The protein family derives its name from the ATP-binding domain found on the protein.

A class of drugs that act by selective inhibition of calcium influx through cellular membranes.

A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290)

Cell membrane glycoproteins that form channels to selectively pass chloride ions. Nonselective blockers include FENAMATES; ETHACRYNIC ACID; and TAMOXIFEN.

An electrophysiologic technique for studying cells, cell membranes, and occasionally isolated organelles. All patch-clamp methods rely on a very high-resistance seal between a micropipette and a membrane; the seal is usually attained by gentle suction. The four most common variants include on-cell patch, inside-out patch, outside-out patch, and whole-cell clamp. Patch-clamp methods are commonly used to voltage clamp, that is control the voltage across the membrane and measure current flow, but current-clamp methods, in which the current is controlled and the voltage is measured, are also used.

The study of the generation and behavior of electrical charges in living organisms particularly the nervous system and the effects of electricity on living organisms.

Potassium channel whose permeability to ions is extremely sensitive to the transmembrane potential difference. The opening of these channels is induced by the membrane depolarization of the ACTION POTENTIAL.

Long-lasting voltage-gated CALCIUM CHANNELS found in both excitable and nonexcitable tissue. They are responsible for normal myocardial and vascular smooth muscle contractility. Five subunits (alpha-1, alpha-2, beta, gamma, and delta) make up the L-type channel. The alpha-1 subunit is the binding site for calcium-based antagonists. Dihydropyridine-based calcium antagonists are used as markers for these binding sites.

The voltage differences across a membrane. For cellular membranes they are computed by subtracting the voltage measured outside the membrane from the voltage measured inside the membrane. They result from differences of inside versus outside concentration of potassium, sodium, chloride, and other ions across cells' or ORGANELLES membranes. For excitable cells, the resting membrane potentials range between -30 and -100 millivolts. Physical, chemical, or electrical stimuli can make a membrane potential more negative (hyperpolarization), or less negative (depolarization).

Potassium channels whose activation is dependent on intracellular calcium concentrations.

The excitable plasma membrane of a muscle cell. (Glick, Glossary of Biochemistry and Molecular Biology, 1990)

Exposure of myocardial tissue to brief, repeated periods of vascular occlusion in order to render the myocardium resistant to the deleterious effects of ISCHEMIA or REPERFUSION. The period of pre-exposure and the number of times the tissue is exposed to ischemia and reperfusion vary, the average being 3 to 5 minutes.

Compounds with a core of fused benzo-pyran rings.

Voltage-gated potassium channels whose primary subunits contain six transmembrane segments and form tetramers to create a pore with a voltage sensor. They are related to their founding member, shaker protein, Drosophila.

A class of drugs that act by inhibition of sodium influx through cell membranes. Blockade of sodium channels slows the rate and amplitude of initial rapid depolarization, reduces cell excitability, and reduces conduction velocity.

CALCIUM CHANNELS that are concentrated in neural tissue. Omega toxins inhibit the actions of these channels by altering their voltage dependence.

Female germ cells derived from OOGONIA and termed OOCYTES when they enter MEIOSIS. The primary oocytes begin meiosis but are arrested at the diplotene state until OVULATION at PUBERTY to give rise to haploid secondary oocytes or ova (OVUM).

The ability of a substrate to allow the passage of ELECTRONS.

The commonest and widest ranging species of the clawed "frog" (Xenopus) in Africa. This species is used extensively in research. There is now a significant population in California derived from escaped laboratory animals.

An element in the alkali group of metals with an atomic symbol K, atomic number 19, and atomic weight 39.10. It is the chief cation in the intracellular fluid of muscle and other cells. Potassium ion is a strong electrolyte that plays a significant role in the regulation of fluid volume and maintenance of the WATER-ELECTROLYTE BALANCE.

A subgroup of TRP cation channels that contain 3-4 ANKYRIN REPEAT DOMAINS and a conserved C-terminal domain. Members are highly expressed in the CENTRAL NERVOUS SYSTEM. Selectivity for calcium over sodium ranges from 0.5 to 10.

A major class of calcium activated potassium channels whose members are voltage-dependent. MaxiK channels are activated by either membrane depolarization or an increase in intracellular Ca(2+). They are key regulators of calcium and electrical signaling in a variety of tissues.

A heterogenous group of transient or low voltage activated type CALCIUM CHANNELS. They are found in cardiac myocyte membranes, the sinoatrial node, Purkinje cells of the heart and the central nervous system.

A subgroup of cyclic nucleotide-regulated ION CHANNELS within the superfamily of pore-loop cation channels. They are expressed in OLFACTORY NERVE cilia and in PHOTORECEPTOR CELLS and some PLANTS.

The muscle tissue of the HEART. It is composed of striated, involuntary muscle cells (MYOCYTES, CARDIAC) connected to form the contractile pump to generate blood flow.

A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.

A derivative of the NIACINAMIDE that is structurally combined with an organic nitrate. It is a potassium-channel opener that causes vasodilatation of arterioles and large coronary arteries. Its nitrate-like properties produce venous vasodilation through stimulation of guanylate cyclase.

Drugs used to cause dilation of the blood vessels.

A family of proton-gated sodium channels that are primarily expressed in neuronal tissue. They are AMILORIDE-sensitive and are implicated in the signaling of a variety of neurological stimuli, most notably that of pain in response to acidic conditions.

Sodium channels found on salt-reabsorbing EPITHELIAL CELLS that line the distal NEPHRON; the distal COLON; SALIVARY DUCTS; SWEAT GLANDS; and the LUNG. They are AMILORIDE-sensitive and play a critical role in the control of sodium balance, BLOOD VOLUME, and BLOOD PRESSURE.

A delayed rectifier subtype of shaker potassium channels that is the predominant VOLTAGE-GATED POTASSIUM CHANNEL of T-LYMPHOCYTES.

A family of voltage-gated potassium channels that are characterized by long N-terminal and C-terminal intracellular tails. They are named from the Drosophila protein whose mutation causes abnormal leg shaking under ether anesthesia. Their activation kinetics are dependent on extracellular MAGNESIUM and PROTON concentration.

A delayed rectifier subtype of shaker potassium channels that is selectively inhibited by a variety of SCORPION VENOMS.

A delayed rectifier subtype of shaker potassium channels that is commonly mutated in human episodic ATAXIA and MYOKYMIA.

Substances which lower blood glucose levels.

A family of iminourea derivatives. The parent compound has been isolated from mushrooms, corn germ, rice hulls, mussels, earthworms, and turnip juice. Derivatives may have antiviral and antifungal properties.

Adenosine 5'-(trihydrogen diphosphate). An adenine nucleotide containing two phosphate groups esterified to the sugar moiety at the 5'-position.

A subgroup of TRP cation channels named after melastatin protein. They have the TRP domain but lack ANKYRIN repeats. Enzyme domains in the C-terminus leads to them being called chanzymes.

An aquatic genus of the family, Pipidae, occurring in Africa and distinguished by having black horny claws on three inner hind toes.

A delayed rectifier subtype of shaker potassium channels that conducts a delayed rectifier current. It contributes to ACTION POTENTIAL repolarization of MYOCYTES in HEART ATRIA.

A family of inwardly-rectifying potassium channels that are activated by PERTUSSIS TOXIN sensitive G-PROTEIN-COUPLED RECEPTORS. GIRK potassium channels are primarily activated by the complex of GTP-BINDING PROTEIN BETA SUBUNITS and GTP-BINDING PROTEIN GAMMA SUBUNITS.

The relationship between the dose of an administered drug and the response of the organism to the drug.

Agents that increase calcium influx into calcium channels of excitable tissues. This causes vasoconstriction in VASCULAR SMOOTH MUSCLE and/or CARDIAC MUSCLE cells as well as stimulation of insulin release from pancreatic islets. Therefore, tissue-selective calcium agonists have the potential to combat cardiac failure and endocrinological disorders. They have been used primarily in experimental studies in cell and tissue culture.

A subgroup of TRP cation channels named after vanilloid receptor. They are very sensitive to TEMPERATURE and hot spicy food and CAPSAICIN. They have the TRP domain and ANKYRIN repeats. Selectivity for CALCIUM over SODIUM ranges from 3 to 100 fold.

A familial, nontransient HYPOGLYCEMIA with defects in negative feedback of GLUCOSE-regulated INSULIN release. Clinical phenotypes include HYPOGLYCEMIA; HYPERINSULINEMIA; SEIZURES; COMA; and often large BIRTH WEIGHT. Several sub-types exist with the most common, type 1, associated with mutations on an ATP-BINDING CASSETTE TRANSPORTERS (subfamily C, member 8).

Irregular microscopic structures consisting of cords of endocrine cells that are scattered throughout the PANCREAS among the exocrine acini. Each islet is surrounded by connective tissue fibers and penetrated by a network of capillaries. There are four major cell types. The most abundant beta cells (50-80%) secrete INSULIN. Alpha cells (5-20%) secrete GLUCAGON. PP cells (10-35%) secrete PANCREATIC POLYPEPTIDE. Delta cells (~5%) secrete SOMATOSTATIN.

The rate dynamics in chemical or physical systems.

Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.

The mitochondria of the myocardium.

A family of delayed rectifier voltage-gated potassium channels that share homology with their founding member, KCNQ1 PROTEIN. KCNQ potassium channels have been implicated in a variety of diseases including LONG QT SYNDROME; DEAFNESS; and EPILEPSY.

A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.

A subfamily of shaker potassium channels that shares homology with its founding member, Shab protein, Drosophila. They regulate delayed rectifier currents in the NERVOUS SYSTEM of DROSOPHILA and in the SKELETAL MUSCLE and HEART of VERTEBRATES.

A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.

A voltage-gated potassium channel that is expressed primarily in the HEART.

Abrupt changes in the membrane potential that sweep along the CELL MEMBRANE of excitable cells in response to excitation stimuli.

Established cell cultures that have the potential to propagate indefinitely.

The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.

A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.

An oral sulfonylurea hypoglycemic agent which stimulates insulin secretion.

A tricyclo bridged hydrocarbon.

Any detectable and heritable change in the genetic material that causes a change in the GENOTYPE and which is transmitted to daughter cells and to succeeding generations.

A major class of calcium-activated potassium channels that are found primarily in excitable CELLS. They play important roles in the transmission of ACTION POTENTIALS and generate a long-lasting hyperpolarization known as the slow afterhyperpolarization.

Single chains of amino acids that are the units of multimeric PROTEINS. Multimeric proteins can be composed of identical or non-identical subunits. One or more monomeric subunits may compose a protomer which itself is a subunit structure of a larger assembly.

A fast inactivating subtype of shaker potassium channels that contains two inactivation domains at its N terminus.

Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.

The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.

A broad group of eukaryotic six-transmembrane cation channels that are classified by sequence homology because their functional involvement with SENSATION is varied. They have only weak voltage sensitivity and ion selectivity. They are named after a DROSOPHILA mutant that displayed transient receptor potentials in response to light. A 25-amino-acid motif containing a TRP box (EWKFAR) just C-terminal to S6 is found in TRPC, TRPV and TRPM subgroups. ANKYRIN repeats are found in TRPC, TRPV & TRPN subgroups. Some are functionally associated with TYROSINE KINASE or TYPE C PHOSPHOLIPASES.

Pyridine moieties which are partially saturated by the addition of two hydrogen atoms in any position.

A shaker subfamily that is prominently expressed in NEURONS and are necessary for high-frequency, repetitive firing of ACTION POTENTIALS.

Striated muscle cells found in the heart. They are derived from cardiac myoblasts (MYOBLASTS, CARDIAC).

A potent direct-acting peripheral vasodilator (VASODILATOR AGENTS) that reduces peripheral resistance and produces a fall in BLOOD PRESSURE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p371)

The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM.

A shaker subfamily of potassium channels that participate in transient outward potassium currents by activating at subthreshold MEMBRANE POTENTIALS, inactivating rapidly, and recovering from inactivation quickly.

A barbiturate that is administered intravenously for the production of complete anesthesia of short duration, for the induction of general anesthesia, or for inducing a hypnotic state. (From Martindale, The Extra Pharmacopoeia, 30th ed, p919)

The nonstriated involuntary muscle tissue of blood vessels.

The physiological widening of BLOOD VESSELS by relaxing the underlying VASCULAR SMOOTH MUSCLE.

A member of the alkali group of metals. It has the atomic symbol Na, atomic number 11, and atomic weight 23.

The species Oryctolagus cuniculus, in the family Leporidae, order LAGOMORPHA. Rabbits are born in burrows, furless, and with eyes and ears closed. In contrast with HARES, rabbits have 22 chromosome pairs.

An edible species of the family Ranidae, occurring in Europe and used extensively in biomedical research. Commonly referred to as "edible frog".

A metallic element that has the atomic symbol Mg, atomic number 12, and atomic weight 24.31. It is important for the activity of many enzymes, especially those involved in OXIDATIVE PHOSPHORYLATION.

The level of protein structure in which combinations of secondary protein structures (alpha helices, beta sheets, loop regions, and motifs) pack together to form folded shapes called domains. Disulfide bridges between cysteines in two different parts of the polypeptide chain along with other interactions between the chains play a role in the formation and stabilization of tertiary structure. Small proteins usually consist of only one domain but larger proteins may contain a number of domains connected by segments of polypeptide chain which lack regular secondary structure.

Agents used for the treatment or prevention of cardiac arrhythmias. They may affect the polarization-repolarization phase of the action potential, its excitability or refractoriness, or impulse conduction or membrane responsiveness within cardiac fibers. Anti-arrhythmia agents are often classed into four main groups according to their mechanism of action: sodium channel blockade, beta-adrenergic blockade, repolarization prolongation, or calcium channel blockade.

A very slow opening and closing voltage-gated potassium channel that is expressed in NEURONS and is commonly mutated in BENIGN FAMILIAL NEONATAL CONVULSIONS.

The lower right and left chambers of the heart. The right ventricle pumps venous BLOOD into the LUNGS and the left ventricle pumps oxygenated blood into the systemic arterial circulation.

The hollow, muscular organ that maintains the circulation of the blood.

A subgroup of cyclic nucleotide-regulated ION CHANNELS of the superfamily of pore-loop cation channels that are opened by hyperpolarization rather than depolarization. The ion conducting pore passes SODIUM, CALCIUM, and POTASSIUM cations with a preference for potassium.

CALCIUM CHANNELS located within the PURKINJE CELLS of the cerebellum. They are involved in stimulation-secretion coupling of neurons.

CELL LINES derived from the CV-1 cell line by transformation with a replication origin defective mutant of SV40 VIRUS, which codes for wild type large T antigen (ANTIGENS, POLYOMAVIRUS TRANSFORMING). They are used for transfection and cloning. (The CV-1 cell line was derived from the kidney of an adult male African green monkey (CERCOPITHECUS AETHIOPS).)

Azoles of one NITROGEN and two double bonds that have aromatic chemical properties.

A class of cell surface receptors that prefer ADENOSINE to other endogenous PURINES. Purinergic P1 receptors are widespread in the body including the cardiovascular, respiratory, immune, and nervous systems. There are at least two pharmacologically distinguishable types (A1 and A2, or Ri and Ra).

A voltage-gated sodium channel subtype that mediates the sodium ion PERMEABILITY of CARDIOMYOCYTES. Defects in the SCN5A gene, which codes for the alpha subunit of this sodium channel, are associated with a variety of CARDIAC DISEASES that result from loss of sodium channel function.

A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.

A disorder of cardiac function caused by insufficient blood flow to the muscle tissue of the heart. The decreased blood flow may be due to narrowing of the coronary arteries (CORONARY ARTERY DISEASE), to obstruction by a thrombus (CORONARY THROMBOSIS), or less commonly, to diffuse narrowing of arterioles and other small vessels within the heart. Severe interruption of the blood supply to the myocardial tissue may result in necrosis of cardiac muscle (MYOCARDIAL INFARCTION).

A tetrameric calcium release channel in the SARCOPLASMIC RETICULUM membrane of SMOOTH MUSCLE CELLS, acting oppositely to SARCOPLASMIC RETICULUM CALCIUM-TRANSPORTING ATPASES. It is important in skeletal and cardiac excitation-contraction coupling and studied by using RYANODINE. Abnormalities are implicated in CARDIAC ARRHYTHMIAS and MUSCULAR DISEASES.

Compounds containing the PhCH= radical.

A very slow opening and closing voltage-gated potassium channel that is expressed in NEURONS and is closely related to KCNQ2 POTASSIUM CHANNEL. It is commonly mutated in BENIGN FAMILIAL NEONATAL CONVULSIONS.

An element of the alkaline earth group of metals. It has an atomic symbol Ba, atomic number 56, and atomic weight 138. All of its acid-soluble salts are poisonous.

Synthetic transcripts of a specific DNA molecule or fragment, made by an in vitro transcription system. This cRNA can be labeled with radioactive uracil and then used as a probe. (King & Stansfield, A Dictionary of Genetics, 4th ed)

A major class of calcium-activated potassium channels that were originally discovered in ERYTHROCYTES. They are found primarily in non-excitable CELLS and set up electrical gradients for PASSIVE ION TRANSPORT.

Elements of limited time intervals, contributing to particular results or situations.

The pore-forming subunits of large-conductance calcium-activated potassium channels. They form tetramers in CELL MEMBRANES.

A benign tumor of the PANCREATIC BETA CELLS. Insulinoma secretes excess INSULIN resulting in HYPOGLYCEMIA.

Theoretical representations that simulate the behavior or activity of biological processes or diseases. For disease models in living animals, DISEASE MODELS, ANIMAL is available. Biological models include the use of mathematical equations, computers, and other electronic equipment.

Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.

Venoms from animals of the order Scorpionida of the class Arachnida. They contain neuro- and hemotoxins, enzymes, and various other factors that may release acetylcholine and catecholamines from nerve endings. Of the several protein toxins that have been characterized, most are immunogenic.

CALCIUM CHANNELS located in the neurons of the brain.

The uptake of naked or purified DNA by CELLS, usually meaning the process as it occurs in eukaryotic cells. It is analogous to bacterial transformation (TRANSFORMATION, BACTERIAL) and both are routinely employed in GENE TRANSFER TECHNIQUES.

A voltage-gated sodium channel subtype that mediates the sodium ion permeability of excitable membranes. Defects in the SCN2A gene which codes for the alpha subunit of this sodium channel are associated with benign familial infantile seizures type 3, and early infantile epileptic encephalopathy type 11.

Damage to the MYOCARDIUM resulting from MYOCARDIAL REPERFUSION (restoration of blood flow to ischemic areas of the HEART.) Reperfusion takes place when there is spontaneous thrombolysis, THROMBOLYTIC THERAPY, collateral flow from other coronary vascular beds, or reversal of vasospasm.

A group of slow opening and closing voltage-gated potassium channels. Because of their delayed activation kinetics they play an important role in controlling ACTION POTENTIAL duration.

A 51-amino acid pancreatic hormone that plays a major role in the regulation of glucose metabolism, directly by suppressing endogenous glucose production (GLYCOGENOLYSIS; GLUCONEOGENESIS) and indirectly by suppressing GLUCAGON secretion and LIPOLYSIS. Native insulin is a globular protein comprised of a zinc-coordinated hexamer. Each insulin monomer containing two chains, A (21 residues) and B (30 residues), linked by two disulfide bonds. Insulin is used as a drug to control insulin-dependent diabetes mellitus (DIABETES MELLITUS, TYPE 1).

Carrier of aroma of butter, vinegar, coffee, and other foods.

CALCIUM CHANNELS located in the neurons of the brain. They are inhibited by the marine snail toxin, omega conotoxin MVIIC.

A technique in which tissue is rendered resistant to the deleterious effects of prolonged ISCHEMIA and REPERFUSION by prior exposure to brief, repeated periods of vascular occlusion. (Am J Physiol 1995 May;268(5 Pt 2):H2063-7, Abstract)

The parts of a macromolecule that directly participate in its specific combination with another molecule.

A toxic dye, chemically related to trinitrophenol (picric acid), used in biochemical studies of oxidative processes where it uncouples oxidative phosphorylation. It is also used as a metabolic stimulant. (Stedman, 26th ed)

A potassium-selective ion channel blocker. (From J Gen Phys 1994;104(1):173-90)

Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures.

A 37-amino acid residue peptide isolated from the scorpion Leiurus quinquestriatus hebraeus. It is a neurotoxin that inhibits calcium activated potassium channels.

The movement of ions across energy-transducing cell membranes. Transport can be active, passive or facilitated. Ions may travel by themselves (uniport), or as a group of two or more ions in the same (symport) or opposite (antiport) directions.

A primary source of energy for living organisms. It is naturally occurring and is found in fruits and other parts of plants in its free state. It is used therapeutically in fluid and nutrient replacement.

A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.

Proteins which are found in membranes including cellular and intracellular membranes. They consist of two types, peripheral and integral proteins. They include most membrane-associated enzymes, antigenic proteins, transport proteins, and drug, hormone, and lectin receptors.

The monomeric units from which DNA or RNA polymers are constructed. They consist of a purine or pyrimidine base, a pentose sugar, and a phosphate group. (From King & Stansfield, A Dictionary of Genetics, 4th ed)

Use of electric potential or currents to elicit biological responses.

Gases or volatile liquids that vary in the rate at which they induce anesthesia; potency; the degree of circulation, respiratory, or neuromuscular depression they produce; and analgesic effects. Inhalation anesthetics have advantages over intravenous agents in that the depth of anesthesia can be changed rapidly by altering the inhaled concentration. Because of their rapid elimination, any postoperative respiratory depression is of relatively short duration. (From AMA Drug Evaluations Annual, 1994, p173)

A family of membrane proteins that selectively conduct SODIUM ions due to changes in the TRANSMEMBRANE POTENTIAL DIFFERENCE. They typically have a multimeric structure with a core alpha subunit that defines the sodium channel subtype and several beta subunits that modulate sodium channel activity.

Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.

A highly poisonous compound that is an inhibitor of many metabolic processes and is used as a test reagent for the function of chemoreceptors. It is also used in many industrial processes.

A 20-carbon-chain fatty acid, unsaturated at positions 8, 11, and 14. It differs from arachidonic acid, 5,8,11,14-eicosatetraenoic acid, only at position 5.

The normality of a solution with respect to HYDROGEN ions; H+. It is related to acidity measurements in most cases by pH = log 1/2[1/(H+)], where (H+) is the hydrogen ion concentration in gram equivalents per liter of solution. (McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)

Unstable isotopes of rubidium that decay or disintegrate emitting radiation. Rb atoms with atomic weights 79-84, and 86-95 are radioactive rubidium isotopes.

A cytochrome oxidase inhibitor which is a nitridizing agent and an inhibitor of terminal oxidation. (From Merck Index, 12th ed)

Proteins prepared by recombinant DNA technology.

A group of enzymes that are dependent on CYCLIC AMP and catalyze the phosphorylation of SERINE or THREONINE residues on proteins. Included under this category are two cyclic-AMP-dependent protein kinase subtypes, each of which is defined by its subunit composition.

A family of voltage-gated eukaryotic porins that form aqueous channels. They play an essential role in mitochondrial CELL MEMBRANE PERMEABILITY, are often regulated by BCL-2 PROTO-ONCOGENE PROTEINS, and have been implicated in APOPTOSIS.

Guanosine cyclic 3',5'-(hydrogen phosphate). A guanine nucleotide containing one phosphate group which is esterified to the sugar moiety in both the 3'- and 5'-positions. It is a cellular regulatory agent and has been described as a second messenger. Its levels increase in response to a variety of hormones, including acetylcholine, insulin, and oxytocin and it has been found to activate specific protein kinases. (From Merck Index, 11th ed)

Layers of lipid molecules which are two molecules thick. Bilayer systems are frequently studied as models of biological membranes.

The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065)

Relatively complete absence of oxygen in one or more tissues.

A type of pancreatic cell representing about 50-80% of the islet cells. Beta cells secrete INSULIN.

An serine-threonine protein kinase that requires the presence of physiological concentrations of CALCIUM and membrane PHOSPHOLIPIDS. The additional presence of DIACYLGLYCEROLS markedly increases its sensitivity to both calcium and phospholipids. The sensitivity of the enzyme can also be increased by PHORBOL ESTERS and it is believed that protein kinase C is the receptor protein of tumor-promoting phorbol esters.

A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure.

Agents that affect ION PUMPS; ION CHANNELS; ABC TRANSPORTERS; and other MEMBRANE TRANSPORT PROTEINS.

Positively charged atoms, radicals or groups of atoms which travel to the cathode or negative pole during electrolysis.

Compounds of four rings containing a nitrogen. They are biosynthesized from reticuline via rearrangement of scoulerine. They are similar to BENZYLISOQUINOLINES. Members include chelerythrine and sanguinarine.

A stable, non-explosive inhalation anesthetic, relatively free from significant side effects.

A free radical gas produced endogenously by a variety of mammalian cells, synthesized from ARGININE by NITRIC OXIDE SYNTHASE. Nitric oxide is one of the ENDOTHELIUM-DEPENDENT RELAXING FACTORS released by the vascular endothelium and mediates VASODILATION. It also inhibits platelet aggregation, induces disaggregation of aggregated platelets, and inhibits platelet adhesion to the vascular endothelium. Nitric oxide activates cytosolic GUANYLATE CYCLASE and thus elevates intracellular levels of CYCLIC GMP.

A voltage-gated sodium channel subtype that mediates the sodium ion PERMEABILITY of SKELETAL MYOCYTES. Defects in the SCN4A gene, which codes for the alpha subunit of this sodium channel, are associated with several MYOTONIC DISORDERS.

A powerful vasodilator used in emergencies to lower blood pressure or to improve cardiac function. It is also an indicator for free sulfhydryl groups in proteins.

Refers to animals in the period of time just after birth.

Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.

The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.

A subtype of striated muscle, attached by TENDONS to the SKELETON. Skeletal muscles are innervated and their movement can be consciously controlled. They are also called voluntary muscles.

A flammable, poisonous gas with a characteristic odor of rotten eggs. It is used in the manufacture of chemicals, in metallurgy, and as an analytical reagent. (From Merck Index, 11th ed)

Inorganic compounds derived from hydrochloric acid that contain the Cl- ion.

An aminoperhydroquinazoline poison found mainly in the liver and ovaries of fishes in the order TETRAODONTIFORMES, which are eaten. The toxin causes paresthesia and paralysis through interference with neuromuscular conduction.

The circulation of blood through the CORONARY VESSELS of the HEART.

The study of PHYSICAL PHENOMENA and PHYSICAL PROCESSES as applied to living things.

The calcium salt of gluconic acid. The compound has a variety of uses, including its use as a calcium replenisher in hypocalcemic states.

A cell line generated from human embryonic kidney cells that were transformed with human adenovirus type 5.

A group of peptide antibiotics from BACILLUS brevis. Gramicidin C or S is a cyclic, ten-amino acid polypeptide and gramicidins A, B, D are linear. Gramicidin is one of the two principal components of TYROTHRICIN.

A family of mechanosensitive sodium channels found primarily in NEMATODES where they play a role in CELLULAR MECHANOTRANSDUCTION. Degenerin sodium channels are structurally-related to EPITHELIAL SODIUM CHANNELS and are named after the fact that loss of their activity results in cellular degeneration.

The innermost layer of the three meninges covering the brain and spinal cord. It is the fine vascular membrane that lies under the ARACHNOID and the DURA MATER.

Genetically engineered MUTAGENESIS at a specific site in the DNA molecule that introduces a base substitution, or an insertion or deletion.

A class of drugs that stimulate sodium influx through cell membrane channels.

The insertion of recombinant DNA molecules from prokaryotic and/or eukaryotic sources into a replicating vehicle, such as a plasmid or virus vector, and the introduction of the resultant hybrid molecules into recipient cells without altering the viability of those cells.

Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.

A condition of decreased oxygen content at the cellular level.

One of the POTASSIUM CHANNEL BLOCKERS, with secondary effect on calcium currents, which is used mainly as a research tool and to characterize channel subtypes.

The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments.

A highly neurotoxic polypeptide from the venom of the honey bee (Apis mellifera). It consists of 18 amino acids with two disulfide bridges and causes hyperexcitability resulting in convulsions and respiratory paralysis.

The veins and arteries of the HEART.

A neurotoxic peptide, which is a cleavage product (VIa) of the omega-Conotoxin precursor protein contained in venom from the marine snail, CONUS geographus. It is an antagonist of CALCIUM CHANNELS, N-TYPE.

RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.

An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH.

Arteries which arise from the abdominal aorta and distribute to most of the intestines.

The physical characteristics and processes of biological systems.

The characteristic 3-dimensional shape of a protein, including the secondary, supersecondary (motifs), tertiary (domains) and quaternary structure of the peptide chain. PROTEIN STRUCTURE, QUATERNARY describes the conformation assumed by multimeric proteins (aggregates of more than one polypeptide chain).

An atom or group of atoms that have a positive or negative electric charge due to a gain (negative charge) or loss (positive charge) of one or more electrons. Atoms with a positive charge are known as CATIONS; those with a negative charge are ANIONS.

A neuronal cell membrane protein that combines with SNAP-25 and SYNAPTOBREVIN 2 to form a SNARE complex that leads to EXOCYTOSIS.

Agents that have a strengthening effect on the heart or that can increase cardiac output. They may be CARDIAC GLYCOSIDES; SYMPATHOMIMETICS; or other drugs. They are used after MYOCARDIAL INFARCT; CARDIAC SURGICAL PROCEDURES; in SHOCK; or in congestive heart failure (HEART FAILURE).

The regulatory subunits of large-conductance calcium-activated potassium channels.

Two regions of sulfonylurea receptor specify the spontaneous bursting and ATP inhibition of KATP channel isoforms. (1/595)

KATP channels are heteromultimers of KIR6.2 and a sulfonylurea receptor, SUR, an ATP binding cassette (ABC) protein with several isoforms. KIR6.2 forms a channel pore whose spontaneous activity and ATP sensitivity are modulated by the receptor via an unknown interaction(s). Side by side comparison of single-channel kinetics and steady-state ATP inhibition of human beta-cell, SUR1/KIR6.2, versus cardiac, SUR2A/KIR6.2 channels demonstrate that the latter have a greater mean burst duration and open probability in the absence of nucleotides and approximately 4-fold higher IC50(ATP). We have used matched chimeras of SUR1 and SUR2A to show that the kinetics, which determine the maximal open probability (Pomax), and the ATP sensitivity are functionally separable and to identify the two segments of SUR responsible for these isoform differences. A region within the first five transmembrane domains specifies the interburst kinetics, whereas a C-terminal segment determines the sensitivity to inhibitory ATP. The separable effects of SUR on ATP inhibition and channel kinetics implies that the cytoplasmic C terminus of SUR either directly modulates the affinity of a weak ATP binding site on the inward rectifier or affects linkage between the binding site and the gate. This is the first identification of parts of an ABC protein that interact with an ion channel subunit to modulate the spontaneous activity and ATP sensitivity of the heteromeric channel. (+info)

ATP-Sensitive K+ channel modulator binding to sulfonylurea receptors SUR2A and SUR2B: opposite effects of MgADP. (2/595)

KATP channels are heteromeric complexes of inwardly rectifying K+ channel subunits and sulfonylurea receptors (SURs). SUR2A and SUR2B, which differ within the carboxyl terminal exon 38, are characteristic for the cardiac and smooth muscle type channels, respectively. Here we compare binding of the tritiated KATP channel opener, [3H]P1075, to membranes from human embryonic kidney (HEK) cells transfected with murine SUR2A and 2B at 37 degrees C. Binding to both SURs required addition of Mg2+ and ATP in the low micromolar range. In the presence of MgATP, micromolar concentrations of MgADP, formed by the ATPase activity of the membrane preparation, increased binding to SUR2A but inhibited binding to SUR2B. Decreasing temperatures strongly reduced [3H]P1075 binding to SUR2A, whereas binding to SUR2B was increased in a bell-shaped manner. Kinetic experiments revealed a faster dissociation of the [3H]P1075-SUR2A complex, whereas the association rate constants for [3H]P1075 binding to SUR2A and 2B were similar. Openers inhibited [3H]P1075 binding to SUR2A with potencies approximately 4 times lower than to SUR2B; in contrast, glibenclamide inhibited [3H]P1075 binding to SUR2A approximately 8 times more potently than to SUR2B. The data suggest that SUR2A and 2B represent the opener receptors of cardiac and vascular smooth muscle KATP channels, respectively, and show that MgADP is an important modulator of opener binding to SUR. The different carboxyl termini of SUR2A and 2B lead to differences in the MgADP dependence and the thermodynamics of [3H]P1075 binding, as well as in the affinities for openers and glibenclamide, underlining the importance of this part of the molecule for KATP channel modulator binding. (+info)

Sulfonylurea and K(+)-channel opener sensitivity of K(ATP) channels. Functional coupling of Kir6.2 and SUR1 subunits. (3/595)

The sensitivity of K(ATP) channels to high-affinity block by sulfonylureas and to stimulation by K(+) channel openers and MgADP (PCOs) is conferred by the regulatory sulfonylurea receptor (SUR) subunit, whereas ATP inhibits the channel through interaction with the inward rectifier (Kir6.2) subunit. Phosphatidylinositol 4, 5-bisphosphate (PIP(2)) profoundly antagonized ATP inhibition of K(ATP) channels expressed from cloned Kir6.2+SUR1 subunits, but also abolished high affinity tolbutamide sensitivity. By stabilizing the open state of the channel, PIP(2) drives the channel away from closed state(s) that are preferentially affected by high affinity tolbutamide binding, thereby producing an apparent loss of high affinity tolbutamide inhibition. Mutant K(ATP) channels (Kir6. 2[DeltaN30] or Kir6.2[L164A], coexpressed with SUR1) also displayed an "uncoupled" phenotype with no high affinity tolbutamide block and with intrinsically higher open state stability. Conversely, Kir6. 2[R176A]+SUR1 channels, which have an intrinsically lower open state stability, displayed a greater high affinity fraction of tolbutamide block. In addition to antagonizing high-affinity block by tolbutamide, PIP(2) also altered the stimulatory action of the PCOs, diazoxide and MgADP. With time after PIP(2) application, PCO stimulation first increased, and then subsequently decreased, probably reflecting a common pathway for activation of the channel by stimulatory PCOs and PIP(2). The net effect of increasing open state stability, either by PIP(2) or mutagenesis, is an apparent "uncoupling" of the Kir6.2 subunit from the regulatory input of SUR1, an action that can be partially reversed by screening negative charges on the membrane with poly-L-lysine. (+info)

Phosphoinositides decrease ATP sensitivity of the cardiac ATP-sensitive K(+) channel. A molecular probe for the mechanism of ATP-sensitive inhibition. (4/595)

Anionic phospholipids modulate the activity of inwardly rectifying potassium channels (Fan, Z., and J.C. Makielski. 1997. J. Biol. Chem. 272:5388-5395). The effect of phosphoinositides on adenosine triphosphate (ATP) inhibition of ATP-sensitive potassium channel (K(ATP)) currents was investigated using the inside-out patch clamp technique in cardiac myocytes and in COS-1 cells in which the cardiac isoform of the sulfonylurea receptor, SUR2, was coexpressed with the inwardly rectifying channel Kir6.2. Phosphoinositides (1 mg/ml) increased the open probability of K(ATP) in low [ATP] (1 microM) within 30 s. Phosphoinositides desensitized ATP inhibition with a longer onset period (>3 min), activating channels inhibited by ATP (1 mM). Phosphoinositides treatment for 10 min shifted the half-inhibitory [ATP] (K(i)) from 35 microM to 16 mM. At the single-channel level, increased [ATP] caused a shorter mean open time and a longer mean closed time. Phosphoinositides prolonged the mean open time, shortened the mean closed time, and weakened the [ATP] dependence of these parameters resulting in a higher open probability at any given [ATP]. The apparent rate constants for ATP binding were estimated to be 0.8 and 0.02 mM(-1) ms(-1) before and after 5-min treatment with phosphoinositides, which corresponds to a K(i) of 35 microM and 5.8 mM, respectively. Phosphoinositides failed to desensitize adenosine inhibition of K(ATP). In the presence of SUR2, phosphoinositides attenuated MgATP antagonism of ATP inhibition. Kir6.2DeltaC35, a truncated Kir6.2 that functions without SUR2, also exhibited phosphoinositide desensitization of ATP inhibition. These data suggest that (a) phosphoinositides strongly compete with ATP at a binding site residing on Kir6.2; (b) electrostatic interaction is a characteristic property of this competition; and (c) in conjunction with SUR2, phosphoinositides render additional, complex effects on ATP inhibition. We propose a model of the ATP binding site involving positively charged residues on the COOH-terminus of Kir6.2, with which phosphoinositides interact to desensitize ATP inhibition. (+info)

Role of ATP-dependent K(+) channels in the electrical excitability of early embryonic stem cell-derived cardiomyocytes. (5/595)

Single, murine embryonic stem cell-derived early stage cardiomyocytes dissociated from embryoid bodies expressed two inward rectifier K(+) channels, I(K1) and the ATP dependent K(+) current. I(K1) exhibited low density in early stage cardiomyocytes, but increased significantly in late stage cells. In contrast, the ATP dependent K(+) current was expressed at similar densities in early and late stage cardiomyocytes. This current was found to be involved in the determination of the membrane potential, since glibenclamide depolarized early cardiomyocytes and exerted a positive chronotropic effect. Some cardiomyocytes displayed a bursting behavior of action potentials, characterized by alternating periods with and without action potentials. During the phases without action potentials, the membrane potential was hyperpolarized, indicating the involvement of K(+) channels in the generation of this bursting behavior. Extracellular recording techniques were applied to spontaneously contracting areas of whole embryoid bodies. In 20% of these bursting behavior similar to that seen in the single cells was observed. In regularly beating embryoid bodies, bursting could be induced by reduction of substrates from the extracellular medium as well as by superfusion with the positive chronotropic agents Bay K 8644 or isoproterenol. Perfusion with substrate-reduced medium induced bursting behavior after a short latency, isoproterenol and Bay K 8644 resulted in a positive chronotropic response followed by bursting behavior with longer latencies. The spontaneous bursting was blocked by glibenclamide. These experimental results suggest that intermittent activation of ATP dependent K(+) channels underlies the bursting behavior observed in single cardiomyocytes and in the whole embryoid body. Conditions of metabolic stress lead to the rhythmic suppression of action potential generation. Our data indicate that ATP dependent K(+) channels play a prominent role in the cellular excitability of early cardiomyocytes. (+info)

KATP channels and 'border zone' arrhythmias: role of the repolarization dispersion between normal and ischaemic ventricular regions. (6/595)

1. In order to investigate the role of KATP channel activation and repolarization dispersion on the 'border zone' arrhythmias induced by ischaemia-reperfusion, the effects of glibenclamide and bimakalim, agents modifying action potential (AP) duration, were studied in an in vitro model of myocardial 'border zone'. 2. The electrophysiological effects of 10 microM glibenclamide and 1 microM bimakalim (n=8 each), respectively KATP channel blocker and activator, were investigated on guinea-pig ventricular strips submitted partly to normal conditions (normal zone, NZ) and partly to simulated ischaemic then reperfused conditions (altered zone, AZ). 3. By preventing the ischaemia-induced AP shortening (P<0.0001), glibenclamide reduced the dispersion of AP duration 90% (APD90) between NZ and AZ (P<0.0001), and concomitantly inhibited the 'border zone' arrhythmias induced by an extrastimulus (ES), their absence being significantly related to the lessened APD90 dispersion (chi2=8.28, P<0.01). 4. Bimakalim, which also reduced the APD90 dispersion (P<0.005) due to differential AP shortening in normal and ischaemic tissues, decreased the incidence of myocardial conduction blocks (25% of preparations versus 83% in control, n=12, P<0.05) and favoured 'border zone' spontaneous arrhythmias (75% of preparations versus 25% in control, P<0.05). 5. During reperfusion, unlike bimakalim, glibenclamide inhibited the ES-induced arrhythmias and reduced the incidence of the spontaneous ones (12% of preparations versus 92% in control, P<0.05), this latter effect being significantly related (chi2=6.13, P<0.02) to the lessened ischaemia-induced AP shortening in the presence of glibenclamide (P<0.0001). 6. These results suggest that KATP blockade may protect the ischaemic-reperfused myocardium from 'border zone' arrhythmias concomitantly with a reduction of APD90 dispersion between normal and ischaemic regions. Conversely, KATP channel activation may modify the incidence of conduction blocks and exacerbate the ischaemia-induced 'border zone' arrhythmias. (+info)

Activation of Ca(2+)-dependent K(+) channels contributes to rhythmic firing of action potentials in mouse pancreatic beta cells. (7/595)

We have applied the perforated patch whole-cell technique to beta cells within intact pancreatic islets to identify the current underlying the glucose-induced rhythmic firing of action potentials. Trains of depolarizations (to simulate glucose-induced electrical activity) resulted in the gradual (time constant: 2.3 s) development of a small (<0.8 nS) K(+) conductance. The current was dependent on Ca(2+) influx but unaffected by apamin and charybdotoxin, two blockers of Ca(2+)-activated K(+) channels, and was insensitive to tolbutamide (a blocker of ATP-regulated K(+) channels) but partially (>60%) blocked by high (10-20 mM) concentrations of tetraethylammonium. Upon cessation of electrical stimulation, the current deactivated exponentially with a time constant of 6.5 s. This is similar to the interval between two successive bursts of action potentials. We propose that this Ca(2+)-activated K(+) current plays an important role in the generation of oscillatory electrical activity in the beta cell. (+info)

(+)-[3H]isradipine and [3H]glyburide bindings to heart and lung membranes from rats with monocrotaline-induced pulmonary hypertension. (8/595)

We examined the binding of a 1,4-dihydropyridine-sensitive Ca2+ channel ligand, (+)-[3H]isradipine (PN200-110), and that of an ATP-sensitive K+ (K(ATP)) channel ligand, [3H]glyburide, to heart, lung and brain membranes isolated from Sprague-Dawley rats made pulmonary hypertensive by monocrotaline, a pyrrolizidine alkaloid. A single subcutaneous injection of monocrotaline increased right ventricular systolic pressure, a measure of pulmonary arterial pressure, and the thickness of the right ventricular free wall in 3 to 4 weeks. The (+)-[3H]PN200-110 and [3H]glyburide binding site densities (Bmax) were reduced in hypertrophied right ventricles when normalized per unit protein in comparison with those of age-matched control (sham) rats, whereas the values of the dissociation constant (Kd) of both ligands bound to the hypertrophied right ventricle were not significantly changed. The [3H]PN200-110 binding to the lung membranes of the monocrotaline-induced pulmonary hypertensive rats was increased. The results indicate that the change in the binding of 1,4-dihydropyridine Ca2+ and K(ATP) channel ligands to heart membranes may contribute to the pathological alteration of cardiopulmonary structure and functions in rats with pulmonary hypertension induced by monocrotaline. (+info)

H. Huopio1, S.-L. Shyng, T. Otonkoski3, and C. G. Nichols4 (2002-08-01). "KATP channels and insulin secretion disorders". ...

https://en.wikipedia.org/wiki/List_of_causes_of_hypoglycemia

A Promising KATP Channel Activating Agent". Cardiovascular Drug Reviews. 18: 25. doi:10.1111/j.1527-3466.2000.tb00031.x. v t e ... Bimakalim is a potassium channel opener. Puddu, Paolo Emilio; Garlid, Keith D; Monti, Francesco; Iwashiro, Katsunori; Picard, ... Potassium channel openers, 2-Pyridones, Benzopyrans, Nitriles, All stub articles, Cardiovascular system drug stubs). ...

https://en.wikipedia.org/wiki/Bimakalim

An ATP-sensitive potassium channel (or KATP channel) is a type of potassium channel that is gated by intracellular nucleotides ... and the ATP/ADP ratio determines KATP channel activity. Under resting conditions, the weakly inwardly rectifying KATP channels ... the KATP channels close, causing the membrane potential of the cell to depolarize, activating voltage-gated calcium channels, ... similar to plasma membrane KATP channels. Four genes have been identified as members of the KATP gene family. The sur1 and ...

https://en.wikipedia.org/wiki/ATP-sensitive_potassium_channel

Both genes encode in ATP sensitive potassium (KATP) channel subunits. This second gene is also located on the short arm of ... Nichols, Colin G.; Singh, Gautam K.; Grange, Dorothy K. (2013-03-29). "KATP channels and cardiovascular disease: Suddenly a ... causes inhibition of voltage-gated potassium channels and contraction of smooth muscle (in ductus). This condition can be ...

https://en.wikipedia.org/wiki/Cantú_syndrome

He was instrumental in cloning the first inward rectifier channel and the regulatory subunit of the KATP channel. He elucidated ... Koster, J.; Marshall, B.A.; Ensor, N.; Corbett, J.A.; Nichols, C.G. (2000). "Targeted Overactivity of β Cell KATP Channels ... Colin Nichols elected to Royal Society, WUSTL Newsroom 2014-06-27 Nichols, C. G. (2006). "KATP channels as molecular sensors of ... Nichol's research investigates the biology of ion channels, particularly potassium channels, and their role in diabetes ...

https://en.wikipedia.org/wiki/Colin_Nichols

Hence, the KATP channel monitors the energy balance within the cell. Depending on the tissue in which the KATP channel is ... The association of four Kir6.x and four SUR subunits form an ion conducting channel commonly referred to as the KATP channel. ... binds to the KATP channel resulting in channel closure. The relative depolarization (decrease in membrane hyperpolarization), ... Under cerebral ischemic conditions, SUR1, the regulatory subunit of the KATP and the NCCa-ATP channels, is expressed in neurons ...

https://en.wikipedia.org/wiki/Sulfonylurea_receptor

Since KATP channels only become activated during periods of low ATP and High ADP, HMR 1883 only affects hypoxic tissue and has ... Activation of the KATP channels on cardiac mitochondria is involved in ischemic preconditioning that results in protection for ... Cardioselective KATP Channel Blockers Derived from a New Series of m-Anisamidoethylbenzenesulfonylthioureas J. Med. Chem. 44 (7 ... HMR 1098 is not an SUR isotype specific inhibitor of heterologous or sarcolemmal KATP channels. J. Mol. Cell. Cardiol. 50(3): ...

https://en.wikipedia.org/wiki/HMR_1883

2004). "Syntaxin-1A inhibits cardiac KATP channels by its actions on nucleotide binding folds 1 and 2 of sulfonylurea receptor ... 2003). "Molecular basis and characteristics of KATP channel in human corporal smooth muscle cells". Int. J. Impot. Res. 15 (4 ... and its regulation of the KATP channel". Circ. Res. 102 (2): 164-76. doi:10.1161/CIRCRESAHA.107.165324. PMID 18239147. Ellis JA ... "Toward understanding the assembly and structure of KATP channels". Physiol. Rev. 78 (1): 227-45. doi:10.1152/physrev.1998.78. ...

https://en.wikipedia.org/wiki/ABCC9

It may be associated with ATP-sensitive K+ (KATP) channels. AGN 192403Moxonidine CR-4056 Phenyzoline (2-(2-phenylethyl)-4,5- ...

https://en.wikipedia.org/wiki/Imidazoline_receptor

Zhuo ML, Huang Y, Liu DP, Liang CC (April 2005). "KATP channel: relation with cell metabolism and role in the cardiovascular ... Ashford ML, Bond CT, Blair TA, Adelman JP (1996). "Cloning and functional expression of a rat heart KATP channel". Nature. 378 ... Tucker SJ, James MR, Adelman JP (July 1995). "Assignment of KATP-1, the cardiac ATP-sensitive potassium channel gene (KCNJ5), ... G protein-coupled inwardly-rectifying potassium channel Inward-rectifier potassium ion channel GRCh38: Ensembl release 89: ...

https://en.wikipedia.org/wiki/KCNJ5

Gloyn AL, Siddiqui J, Ellard S (2006). "Mutations in the genes encoding the pancreatic beta-cell KATP channel subunits Kir6.2 ( ... Kir6.2 is a major subunit of the ATP-sensitive K+ channel, a lipid-gated inward-rectifier potassium ion channel. The gene ... "Molecular cell biology of KATP channels: implications for neonatal diabetes". Expert Rev Mol Med. 9 (21): 1-17. doi:10.1017/ ... Inward-rectifier potassium ion channel Potassium channel GRCh38: Ensembl release 89: ENSG00000187486 - Ensembl, May 2017 GRCm38 ...

https://en.wikipedia.org/wiki/Kir6.2

In cardiac myocytes, caveolin-3 negatively regulates ATP-dependent potassium channels (KATP) localized in caveolae. KATP ... other isoforms of caveolin do not show this type of effect on KATP channels. The amount of KATP activation during times of ... Caveolin-3 influences the opening of L-Type calcium channels (LTCC) which play a role in cardiac myocyte contraction. ... Garg V, Sun W, Hu K (2009). "Caveolin-3 negatively regulates recombinant cardiac K(ATP) channels". Biochem. Biophys. Res. ...

https://en.wikipedia.org/wiki/Caveolin_3

... sees that channel trafficking requires KATP channels need the shielding of ER retention signal.E282K prevents the KATP channel ... is needed in KATP channel mechanism.R1215Q mutations (ABCC8 gene) affect ADP gating which in turn inhibits KATP channel. In ... Diazoxide works by opening the KATP channels of the beta cells. Octreotide must be given by injection several times a day or a ... especially those involving abnormalities of KATP channel function, can worsen or improve with time. The potential harm from ...

https://en.wikipedia.org/wiki/Congenital_hyperinsulinism

The PKC is presumably phosphorylating the KATP channel instead of ATP. The stonefish, Synanceia verrucosa, has a diverse set of ... Verrucotoxin has been studied to interact with both calcium ion channels and potassium ATP channels. The calcium ion channel is ... Wang, Jian-Wu; Yazawa, Kazuto; Hao, Li-Ying; Onoue, Yoshio; Kameyama, Masaki (June 2007). "Verrucotoxin inhibits KATP channels ... Ichthyotoxins, Potassium channel blockers, Calcium channel openers, Glycoproteins). ...

https://en.wikipedia.org/wiki/Verrucotoxin

ABCC8 is the regulatory subunit of the ATP-sensitive potassium (KATP) channel, which is located on the plasma membrane of ... This protein is thought to be an endogenous regulator of KATP channels. In vitro studies have demonstrated that this protein ... a possible regulator of sulfonylurea-sensitive KATP channel: Molecular cloning, expression and biological properties". Proc ... modulates insulin secretion through the interaction with KATP channel, and this gene has been proposed as a candidate gene for ...

https://en.wikipedia.org/wiki/ENSA_(gene)

"Titration of KATP channel expression in mammalian cells utilizing recombinant baculovirus transduction". Receptors & Channels. ... Receptors and Channels. 10 (3-4): 117-124. doi:10.1080/10606820490515012. PMID 15512846. Cheng, T; Xu, CY; Wang, YB; Chen, M; ... Receptors and Channels. 10 (3-4): 99-107. doi:10.1080/10606820490514969. PMID 15512844. Ames, Robert S; Kost, Thomas A; ...

https://en.wikipedia.org/wiki/BacMam

"Ketogenic Diet Metabolites Reduce Firing in Central Neurons by Opening KATP Channels". The Journal of Neuroscience. 27 (14): ...

https://en.wikipedia.org/wiki/Capric_acid

Sulfonylureas are effective in the KATP channel forms of neonatal-onset diabetes. The mouse model of MODY diabetes suggested ...

https://en.wikipedia.org/wiki/Maturity-onset_diabetes_of_the_young

MLC901 can activate KATP channels, which has a neuroprotective effect against brain ischemia. Neuroaid is not effective in ...

https://en.wikipedia.org/wiki/NeuroAiD

1999). "Block of human aorta Kir6.1 by the vascular KATP channel inhibitor U37883A". Br. J. Pharmacol. 128 (3): 667-672. doi: ... 2003). "Molecular basis and characteristics of KATP channel in human corporal smooth muscle cells". Int. J. Impot. Res. 15 (4 ... 2001). "Pharmacological comparison of native mitochondrial K(ATP) channels with molecularly defined surface K(ATP) channels". ... Potassium inwardly-rectifying channel, subfamily J, member 8, also known as KCNJ8, is a human gene encoding the Kir6.1 protein ...

https://en.wikipedia.org/wiki/KCNJ8

... is also the ATP-sensitive potassium channel responsible for pancreatic beta-cell insulin release. KATP (101.9 FM, "The ... 2017 101.9 The Bull KATP in the FCC FM station database KATP on Radio-Locator KATP in Nielsen Audio's FM station database ... On March 27, 2017, KATP rebranded from "Blake FM" to "101.9 The Bull". Blake FM Leave Behind a Bull in Amarillo Radioinsight - ...

https://en.wikipedia.org/wiki/KATP

"Clinical characteristics and biochemical mechanisms of congenital hyperinsulinism associated with dominant KATP channel ... FHI-GCK, caused by mutations in GCK, may be much milder than FHI-KATP; however, some persons have severe, diazoxide- ... Individuals with autosomal dominant FHI-KATP tend to be appropriate for gestational age at birth, to present at approximately ... Individuals with autosomal recessive familial hyperinsulinism, caused by mutations in either ABCC8 or KCNJ11 (FHI-KATP), tend ...

https://en.wikipedia.org/wiki/Glutamate_dehydrogenase_1

Gross ER, Hsu AK, Gross GJ (July 2007). "GSK3β inhibition and KATP channel opening mediate acute opioid-induced ...

https://en.wikipedia.org/wiki/BW373U86

"Clinical characteristics and biochemical mechanisms of congenital hyperinsulinism associated with dominant KATP channel ...

https://en.wikipedia.org/wiki/Hyperinsulinism-hyperammonemia_syndrome

Ashcroft's research focuses on ATP-sensitive potassium (KATP)channels and their role in insulin secretion. Ashcroft is working ... Ashcroft has authored a few science and popular science books based on ion channel physiology: Ion Channels and Disease: ... Ashcroft is a director of Oxion: Ion Channels and Disease Initiative, a research and training programme on integrative ion ... Dame Frances Mary Ashcroft DBE FRS FMedSci (born 1952) is a British ion channel physiologist. She is Royal Society ...

https://en.wikipedia.org/wiki/Frances_Ashcroft

"Loss of functional KATP channels in pancreatic β-cells causes persistent hyperinsulinemic hypoglycemia of infancy". Nature ...

https://en.wikipedia.org/wiki/Al_Aynsley-Green

"Ventricular fibrillation with prominent early repolarization associated with a rare variant of KCNJ8/KATP channel". Journal of ... It is thought the causing mechanism of early repolarization is a more excitable ion channel system, which causes a quicker ... October 2010). "Gain-of-function mutation S422L in the KCNJ8-encoded cardiac K(ATP) channel Kir6.1 as a pathogenic substrate ... Genes associated with ER and ATP sensitive potassium current channel mutations are KCNJ8, ABCC9 Others associated with ...

https://en.wikipedia.org/wiki/Benign_early_repolarization

KATP. Disease-associated variants of either subunit of KATP, KCNJ11 and ABCC8, can result in a channel that is "stuck open", ... NDM is not initiated by an autoimmune mechanism but mutations in KATP-sensitive channel, KCNJ11, ABCC8 and INS genes are ... all due to the presence of KATP channels in the brain. These can range from unnoticably mild to severe, and can sometimes ... People with KATP channel variations are at increased risk of developing attention deficit hyperactivity disorder, sleep ...

https://en.wikipedia.org/wiki/Neonatal_diabetes

... a possible regulator of sulfonylurea-sensitive KATP channel: molecular cloning, expression and biological properties". Proc. ...

https://en.wikipedia.org/wiki/ARPP-19

They are insulin secretagogues, triggering insulin release by inhibiting the KATP channel of the pancreatic beta cells. Eight ... By closing the potassium channels of the pancreatic beta cells, they open the calcium channels, thereby enhancing insulin ... They act on the same potassium channels as sulfonylureas, but at a different binding site. ...

https://en.wikipedia.org/wiki/Diabetes_medication

"Isolation of a cDNA clone encoding a KATP channel-like protein expressed in insulin-secreting cells, localization of the human ... G protein-coupled inwardly-rectifying potassium channel Inward-rectifier potassium ion channel GRCh38: Ensembl release 89: ... "Characterization and variation of a human inwardly-rectifying-K-channel gene (KCNJ6): a putative ATP-sensitive K-channel ... G protein-activated inward rectifier potassium channel 2 is a protein that in humans is encoded by the KCNJ6 gene. Mutation in ...

https://en.wikipedia.org/wiki/KCNJ6

June 2008). "Elimination of KATP Channels in Mouse Islets Results in Elevated U-13CGlucose Metabolism, Glutaminolysis, and ...

https://en.wikipedia.org/wiki/Pyruvate_cycling

KATP, BK, IK, CLIC5, Kv7.4 at the inner membrane and VDAC and CLIC4 as outer membrane channels. Some ion channels are ... Sodium channels Voltage-gated sodium channels (NaVs) Epithelial sodium channels (ENaCs) Calcium channels (CaVs) Proton channels ... Plasma membrane channels Examples: Voltage-gated potassium channels (Kv), Sodium channels (Nav), Calcium channels (Cav) and ... Ion channels may be classified by gating, i.e. what opens and closes the channels. For example, voltage-gated ion channels open ...

https://en.wikipedia.org/wiki/Ion_channel

KXSS, along with its sister stations KPRF-FM, KATP-FM, KMXJ-FM, and KIXZ, was acquired along with approximately fifty other ... The 96.9 frequency was, until 2008, home to a country music format as "96.9 KMML," under the ownership of Clear Channel ... Communications; however, it was one of close to 450 radio stations sold by Clear Channel in the process of privatization, ...

https://en.wikipedia.org/wiki/KXSS-FM

KATP channel closure, and the opening of voltage gated calcium channels causing insulin granule fusion and exocytosis. Voltage- ... These ATP-sensitive potassium ion channels are normally open and the calcium ion channels are normally closed. Potassium ions ... gated calcium channels and ATP-sensitive potassium ion channels are embedded in the plasma membrane of beta cells. ... The ATP-sensitive potassium ion channels close when this ratio rises. This means that potassium ions can no longer diffuse out ...

https://en.wikipedia.org/wiki/Beta_cell

... has made many significant contributions to physiology including the discovery of the KATP ion channel. "Akinori ... Noma, A. (1983). "ATP-regulated K+ channels in cardiac muscle". Nature. 305 (5930): 147-148. doi:10.1038/305147a0. PMID 6310409 ...

https://en.wikipedia.org/wiki/Akinori_Noma

Moreover, under ischemic conditions SUR1, the regulatory subunit of the KATP- and the NCCa-ATP-channels, is expressed in ... The medication works by binding to and inhibiting the ATP-sensitive potassium channels (KATP) inhibitory regulatory subunit ... Serrano-Martín X, Payares G, Mendoza-León A (December 2006). "Glibenclamide, a blocker of K+(ATP) channels, shows ... This inhibition causes cell membrane depolarization, opening voltage-dependent calcium channels.[medical citation needed] This ...

https://en.wikipedia.org/wiki/Glibenclamide

They bind to an ATP-dependent K+ (KATP) channel on the cell membrane of pancreatic beta cells in a similar manner to ... This depolarization opens voltage-gated Ca2+ channels. The rise in intracellular calcium leads to increased fusion of insulin ...

https://en.wikipedia.org/wiki/Meglitinide

Wulfkuhle, Virginia A. "KATP Field School Will Uncover New Information at Pawnee Indian Museum State Historic Site". Kansas ... from the bank's base to the present channel. The remains of over 100 earth lodges lie on the terrace between the bank and hills ...

https://en.wikipedia.org/wiki/Pike-Pawnee_Village_Site

"Exploitation of the KATP Channel Opener Diazoxide during Cardiac Surgery." During her tenure at the Washington University ...

https://en.wikipedia.org/wiki/Jennifer_S._Lawton

Kim, SJ; Lee, YJ; Kim, JB (Jan 2010). "Reduced expression and abnormal localization of the KATP channel subunit SUR2A in ... Voltage-gated sodium channel (Nav1.4) mutations are among the key causes behind periodic paralysis. Hyper-kalemic PP (hyperPP) ... The underlying mechanism of these diseases are malfunctions in the ion channels in skeletal muscle cell membranes that allow ... Imparts pH-Sensitivity in Skeletal Muscle Voltage-gated Sodium Channels". Scientific Reports. 8 (1): 13. Bibcode:2018NatSR... ...

https://en.wikipedia.org/wiki/Periodic_paralysis

... activates KATP channels in the mitochondria of the myocardium, which appears to relay the cardioprotective effects, ... Studies show that this is due to its KATP channel agonist action which causes pharmacological preconditioning and provides ... PKG acts on K+ channels to promote K+ efflux and the ensuing hyperpolarization inhibits voltage-gated calcium channels. Overall ... which is associated with increased ATP-sensitive K+ channel (KATP) opening. Nicorandil stimulates guanylate cyclase to increase ...

https://en.wikipedia.org/wiki/Nicorandil

... which codes for the Kir6.2 subunit of the beta cell KATP channel. This disease is considered to be a type of maturity onset ...

https://en.wikipedia.org/wiki/Permanent_neonatal_diabetes

KATP channel disorders) Paternal SUR1 mutation with clonal loss of heterozygosity of 11p15 Paternal Kir6.2 mutation with clonal ... loss of heterozygosity of 11p15 Diffuse hyperinsulinism KATP channel disorders SUR1 mutations Kir6.2 mutations Glucokinase gain ...

https://en.wikipedia.org/wiki/Hyperinsulinemic_hypoglycemia

Insulin signaling activates the adenosine triphosphate (ATP)-sensitive potassium (KATP) channels in the arcuate nucleus, ... channels control hepatic glucose production". Nature. 434 (7036): 1026-31. Bibcode:2005Natur.434.1026P. doi:10.1038/nature03439 ...

https://en.wikipedia.org/wiki/Vagus_nerve

... is thought to stimulate insulin secretion by closing the ATP-sensitive potassium KATP channels in pancreatic β ...

https://en.wikipedia.org/wiki/Mitiglinide

... therefore no increase in ATP concentration which is required to close the KATP channel in the beta cells of the pancreas ...

https://en.wikipedia.org/wiki/Mannoheptulose

... to predict the extent of sulphonylurea inhibition of KATP channels at therapeutic concentrations in vivo. KATP currents from ... In contrast, the free gliclazide concentration in plasma is high enough to close KATP channels and stimulate insulin secretion. ... We therefore measured the ability of gliclazide and glibenclamide to inhibit KATP channels and stimulate insulin secretion in ... In contrast, glibenclamide inhibition of recombinant KATP channels was dramatically suppressed by albumin (predicted free drug ...

https://www.neuroscience.ox.ac.uk/publications/847233

4. Thus, myocyte-KATP channels play a negligible role modulating intact in vivo cardiac contraction or arrhythmia in normal and ... 4. Thus, myocyte-KATP channels play a negligible role modulating intact in vivo cardiac contraction or arrhythmia in normal and ... 4. Thus, myocyte-KATP channels play a negligible role modulating intact in vivo cardiac contraction or arrhythmia in normal and ... Cardiomyocyte KATP channels were inhibited by HMR 1098, and data obtained under basal conditions, during epinephrine infusion ...

https://jhu.pure.elsevier.com/en/publications/effects-of-cardioselective-ksubatpsub-channel-antagonism-on-basal

K-atp channel closes and increases k+ within cell causing depolarisation and... ... What does K-ATP channel do in beta cells when ATP increases within cell? A. ... A. K-atp channel closes and increases k+ within cell causing depolarisation and insulin release. B. K-atp channel closes and ... C. K-atp channel opens and increases k+ within cell causing depolarisation and insulin release. D. K-atp channel opens and ...

https://www.usmle-forums.com/threads/what-does-k-atp-channel-do-in-beta-cells-when-atp-increases-within-cell.152682/?u=59969

Glimepiride block of Kir6.2/SUR1 Kir6.2/SUR2A and Kir6.2/SUR2A and Kir6.2/SUR2B K-ATP channels. ... Glimepiride block of Kir6.2/SUR1 Kir6.2/SUR2A and Kir6.2/SUR2A and Kir6.2/SUR2B K-ATP channels. ...

https://www.dpag.ox.ac.uk/publications/114489

... channels greatly improves postischemic myocardial recovery, the final effector mechanism for KATP channel-induced ... channels greatly improves postischemic myocardial recovery, the final effector mechanism for KATP channel-induced ... channels greatly improves postischemic myocardial recovery, the final effector mechanism for KATP channel-induced ... RhoA is a GTPase that regulates a variety of cellular processes known to be involved with KATP channel cardioprotection. Our ...

https://ohsu.pure.elsevier.com/en/publications/fasudil-prevents-ksubatpsub-channel-induced-improvement-in-postis

The KCNJ5 gene provides instructions for making a protein that functions as a potassium channel, which means that it transports ... G protein-activated inward rectifier potassium channel 4. *GIRK4. *heart KATP channel ... in the potassium channel. The altered potassium channels are less selective, allowing other ions, particularly sodium, to pass ... Potassium channels produced from the KCNJ5 gene are found in several tissues, including the adrenal glands, which are small ...

https://medlineplus.gov/genetics/gene/kcnj5/

Effect of KATP channel openers on myogenic and neurogenic responses in goat urinary bladder. Indian Journal of Experimental ... KATP-channel openers namely, cromakalim or pinacidil (10(-7) - 10(-4) M) added cumulatively, elicited a concentration-related ... Effect of KATP channel openers on myogenic and neurogenic responses in goat urinary bladder. ... Glibenclamide, a KATP-channel blocker inhibited the cromakalim-induced concentration-related relaxation of spontaneous ...

https://imsear.searo.who.int/handle/123456789/55654

The role of K ATP channels in cerebral ischemic stroke and diabetes ... Keywords: potassium channels; KATP channels; KATP channel blockers; sulfonylurea; stroke; diabetes ... KATP channels play important roles in controlling and regulating cellular functions in response to metabolic state, which are ... The role of KATP channels in cerebral ischemic stroke and diabetes Vivian SZETO1, Nai-hong CHEN2, Hong-shuo SUN1,3,4, Zhong- ...

http://www.chinaphar.com/article/view/9771

... but when Mg2+ was present ATP blocked mutant channels containing SUR1 much less than SUR2A channels. Mg-nucleotide activation ... currents through heterozygous SUR1-containing channels to a greater extent than for heterozygous SUR2A-containing channels. The ... However, despite the importance of K(ATP) channels in the heart, patients have no obvious cardiac problems. We examined the ... In the absence of Mg2+, both mutations reduced ATP inhibition of SUR1- and SUR2A-containing channels to similar extents, ...

https://www.cardioscience.ox.ac.uk/publications/113630

Ocular Hypotensive Properties and Biochemical Profile of QLS-101, a Novel ATP-Sensitive Potassium (KATP) Channel Opening ... Ocular Hypotensive Properties and Biochemical Profile of QLS-101, a Novel ATP-Sensitive Potassium (KATP) Channel Opening ...

https://qlaris.bio/publications-posters/ocular-hypotensive-properties-and-biochemical-profile-of-qls-101-a-novel-atp-sensitive-potassium-katp-channel-opening-prodrug/

KATP) channels. The authors have previously shown that isoflurane enhances sensitivity of the sarcolemmal KATP channel to the ... A possible role of the mitochondrial KATP channels was tested using a blocker of these channels, 5-hydroxydecanoate. ResultsThe ... myocytes were isolated from guinea pig hearts for the whole cell patch clamp recordings of the sarcolemmal KATP channel current ... that reactive oxygen species contribute to the mechanism by which isoflurane sensitizes the cardiac sarcolemmal KATP channel to ...

https://www.semanticscholar.org/paper/Contribution-of-Reactive-Oxygen-Species-to-of-to-An-Stadnicka/5781d3f4d6b3646f9ac2ad7c897111eb39e057ac

KATP Channels Katz Adjustment Scales use Psychiatric Status Rating Scales Kava Kava-Kava use Piper methysticum (Homeopathy) ... Kv1.6 Potassium Channel Kv3.1 Potassium Channel use Shaw Potassium Channels Kv3.2 Potassium Channel use Shaw Potassium Channels ...

https://decs.bvs.br/I/DeCS2010_Alfab-K.htm

Satake N, Shibata M. The involvement of KCa, KATP and Kv channels in vasorelaxing responses to acetylcholine in rat aortic ... The involvement of KCa, KATP and Kv channels in vasorelaxing responses to acetylcholine in rat aortic rings. / Satake, N.; ... Satake, N & Shibata, M 1997, The involvement of KCa, KATP and Kv channels in vasorelaxing responses to acetylcholine in rat ... Satake, N. ; Shibata, M. / The involvement of KCa, KATP and Kv channels in vasorelaxing responses to acetylcholine in rat ...

https://shibaura.pure.elsevier.com/en/publications/the-involvement-of-kca-katp-and-kv-channels-in-vasorelaxing-respo

Molecular basis and structural insight of vascular KATP channel gating by s-glutathionylationexternal icon. Yang Y, Shi W, Chen ...

https://www.cdc.gov/library/sciclips/issues/v3issue17.html

Hydrogen sulfide opens the KATP channel on rat atrial and ventricular myocytes. Cardiology 115, 120-126 (2010). ... Alpha lipoic acid protects the heart against myocardial post ischemia-reperfusion arrhythmias via KATP channel activation in ... Hydrogen sulfide inhibited L-type calcium channels (CaV1.2) via up-regulation of the channel sulfhydration in vascular smooth ... Interaction between hydrogen sulfide-induced sulfhydration and tyrosine nitration in the KATP channel complex. Am. J. Physiol. ...

https://www.nature.com/articles/s41569-022-00741-6?error=cookies_not_supported&code=271f9730-5002-4035-84bb-2aed32df8bd9

Novel dominant KATP channel mutations in infants with congenital hyperinsulinism: Validation by in vitro expression studies and ... Leptin-induced Trafficking of KATP Channels: A Mechanism to Regulate Pancreatic β-cell Excitability and Insulin Secretion. Int ... Mechanism of pharmacochaperoning in a mammalian KATP channel revealed by cryo-EM. Elife. 2019 Jul 25;8:e46417. ... Sung MW, Yang Z, Driggers CM, Patton BL, Mostofian B, Russo JD, Zuckerman DM, Shyng SL. Vascular KATP channel structural ...

https://www.ohsu.edu/school-of-medicine/chemical-physiology-and-biochemistry/publications

KATP binds nucleotides (Usher et al. 2021). Mitochondrial KATP channels stabilize intracellular Ca2+ during hypoxia in retinal ... KATP channels are metabolic sensors that couple cell energetics to membrane excitability. In pancreatic beta-cells, channels ... Channel closure is facilitated by ATP, which binds to the pore-forming subunit (Kir6.2). Conversely, channel opening is ... Many mutations in SUR1 render the channel unable to traffic to the cell surface, thereby reducing channel function. Many ...

https://tcdb.org/search/result.php?tc=1.A.2.1.17

Description: Vascular Kir6 (KATP) channel blocker Chemical Name: N-Cyclohexyl-N-tricyclo[3.3.1.13,7]dec-1-yl-4- ... Different molecular sites of action for the KATP channel inhibitors, PNU-99963 and PNU-37883A. Cui et al.. Br.J.Pharmacol., ... Molecular analysis of the subtype-selective inhibition of cloned KATP channels by PNU-37883A. Kovalev et al.. Br.J.Pharmacol., ... PNU 37883 hydrochloride is a novel antagonist selective for the vascular form of Kir6 (KATP) channel; inhibits Kir6 currents in ...

https://www.rndsystems.com/products/pnu-37883-hydrochloride_2095

KATP) channels have a regulatory effect on them. AIM: Investigation of the effects of KATP channel modulators,.. ... Effect of atp-sensitive potassium channel modulators on gastric lesions induced by indomethacin. *In: Academic Pharmacy Section ...

https://www.fip.org/?page=abstracts&action=favoriteadd&item=756

SUBSTRATE-DEPENDENT CHANGES IN MITOCHONDRIAL-FUNCTION, [CA-2+]I AND KATP CHANNELS IN MOUSE PANCREATIC BETA-CELLS INVITRO ...

https://ora.ox.ac.uk/?f%5Bf_contributors__name%5D%5B%5D=Duchen%2C+M&per_page=20&sort=computed__contains_full_text+desc

K-ATP ... channel ...

https://ki.se/en/research/sicof

KATP channels and insulin secretion KATP channels and insulin secretion 50 min ... a training and research programme on the integrative physiology of ion channels. ...

https://hstalks.com/expert/1876/prof-frances-mary-ashcroft/

Furthermore, GE uses the ATP-sensitive potassium (KATP) channel to sense glucose, as occurs in beta-cells. However, while KATP ... Fioramonti X, Lorsignol A, Taupignon A, Penicaud L. A new ATP-sensitive K+ channel-independent mechanism is involved in glucose ... Glucose-induced excitation of hypothalamic neurones is mediated by ATP-sensitive K+ channels. Pflugers Arch1990 Jan;415(4):479- ... channels are expressed in all GE neurons, only approximately half of VMH GE neurons express glucokinase, and approximately 30% ...

https://www.intechopen.com/chapters/44429

... channel plays a vitally important role in regulating insulin secretion and show how mutations in KATP channel genes can cause ... Add to Calendar 05/29/13 06:30 PM 05/29/13 07:30 PM United Kingdom (GMT) From bench to bedside: KATP channels and neonatal ... It will also reveal how an understanding of KATP channel function has led to a new therapy for patients with neonatal diabetes. ... Professor Ashcrofts research focuses on ion channels and their role in insulin secretion. She was awarded the Croonian Lecture ...

https://royalsociety.org/science-events-and-lectures/2013/croonian-lecture/

Ashcroft FM, Rorsman P. KATP channels and islet hormone secretion: new insights and controversies. Nat Rev Endocrinol. 2013;9( ... K+ channels. insulin secretion↑. hypoglycemia. weight gain. [100, 101, 114]. TZDs. Troglitazone/. Roziglitazone/. Pioglitazone ... Among these susceptible loci, KCNJ11 encodes the islet ATP-sensitive potassium channel Kir6.2; TCF7L2 regulates proglucagon ... Examples of candidate genes are KCNJ11 (potassium inwardly rectifying channel, subfamily J, member 11), TCF7L2 (transcription ...

https://medsci.org/v11p1185.htm

Ligand-insensitive state of cardiac ATP-sensitive K+ channels: Basis for channel opening. Alekseev, A. E., Brady, P. A. & ... KATP channel dependent heart multiome atlas. Arrell, D. K., Park, S., Yamada, S., Alekseev, A. E., Garmany, A., Jeon, R., ... KATP channel pharmacogenomics: From bench to bedside. Sattiraju, S., Reyes, S., Kane, G. C. & Terzic, A., Feb 2008, In: ... KATP channel mutation confers risk for vein of Marshall adrenergic atrial fibrillation. Olson, T. M., Alekseev, A. E., Moreau, ...

https://mayoclinic.pure.elsevier.com/en/persons/andre-terzic/publications/?type=%2Fdk%2Fatira%2Fpure%2Fresearchoutput%2Fresearchoutputtypes%2Fcontributiontojournal%2Farticle&ordering=title&descending=false&page=3

PANCREATIC BETA-CELLS; K-ATP CHANNELS; ENDOPLASMIC-RETICULUM; CA2+ CONCENTRATION; DELTA-CELLS; INSULIN; SOMATOSTATIN; RELEASE; ... a-Cell K s i m ., was decreased by small-conductance Caactivated K+ (SK) channel inhibitors apamin and UCL 1684. ... Glucose-mediated inhibition of calcium-activated potassium channels limits α-cell calcium influx and glucagon secretion ... largeconductance Ca2+-activated K+ (BK) channel inhibitor iberiotoxin (IbTx), and intermediate-conductance Ca2+-activated K+ ( ...

https://epub.uni-regensburg.de/48809/

Probing the Putative Role of KATP Channels and Biological Variability in a Mathematical Model of Chondrocyte Electrophysiology ...

https://www.mn.uio.no/ifi/english/people/aca/mariapfj/index.html

Mitochondrial KATP channels contribute to the protective effects of hydrogen sulfide against impairment of central ...

https://amedeo.com/medicine/smo/j1020.htm

KATP channel blocker; inhibits SUR1 €50.00 3503 Glipizide KATP channel blocker; inhibits SUR1 €50.00 ... KCNQ2/KCNQ3 channel opener; Anti-convulsant €80.00 3495 Ivabradine hydrochloride Selective sinus node I(f) channel inhibitor € ... Kv1.3 potassium channel blocker €110.00 3032 LUF7244 Potent negative allosteric modulator (NAM) of the Kv11.1 (hERG) channel € ... K+ channel opener (Ca2+ activated) €50.00 3019 A2764 dihydrochloride Selective inhibitor of the TRESK potassium channel €105.00 ...

https://www.axonmedchem.com/products/research-areas?endogenous_substrate=174

Recently accumulated evidence underscoring the importance of mitochondria, reactive oxygen species, and KATP channels in cardioprotective signaling by volatile anesthetics is reviewed, and current concepts and controversies regarding the specific roles of the mitochondrial and the sarcolemmal KATp channels are addressed. (semanticscholar.org)

BackgroundMyocardial protection by volatile anesthetics involves activation of cardiac adenosine triphosphate-sensitive potassium (KATP) channels. (semanticscholar.org)
Increased expression of adenosine triphosphate-sensitive K+ channels in mitral dysfunction: mechanically stimulated transcription and hypoxia-induced protein stability? (univr.it)
The aim of this study was to test whether adenosine triphosphate-sensitive K(+) (KATP) channel expression relates to mechanical and hypoxic stress within the left human heart.The KATP channels play a vital role in preserving the metabolic integrity of the stressed heart. (univr.it)

Functional effects of naturally occurring KCNJ11 mutations causing neonatal diabetes on cloned cardiac KATP channels. (ox.ac.uk)
Mutations in the pancreatic ATP-sensitive K + (K(ATP)) channel proteins sulfonylurea receptor 1 (SUR1) and Kir6.2, encoded by ABCC8 and KCNJ11, respectively, is the most common cause of the disease. (tcdb.org)
SUR2A forms cardiac and smooth muscle-type KATP channels with KCNJ11(Kir6.2) and is involved in regulation and activation. (antibodiesinc.com)
Caused in most cases by gain of channel function mutations in the KCNJ11 gene (11p15.1), encoding a subunit of the ATP-sensitive potassium (KATP) channel. (cdc.gov)

We used this data, together with estimates of free drug concentrations from binding studies, to predict the extent of sulphonylurea inhibition of KATP channels at therapeutic concentrations in vivo. (ox.ac.uk)
1. Inhibition of cardiomyocyte-specific ATP-sensitive potassium (K ATP ) channels prolongs the action potential during intense ischaemia with attendant antiarrhythmic effects. (elsevier.com)
KATP-channel openers namely, cromakalim or pinacidil (10(-7) - 10(-4) M) added cumulatively, elicited a concentration-related inhibition of both amplitude and rate of spontaneous contractions. (who.int)
In the absence of Mg2+, both mutations reduced ATP inhibition of SUR1- and SUR2A-containing channels to similar extents, but when Mg2+ was present ATP blocked mutant channels containing SUR1 much less than SUR2A channels. (ox.ac.uk)
Conversely, channel opening is potentiated by phosphoinositol bisphosphate (PIP 2 ), which binds to Kir6.2 and reduces channel inhibition by ATP. (tcdb.org)
Molecular analysis of the subtype-selective inhibition of cloned K ATP channels by PNU-37883A. (rndsystems.com)
Although apamin transiently increased Ca2+ influx into a-cells at low glucose (42.9 +/- 10.6%), sustained SK (38.5 +/- 10.4%) or BK channel inhibition (31.0 +/- 11.7%) decreased alpha-cell Ca2+ influx. (uni-regensburg.de)
Total alpha-cell Ca-c(2+) was similarly reduced (28.3 +/- 11.1%) following prolonged treatment with high glucose, but it was not decreased further by SK or BK channel inhibition. (uni-regensburg.de)

Sulphonylurea drugs stimulate insulin secretion from pancreatic β-cells primarily by inhibiting ATP sensitive potassium (KATP) channels in the β-cell membrane. (ox.ac.uk)
We therefore measured the ability of gliclazide and glibenclamide to inhibit KATP channels and stimulate insulin secretion in the presence of serum albumin. (ox.ac.uk)
In contrast, the free gliclazide concentration in plasma is high enough to close KATP channels and stimulate insulin secretion. (ox.ac.uk)
K ATP channels mediate insulin secretion in pancreatic islet beta cells, and controlling vascular tone. (chinaphar.com)
In pancreatic beta-cells, channels formed by SUR1 and Kir6.2 regulate insulin secretion and are the targets of antidiabetic sulfonylureas. (tcdb.org)
This lecture will describe how a membrane protein pore known as the ATP-sensitive potassium (KATP) channel plays a vitally important role in regulating insulin secretion and show how mutations in KATP channel genes can cause neonatal diabetes, a rare genetic form of diabetes that develops soon after birth, and occasionally also developmental problems. (royalsociety.org)
Professor Ashcroft's research focuses on ion channels and their role in insulin secretion. (royalsociety.org)
She was awarded the Croonian Lecture for outstanding work on the link between glucose metabolism and insulin secretion, and the key role and mechanism of action of the ATP-sensitive potassium channel, and its role in neonatal diabetes. (royalsociety.org)
We examined this idea for 3 ADs: paroxetine, clomipramine and, with particular emphasis, fluoxetine, on insulin secretion, mitochondrial function, cellular bioenergetics, KATP channel activity, and caspase activity in murine and human cell-line models of pancreatic β-cells. (nottingham.ac.uk)

KCNJ5 gene mutations associated with this condition change single protein building blocks (amino acids) in the potassium channel. (medlineplus.gov)
As in aldosterone-producing adenomas (described above), KCNJ5 gene mutations result in production of less-selective potassium channels. (medlineplus.gov)
K+ channel mutations in adrenal aldosterone-producing adenomas and hereditary hypertension. (medlineplus.gov)
A Meta-Analysis of Somatic KCNJ5 K(+) Channel Mutations In 1636 Patients With an Aldosterone-Producing Adenoma. (medlineplus.gov)
Both mutations also increased resting whole-cell K(ATP) currents through heterozygous SUR1-containing channels to a greater extent than for heterozygous SUR2A-containing channels. (ox.ac.uk)
Many mutations in SUR1 render the channel unable to traffic to the cell surface, thereby reducing channel function. (tcdb.org)
predominance of recessive KATP channel mutations. (cdc.gov)
Investigations into the molecular basis of CHI have led to the discovery of mutations in the sulfonylurea receptor and an inwardly rectifying potassium channel. (medscape.com)

Glimepiride block of Kir6.2/SUR1 Kir6.2/SUR2A and Kir6.2/SUR2A and Kir6.2/SUR2B K-ATP channels. (ox.ac.uk)
ATP-sensitive K+ (K(ATP)) channels are hetero-octamers of inwardly rectifying K+ channel (Kir6.2) and sulphonylurea receptor subunits (SUR1 in pancreatic beta-cells, SUR2A in heart). (ox.ac.uk)
We examined the effects of adenine nucleotides on K(ATP) channels containing wild-type or mutant (Q52R, R201H) Kir6.2 plus either SUR1 or SUR2A. (ox.ac.uk)
Kir6.2 is an ATP-sensitive potassium (K ATP ) channel coupling cell metabolism to electrical activity by regulating K + fluxes across the plasma membrane. (tcdb.org)
Channel closure is facilitated by ATP, which binds to the pore-forming subunit (Kir6.2). (tcdb.org)
a cryo-EM structure of a hamster SUR1/rat Kir6.2 channel bound to a high-affinity sulfonylurea drug glibenclamide and ATP has been solved at 3.63 Å resolution. (tcdb.org)
Pharmacological inhibitors and ATP enrich a channel conformation in which the Kir6.2 cytoplasmic domain is closely associated with the transmembrane domain, while depleting one where the Kir6.2 cytoplasmic domain is extended away into the cytoplasm. (tcdb.org)
The structures resolved key contacts between the distal N-terminus of Kir6.2 and SUR1's ABC module involving residues implicated in channel function and showed a SUR1 residue, K134, participates in PIP2 binding. (tcdb.org)
Proteins and messenger ribonucleic acids (mRNAs) of KATP pore subunits and mRNAs of their known transcriptional regulators (forkhead box [FOX] F2, FOXO1, FOXO3, and hypoxia inducible factor [HIF]-1α) were measured respectively by Western blotting, immunohistochemistry, and quantitative real-time polymerase chain reaction, and submitted to statistical analysis.In all heart chambers, Kir6.2 mRNA correlated with HIF-1α mRNA. (univr.it)
Overlapping distribution of K-ATP channel-forming Kir6.2 subunit and the sulfonylurea receptor SUR1 in rodent brain. (mpg.de)

Glibenclamide, a KATP-channel blocker inhibited the cromakalim-induced concentration-related relaxation of spontaneous contractions with a significant increase in its mean IC50. (who.int)
The present results suggest that in the goat detrusor muscle, agonist and EFS-induced contractile responses were more potently inhibited by cromakalim than pinacidil with activation of glibenclamide sensitive KATP channels. (who.int)

Omega-3-polyunsaturated fatty acids (PUFA), which can suppress cardiac myocyte electrical activity, may also reduce ion channel activity in insulin-secreting cells. (cyberleninka.org)

The KCNJ5 gene provides instructions for making a protein that functions as a potassium channel, which means that it transports positively charged atoms (ions) of potassium (K + ) into and out of cells. (medlineplus.gov)
Redox modulation of vascular tone: focus of potassium channel mechanisms of dilation. (semanticscholar.org)
The effect of ROS on potassium channel function in the vasculature is reviewed and discerning the activity of enzymes regulating production or degradation of ROS is important when assessing tissue perfusion in health and disease. (semanticscholar.org)
This review highlights the most recent and interesting articles on the physiologic properties and functions of ATP-dependent potassium channels in the cardiovascular system and on the role of the potassium channel openers for the treatment of cardiovascular dysfunction. (semanticscholar.org)

AMPA receptors (AMPARs) are glutamate-gated ion channels that mediate the majority of fast excitatory synaptic transmission throughout the brain. (uib.no)

KATP currents from mouse pancreatic β-cells and Xenopus oocytes were measured using the patch-clamp technique. (ox.ac.uk)
Bovine serum albumin (60g/l) produced a mild, non-significant reduction of gliclazide block of KATP currents in pancreatic β-cells and Xenopus oocytes. (ox.ac.uk)
alpha-Cells displayed K-SLOW, currents that were dependent on Ca2+ influx through L- and P/Q-type voltage-dependent Ca2+ channels (VDCCs) as well as Ca2+ released from endoplasmic reticulum stores. (uni-regensburg.de)

K ATP channel is a hetero-octameric complex, consisting of four pore-forming Kir6.x and four regulatory sulfonylurea receptor SURx subunits. (chinaphar.com)
Expression pattern in brain of TASK-1, TASK-3, and a tandem pore domain K+ channel subunit, TASK-5, associated with the central auditory nervous system. (mpg.de)
Kir6.1 is the principal pore-forming subunit of astrocyte but not neuronal plasma membrane K-ATP channels. (mpg.de)

These subunits are differentially expressed in various cell types, thus determining the sensitivity of the cells to specific channel modifiers. (chinaphar.com)
Ontogeny of gene expression of Kir channel subunits in the rat. (mpg.de)

Mg-nucleotide activation of SUR1, but not SUR2A, channels was markedly increased by the R201H mutation. (ox.ac.uk)

Four groups of perfused rat hearts were subjected to 36 min of zero-flow ischemia and 44 min of reperfusion with continuous measurements of mechanical function and 31 P NMR high-energy phosphate data: 1) untreated, 2) pinacidil (10 μM) to activate K ATP channels, 3) fasudil (15 μM) to inhibit ROCK, and 4) both fasudil and pinacidil. (elsevier.com)
The authors have previously shown that isoflurane enhances sensitivity of the sarcolemmal KATP channel to the opener, pinacidil. (semanticscholar.org)

Whereas activation of ATP-dependent potassium (K ATP ) channels greatly improves postischemic myocardial recovery, the final effector mechanism for K ATP channel-induced cardioprotection remains elusive. (elsevier.com)

A G-protein-activated inwardly rectifying K+ channel (GIRK4) from human hippocampus associates with other GIRK channels. (mpg.de)

It will also reveal how an understanding of KATP channel function has led to a new therapy for patients with neonatal diabetes. (royalsociety.org)

Distribution of inwardly rectifying potassium channels in the brain. (mpg.de)
Ontogeny of inwardly K + channel expression in the rat. (mpg.de)
Distribution and localization of a G protein-coupled inwardly rectifying K+ channel in the rat. (mpg.de)

Neither fluoxetine, antimycin nor rotenone could reactivate KATP channel activity blocked by glucose unlike the mitochondrial uncoupler, FCCP. (nottingham.ac.uk)
The extracellular glucose concentration monitors the gating of KATP channels of sleep-promoting neurons, highlighting that these neurons can adapt their excitability according to the extracellular energy status… Glucose-induced excitation of sleep-promoting VLPO neurons should therefore be involved in the drowsiness that one feels after a high-sugar meal. (drsharma.ca)

Mechanical effects of selective myocyte K ATP channel blockade on basal, β-adrenergic stimulated, and ischemic responses were therefore tested in dogs with cardiac failure induced by tachypacing. (elsevier.com)
In this review, we discussed the potential effects of K ATP channel blockers when used under pathological conditions related to diabetics and cerebral ischemic stroke. (chinaphar.com)

Cardiomyocyte K ATP channels were inhibited by HMR 1098, and data obtained under basal conditions, during epinephrine infusion to raise metabolic demand, during regional ischaemia, and with combined ischaemia + epinephrine. (elsevier.com)
4. Thus, myocyte-K ATP channels play a negligible role modulating intact in vivo cardiac contraction or arrhythmia in normal and failing heart with and without increased metabolic demand and/or regional ischaemia. (elsevier.com)
KATP channels play important roles in controlling and regulating cellular functions in response to metabolic state, which are inhibited by ATP and activated by Mg-ADP, allowing the cell to couple cellular metabolic state (ATP/ADP ratio) to electrical activity of the cell membrane. (chinaphar.com)
KATP channels are metabolic sensors that couple cell energetics to membrane excitability. (tcdb.org)

The altered potassium channels are less selective, allowing other ions, particularly sodium, to pass through. (medlineplus.gov)

IMSEAR at SEARO: Effect of KATP channel openers on myogenic and neurogenic responses in goat urinary bladder. (who.int)

Under pathophysiological conditions, K ATP channels play cytoprotective role in cardiac myocytes and neurons during ischemia and/ or hypoxia. (chinaphar.com)
Knowlton C, Kutterer S, Roeper J, Canavier CC (2018) Calcium dynamics control K-ATP channel-mediated bursting in substantia nigra dopamine neurons: a combined experimental and modeling study. (yale.edu)

RhoA is a GTPase that regulates a variety of cellular processes known to be involved with K ATP channel cardioprotection. (elsevier.com)

Mitochondrial KATP channels stabilize intracellular Ca 2+ during hypoxia in retinal horizontal cells of goldfish ( Carassius auratus ) ( Country and Jonz 2021 ). (tcdb.org)

Different molecular sites of action for the K ATP channel inhibitors, PNU-99963 and PNU-37883A. (rndsystems.com)
a-Cell K s i m ., was decreased by small-conductance Ca'activated K+ (SK) channel inhibitors apamin and UCL 1684. (uni-regensburg.de)

She is the Royal Society GlaxoSmithKline Research Professor, a Fellow of Trinity College, Oxford and Director of OXION, a training and research programme on the integrative physiology of ion channels. (hstalks.com)

and protein kinasing C- ϵ can modulate the channel function. (semanticscholar.org)
Exogenously administered B-type natriuretic peptide (BNP) has been shown to offer cardioprotection through activation of particulate guanylyl cyclase (pGC), protein kinase G (PKG) and KATP channel opening. (uib.no)
Brain localization and behavioral impact of the G-protein-gated K + channel subunit GIRK 4. (mpg.de)

ATP-sensitive potassium (K ATP ) channels are ubiquitously expressed on the plasma membrane of cells in multiple organs, including the heart, pancreas and brain. (chinaphar.com)

Satake, N & Shibata, M 1997, ' The involvement of KCa, KATP and Kv channels in vasorelaxing responses to acetylcholine in rat aortic rings ', Gen Pharmacol , vol. 28, pp. 453-457. (elsevier.com)

2012), ' Heterogeneity of ATP-sensitive K+ channels in cardiac myocytes: enrichment at the intercalated disk. . (antibodiesinc.com)

Isoflurane prevents experimental TCM and preserves LV function, an effect not mediated via opening of K-ATP channels. (biomedcentral.com)
The syndrome is caused by changes in the structure and function of certain cardiac ion channels and reduced expression of Connexin 43 (Cx43) in the Right Ventricle (RV), predominantly in the Right Ventricular Outflow Tract (VSVD), causing electromechanical abnormalities. (bvsalud.org)

Binding of sulphonylureas to plasma proteins - A KATP channel perspective. (ox.ac.uk)

The flow of sodium ions into adrenal gland cells affects the electrical charge across the cell membrane, activating another type of channel that allows calcium ions to enter. (medlineplus.gov)

These data support the hypothesis that ROCK activity plays a role in K ATP channel-induced cardioprotection. (elsevier.com)
Probing the Putative Role of KATP Channels and Biological Variability in a Mathematical Model of Chondrocyte Electrophysiology. (uio.no)

What does K-ATP channel do in beta cells when ATP increases within cell? (usmle-forums.com)

The effect of isoflurane on vascular KATP channels and compare it with that on cardiac K ATP channels is examined to examine the effect of the drug on vasodilatation in animals and humans. (semanticscholar.org)
It seems probable that ATP-sensitive potassium (KATP) channels have a regulatory effect on them. (fip.org)

Our goal was to determine whether the activity of a key rhoA effector, rho kinase (ROCK), is required for K ATP channel-induced cardioprotection. (elsevier.com)

However, despite the importance of K(ATP) channels in the heart, patients have no obvious cardiac problems. (ox.ac.uk)

HN - 2008 MH - Superior Sagittal Sinus UI - D054063 MN - A07.231.908.224.667 MS - The long large endothelium-lined venous channel on the top outer surface of the brain. (bvsalud.org)

Potassium channels produced from the KCNJ5 gene are found in several tissues, including the adrenal glands, which are small hormone-producing glands located on top of each kidney. (medlineplus.gov)

Anatomy27

Organisms14

Diseases5

Chemicals and Drugs161

Analytical, Diagnostic and Therapeutic Techniques and Equipment13

Phenomena and Processes30

Disciplines and Occupations2

Technology, Industry, Agriculture1

Information Science2

Two regions of sulfonylurea receptor specify the spontaneous bursting and ATP inhibition of KATP channel isoforms. (1/595)

ATP-Sensitive K+ channel modulator binding to sulfonylurea receptors SUR2A and SUR2B: opposite effects of MgADP. (2/595)

Sulfonylurea and K(+)-channel opener sensitivity of K(ATP) channels. Functional coupling of Kir6.2 and SUR1 subunits. (3/595)

Phosphoinositides decrease ATP sensitivity of the cardiac ATP-sensitive K(+) channel. A molecular probe for the mechanism of ATP-sensitive inhibition. (4/595)

Role of ATP-dependent K(+) channels in the electrical excitability of early embryonic stem cell-derived cardiomyocytes. (5/595)

KATP channels and 'border zone' arrhythmias: role of the repolarization dispersion between normal and ischaemic ventricular regions. (6/595)

Activation of Ca(2+)-dependent K(+) channels contributes to rhythmic firing of action potentials in mouse pancreatic beta cells. (7/595)

(+)-[3H]isradipine and [3H]glyburide bindings to heart and lung membranes from rats with monocrotaline-induced pulmonary hypertension. (8/595)

KATP Channels

Potassium Channels, Inwardly Rectifying

Sulfonylurea Receptors

Ion Channels

Glyburide

Potassium Channels

Potassium Channel Blockers

Calcium Channels

Receptors, Drug

Decanoic Acids

Hydroxy Acids

Ion Channel Gating

Adenosine Triphosphate

Cromakalim

Diazoxide

Pinacidil

ATP-Binding Cassette Transporters

Calcium Channel Blockers

Tolbutamide

Chloride Channels

Patch-Clamp Techniques

Electrophysiology

Potassium Channels, Voltage-Gated

Calcium Channels, L-Type

Sulfonylurea Compounds

Membrane Potentials

Potassium Channels, Calcium-Activated

Sarcolemma

Ischemic Preconditioning, Myocardial

Benzopyrans

Shaker Superfamily of Potassium Channels

Sodium Channel Blockers

Calcium Channels, N-Type

Oocytes

Electric Conductivity

Xenopus laevis

Potassium

TRPC Cation Channels

Large-Conductance Calcium-Activated Potassium Channels

Calcium Channels, T-Type

Cyclic Nucleotide-Gated Cation Channels

Myocardium

Rats, Sprague-Dawley

Nicorandil

Vasodilator Agents

Acid Sensing Ion Channels

Epithelial Sodium Channels

Kv1.3 Potassium Channel

Ether-A-Go-Go Potassium Channels

Kv1.2 Potassium Channel

Kv1.1 Potassium Channel

Hypoglycemic Agents

Guanidines

Adenosine Diphosphate

TRPM Cation Channels

Xenopus

Kv1.5 Potassium Channel

G Protein-Coupled Inwardly-Rectifying Potassium Channels

Dose-Response Relationship, Drug

Calcium Channel Agonists

TRPV Cation Channels

Congenital Hyperinsulinism

Islets of Langerhans

Kinetics

Cells, Cultured

Mitochondria, Heart

KCNQ Potassium Channels

Calcium

Shab Potassium Channels

Guinea Pigs

KCNQ1 Potassium Channel

Action Potentials

Cell Line

Cell Membrane

Rats, Wistar

Gliclazide

Adamantane

Mutation

Small-Conductance Calcium-Activated Potassium Channels

Protein Subunits