Ion channels that specifically allow the passage of SODIUM ions. A variety of specific sodium channel subtypes are involved in serving specialized functions such as neuronal signaling, CARDIAC MUSCLE contraction, and KIDNEY function.
A voltage-gated sodium channel subtype found widely expressed in neurons of the central and peripheral nervous systems. Defects in the SCN8A gene which codes for the alpha subunit of this sodium channel are associated with ATAXIA and cognitive deficits.
A voltage-gated sodium channel subtype that is expressed in nociceptors, including spinal and trigeminal sensory neurons. It plays a role in the transmission of pain signals induced by cold, heat, and mechanical stimuli.
A voltage-gated sodium channel subtype found widely expressed in nociceptive primary sensory neurons. Defects in the SCN9A gene, which codes for the alpha subunit of this sodium channel, are associated with several pain sensation-related disorders.
A voltage-gated sodium channel subtype found in neuronal tissue that mediates the sodium ion PERMEABILITY of excitable membranes.
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 voltage-gated sodium channel subtype found in the neurons of the NERVOUS SYSTEM and DORSAL ROOT GANGLIA. It may play a role in the generation of heat and mechanical pain hypersensitivity.
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.
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.
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.
A member of the alkali group of metals. It has the atomic symbol Na, atomic number 11, and atomic weight 23.
A voltage-gated sodium channel subtype that is predominantly expressed in the CENTRAL NERVOUS SYSTEM. Defects in the SCN1A gene which codes for the alpha subunit of this sodium channel are associated with DRAVET SYNDROME, generalized epilepsy with febrile seizures plus, type 2 (GEFS+2), and familial hemiplegic migraine type 3.
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.
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.
A peripheral arterial disease that is characterized by the triad of ERYTHEMA, burning PAIN, and increased SKIN TEMPERATURE of the extremities (or red, painful extremities). Erythromelalgia may be classified as primary or idiopathic, familial or non-familial. Secondary erythromelalgia is associated with other diseases, the most common being MYELOPROLIFERATIVE DISORDERS.
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.
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.
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.
Sensory ganglia located on the dorsal spinal roots within the vertebral column. The spinal ganglion cells are pseudounipolar. The single primary branch bifurcates sending a peripheral process to carry sensory information from the periphery and a central branch which relays that information to the spinal cord or brain.
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.
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 class of drugs that stimulate sodium influx through cell membrane channels.
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.
A compound that contains a reduced purine ring system but is not biosynthetically related to the purine alkaloids. It is a poison found in certain edible mollusks at certain times; elaborated by GONYAULAX and consumed by mollusks, fishes, etc. without ill effects. It is neurotoxic and causes RESPIRATORY PARALYSIS and other effects in MAMMALS, known as paralytic SHELLFISH poisoning.
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).
Abrupt changes in the membrane potential that sweep along the CELL MEMBRANE of excitable cells in response to excitation stimuli.
Potassium channels where the flow of K+ ions into the cell is greater than the outward flow.
A group of proteins that associate with DYSTROPHIN at the CELL MEMBRANE to form the DYSTROPHIN-ASSOCIATED PROTEIN COMPLEX.
Batrachotoxin is the 20-alpha-bromobenzoate of batrachotoxin A; they are toxins from the venom of a small Colombian frog, Phyllobates aurotaenia, cause release of acetylcholine, destruction of synaptic vesicles and depolarization of nerve and muscle fibers.
A class of drugs that act by selective inhibition of calcium influx through cellular membranes.
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.
The protein constituents of muscle, the major ones being ACTINS and MYOSINS. More than a dozen accessory proteins exist including TROPONIN; TROPOMYOSIN; and DYSTROPHIN.
A class of drugs that inhibit the activation of VOLTAGE-GATED SODIUM CHANNELS.
Cell membrane glycoproteins that form channels to selectively pass chloride ions. Nonselective blockers include FENAMATES; ETHACRYNIC ACID; and TAMOXIFEN.
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.
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.
The ability of a substrate to allow the passage of ELECTRONS.
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.
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).
A benzoate-cevane found in VERATRUM and Schoenocaulon. It activates SODIUM CHANNELS to stay open longer than normal.
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.
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.
A voltage-gated sodium channel beta subunit abundantly expressed in SKELETAL MUSCLE; HEART; and BRAIN. It non-covalently associates with voltage-gated alpha subunits. Defects in the SCN1B gene, which codes for this beta subunit, are associated with generalized epilepsy with febrile seizures plus, type 1, and Brugada syndrome 5.
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.
Different forms of a protein that may be produced from different GENES, or from the same gene by ALTERNATIVE SPLICING.
A subclass of sodium channel blockers that are specific for EPITHELIAL SODIUM CHANNELS.
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.
A pyrazine compound inhibiting SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS. This inhibition creates a negative potential in the luminal membranes of principal cells, located in the distal convoluted tubule and collecting duct. Negative potential reduces secretion of potassium and hydrogen ions. Amiloride is used in conjunction with DIURETICS to spare POTASSIUM loss. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p705)
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.
An aquatic genus of the family, Pipidae, occurring in Africa and distinguished by having black horny claws on three inner hind toes.
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.
Potassium channels whose activation is dependent on intracellular calcium concentrations.
The rate dynamics in chemical or physical systems.
A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Its actions are more intense and its effects more prolonged than those of PROCAINE but its duration of action is shorter than that of BUPIVACAINE or PRILOCAINE.
A voltage-gated sodium channel beta subunit subtype that non-covalently associates with voltage-gated alpha subunits. Defects in the SCN3B gene which codes for this beta subunit are associated with Brugada syndrome 7.
Regularly spaced gaps in the myelin sheaths of peripheral axons. Ranvier's nodes allow saltatory conduction, that is, jumping of impulses from node to node, which is faster and more energetically favorable than continuous conduction.
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.
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.
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.
CALCIUM CHANNELS that are concentrated in neural tissue. Omega toxins inhibit the actions of these channels by altering their voltage dependence.
A tumor made up of nerve cells and nerve fibers. (Dorland, 27th ed)
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.
The active insecticidal constituent of CHRYSANTHEMUM CINERARIIFOLIUM flowers. Pyrethrin I is the pyretholone ester of chrysanthemummonocarboxylic acid and pyrethrin II is the pyretholone ester of chrysanthemumdicarboxylic acid monomethyl ester.
Antiarrhythmic agent pharmacologically similar to LIDOCAINE. It may have some anticonvulsant properties.
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.
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 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.
A delayed rectifier subtype of shaker potassium channels that is selectively inhibited by a variety of SCORPION VENOMS.
A voltage-gated sodium channel beta subunit that binds covalently to voltage-gated alpha subunits.
A voltage-gated sodium channel beta subunit subtype that covalently associates with voltage-gated alpha subunits. Defects in the SCN4B gene, which codes for this beta subunit, are associated with long QT syndrome-10.
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.
Peptide neurotoxins from the marine fish-hunting snails of the genus CONUS. They contain 13 to 29 amino acids which are strongly basic and are highly cross-linked by disulfide bonds. There are three types of conotoxins, omega-, alpha-, and mu-. OMEGA-CONOTOXINS inhibit voltage-activated entry of calcium into the presynaptic membrane and therefore the release of ACETYLCHOLINE. Alpha-conotoxins inhibit the postsynaptic acetylcholine receptor. Mu-conotoxins prevent the generation of muscle action potentials. (From Concise Encyclopedia Biochemistry and Molecular Biology, 3rd ed)
Insects of the order Dictyoptera comprising several families including Blaberidae, BLATTELLIDAE, Blattidae (containing the American cockroach PERIPLANETA americana), Cryptocercidae, and Polyphagidae.
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 superorder of CEPHALOPODS comprised of squid, cuttlefish, and their relatives. Their distinguishing feature is the modification of their fourth pair of arms into tentacles, resulting in 10 limbs.
Arthropods of the order Scorpiones, of which 1500 to 2000 species have been described. The most common live in tropical or subtropical areas. They are nocturnal and feed principally on insects and other arthropods. They are large arachnids but do not attack man spontaneously. They have a venomous sting. Their medical significance varies considerably and is dependent on their habits and venom potency rather than on their size. At most, the sting is equivalent to that of a hornet but certain species possess a highly toxic venom potentially fatal to humans. (From Dorland, 27th ed; Smith, Insects and Other Arthropods of Medical Importance, 1973, p417; Barnes, Invertebrate Zoology, 5th ed, p503)
Nerve fibers that are capable of rapidly conducting impulses away from the neuron cell body.
The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.
The relationship between the dose of an administered drug and the response of the organism to the drug.
Compounds that either stimulate the opening or prevent closure of EPITHELIAL SODIUM ION CHANNELS.
Sodium or sodium compounds used in foods or as a food. The most frequently used compounds are sodium chloride or sodium glutamate.
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.
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.
Toxic substances from microorganisms, plants or animals that interfere with the functions of the nervous system. Most venoms contain neurotoxic substances. Myotoxins are included in this concept.
Established cell cultures that have the potential to propagate indefinitely.
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 delayed rectifier subtype of shaker potassium channels that is commonly mutated in human episodic ATAXIA and MYOKYMIA.
A delayed rectifier subtype of shaker potassium channels that is the predominant VOLTAGE-GATED POTASSIUM CHANNEL of T-LYMPHOCYTES.
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 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 ubiquitous sodium salt that is commonly used to season food.
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.
Compounds based on an 8-membered heterocyclic ring including an oxygen. They can be considered medium ring ethers.
Prolonged failure of muscle relaxation after contraction. This may occur after voluntary contractions, muscle percussion, or electrical stimulation of the muscle. Myotonia is a characteristic feature of MYOTONIC DISORDERS.
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.
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.
A voltage-gated potassium channel that is expressed primarily in the HEART.
Toxic or poisonous substances elaborated by marine flora or fauna. They include also specific, characterized poisons or toxins for which there is no more specific heading, like those from poisonous FISHES.
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.
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.
Drugs that block nerve conduction when applied locally to nerve tissue in appropriate concentrations. They act on any part of the nervous system and on every type of nerve fiber. In contact with a nerve trunk, these anesthetics can cause both sensory and motor paralysis in the innervated area. Their action is completely reversible. (From Gilman AG, et. al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed) Nearly all local anesthetics act by reducing the tendency of voltage-dependent sodium channels to activate.
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.
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.
Elements of limited time intervals, contributing to particular results or situations.
Venoms from jellyfish; CORALS; SEA ANEMONES; etc. They contain hemo-, cardio-, dermo- , and neuro-toxic substances and probably ENZYMES. They include palytoxin, sarcophine, and anthopleurine.
Genetically engineered MUTAGENESIS at a specific site in the DNA molecule that introduces a base substitution, or an insertion or deletion.
Use of electric potential or currents to elicit biological responses.
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.
Proteins obtained from species in the class of AMPHIBIANS.
The study of PHYSICAL PHENOMENA and PHYSICAL PROCESSES as applied to living things.
Venoms of arthropods of the order Araneida of the ARACHNIDA. The venoms usually contain several protein fractions, including ENZYMES, hemolytic, neurolytic, and other TOXINS, BIOLOGICAL.
A fast inactivating subtype of shaker potassium channels that contains two inactivation domains at its N terminus.
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.
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.
A cell line generated from human embryonic kidney cells that were transformed with human adenovirus type 5.
A genus of fish, in the family GYMNOTIFORMES, capable of producing an electric shock that immobilizes fish and other prey. The species Electrophorus electricus is also known as the electric eel, though it is not a true eel.
A shaker subfamily that is prominently expressed in NEURONS and are necessary for high-frequency, repetitive firing of ACTION POTENTIALS.
Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures.
A potassium-selective ion channel blocker. (From J Gen Phys 1994;104(1):173-90)
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.
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.
Pinched-off nerve endings and their contents of vesicles and cytoplasm together with the attached subsynaptic area of the membrane of the post-synaptic cell. They are largely artificial structures produced by fractionation after selective centrifugation of nervous tissue homogenates.
The parts of a macromolecule that directly participate in its specific combination with another molecule.
Polycyclic ethers produced by Gambierdiscus (DINOFLAGELLATES) from gambiertoxins, which are ingested by fish which in turn may be ingested by humans who are susceptible to the CIGUATERA POISONING.
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.
Inorganic compounds derived from hydrochloric acid that contain the Cl- ion.
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 variety of neuromuscular conditions resulting from MUTATIONS in ION CHANNELS manifesting as episodes of EPILEPSY; HEADACHE DISORDERS; and DYSKINESIAS.
The hollow, muscular organ that maintains the circulation of the blood.
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.
The physical characteristics and processes of biological systems.
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 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)
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
Layers of lipid molecules which are two molecules thick. Bilayer systems are frequently studied as models of biological membranes.
Body organ that filters blood for the secretion of URINE and that regulates ion concentrations.
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)
Pesticides designed to control insects that are harmful to man. The insects may be directly harmful, as those acting as disease vectors, or indirectly harmful, as destroyers of crops, food products, or textile fabrics.
The naturally occurring or experimentally induced replacement of one or more AMINO ACIDS in a protein with another. If a functionally equivalent amino acid is substituted, the protein may retain wild-type activity. Substitution may also diminish, enhance, or eliminate protein function. Experimentally induced substitution is often used to study enzyme activities and binding site properties.
The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.
A condition that is characterized by episodes of fainting (SYNCOPE) and varying degree of ventricular arrhythmia as indicated by the prolonged QT interval. The inherited forms are caused by mutation of genes encoding cardiac ion channel proteins. The two major forms are ROMANO-WARD SYNDROME and JERVELL-LANGE NIELSEN SYNDROME.
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 heterogenous group of inherited disorders characterized by recurring attacks of rapidly progressive flaccid paralysis or myotonia. These conditions have in common a mutation of the gene encoding the alpha subunit of the sodium channel in skeletal muscle. They are frequently associated with fluctuations in serum potassium levels. Periodic paralysis may also occur as a non-familial process secondary to THYROTOXICOSIS and other conditions. (From Adams et al., Principles of Neurology, 6th ed, p1481)
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.
An autosomal dominant defect of cardiac conduction that is characterized by an abnormal ST-segment in leads V1-V3 on the ELECTROCARDIOGRAM resembling a right BUNDLE-BRANCH BLOCK; high risk of VENTRICULAR TACHYCARDIA; or VENTRICULAR FIBRILLATION; SYNCOPAL EPISODE; and possible sudden death. This syndrome is linked to mutations of gene encoding the cardiac SODIUM CHANNEL alpha subunit.
Commonly observed structural components of proteins formed by simple combinations of adjacent secondary structures. A commonly observed structure may be composed of a CONSERVED SEQUENCE which can be represented by a CONSENSUS SEQUENCE.
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.
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.
Positively charged atoms, radicals or groups of atoms which travel to the cathode or negative pole during electrolysis.
A family of membrane-associated proteins responsible for the attachment of the cytoskeleton. Erythrocyte-related isoforms of ankyrin attach the SPECTRIN cytoskeleton to a transmembrane protein (ANION EXCHANGE PROTEIN 1, ERYTHROCYTE) in the erythrocyte plasma membrane. Brain-related isoforms of ankyrin also exist.
The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.
The pore-forming subunits of large-conductance calcium-activated potassium channels. They form tetramers in CELL MEMBRANES.
CALCIUM CHANNELS located within the PURKINJE CELLS of the cerebellum. They are involved in stimulation-secretion coupling of neurons.
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).
Straight tubes commencing in the radiate part of the kidney cortex where they receive the curved ends of the distal convoluted tubules. In the medulla the collecting tubules of each pyramid converge to join a central tube (duct of Bellini) which opens on the summit of the papilla.
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.
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.
Contractile tissue that produces movement in animals.
Venoms from mollusks, including CONUS and OCTOPUS species. The venoms contain proteins, enzymes, choline derivatives, slow-reacting substances, and several characterized polypeptide toxins that affect the nervous system. Mollusk venoms include cephalotoxin, venerupin, maculotoxin, surugatoxin, conotoxins, and murexine.
A hormone secreted by the ADRENAL CORTEX that regulates electrolyte and water balance by increasing the renal retention of sodium and the excretion of potassium.
A quality of cell membranes which permits the passage of solvents and solutes into and out of cells.
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.
The order Actiniaria, in the class ANTHOZOA, comprised of large, solitary polyps. All species are carnivorous.
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 member of the alkali metals. It has an atomic symbol Cs, atomic number 50, and atomic weight 132.91. Cesium has many industrial applications, including the construction of atomic clocks based on its atomic vibrational frequency.
Neurons which conduct NERVE IMPULSES to the CENTRAL NERVOUS SYSTEM.
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.
An antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide.
Compounds based on N-phenylacetamide, that are similar in structure to 2-PHENYLACETAMIDES. They are precursors of many other compounds. They were formerly used as ANALGESICS and ANTIPYRETICS, but often caused lethal METHEMOGLOBINEMIA.
Proteins prepared by recombinant DNA technology.
A mutation in which a codon is mutated to one directing the incorporation of a different amino acid. This substitution may result in an inactive or unstable product. (From A Dictionary of Genetics, King & Stansfield, 5th ed)
A surface anesthetic that acts by preventing transmission of impulses along NERVE FIBERS and at NERVE ENDINGS.
CALCIUM CHANNELS located in the neurons of the brain.
The electrical properties, characteristics of living organisms, and the processes of organisms or their parts that are involved in generating and responding to electrical charges.
The degree of similarity between sequences of amino acids. This information is useful for the analyzing genetic relatedness of proteins and species.
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.
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.
CALCIUM CHANNELS located in the neurons of the brain. They are inhibited by the marine snail toxin, omega conotoxin MVIIC.
Stable sodium atoms that have the same atomic number as the element sodium, but differ in atomic weight. Na-23 is a stable sodium isotope.
A clinically diverse group of epilepsy syndromes characterized either by myoclonic seizures or by myoclonus in association with other seizure types. Myoclonic epilepsy syndromes are divided into three subtypes based on etiology: familial, cryptogenic, and symptomatic (i.e., occurring secondary to known disease processes such as infections, hypoxic-ischemic injuries, trauma, etc.).
A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure.
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.
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.
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.
CELL LINE derived from the ovary of the Chinese hamster, Cricetulus griseus (CRICETULUS). The species is a favorite for cytogenetic studies because of its small chromosome number. The cell line has provided model systems for the study of genetic alterations in cultured mammalian cells.
A potent anti-arrhythmia agent, effective in a wide range of ventricular and atrial ARRHYTHMIAS and TACHYCARDIAS.
Arthropods of the class ARACHNIDA, order Araneae. Except for mites and ticks, spiders constitute the largest order of arachnids, with approximately 37,000 species having been described. The majority of spiders are harmless, although some species can be regarded as moderately harmful since their bites can lead to quite severe local symptoms. (From Barnes, Invertebrate Zoology, 5th ed, p508; Smith, Insects and Other Arthropods of Medical Importance, 1973, pp424-430)
A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.
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.
A family of immunoglobulin-related cell adhesion molecules that are involved in NERVOUS SYSTEM patterning.
A genus in the family Blattidae containing several species, the most common being P. americana, the American cockroach.
An anionic surfactant, usually a mixture of sodium alkyl sulfates, mainly the lauryl; lowers surface tension of aqueous solutions; used as fat emulsifier, wetting agent, detergent in cosmetics, pharmaceuticals and toothpastes; also as research tool in protein biochemistry.
A glutamate antagonist (RECEPTORS, GLUTAMATE) used as an anticonvulsant (ANTICONVULSANTS) and to prolong the survival of patients with AMYOTROPHIC LATERAL SCLEROSIS.
Striated muscle cells found in the heart. They are derived from cardiac myoblasts (MYOBLASTS, CARDIAC).
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)
A 37-amino acid residue peptide isolated from the scorpion Leiurus quinquestriatus hebraeus. It is a neurotoxin that inhibits calcium activated potassium channels.
Members of the class of compounds composed of AMINO ACIDS joined together by peptide bonds between adjacent amino acids into linear, branched or cyclical structures. OLIGOPEPTIDES are composed of approximately 2-12 amino acids. Polypeptides are composed of approximately 13 or more amino acids. PROTEINS are linear polypeptides that are normally synthesized on RIBOSOMES.
Additionally, grayanotoxin only binds to the activated conformation of sodium channels. Normally, voltage gated sodium channels ... grayanotoxin is classified as a reversible Nav1.x agonist. Prolonged sodium channel activation and cell depolarization leads to ... At the peak of the action potential, voltage-gated sodium channels are quickly inactivated and are only reset once the cell has ... The toxicity of grayanotoxin is derived from its ability to interfere with voltage-gated sodium channels located in the cell ...
"Voltage-gated", also called "voltage-sensitive" and "voltage-dependent" sodium channel also known as "VGSCs" or "Nav channel" ... Invertebrates possess two Nav channels (Nav1 and Nav2), whereas vertebrate Nav channels are of the Nav1 family. Sodium-channel ... of some voltage gated sodium channels in a very powerful and reversible manner, without affection of other ion channels. " ... April 2012). "Voltage-Gated Sodium Channels at 60: Structure, Function, and Pathophysiology". The Journal of Physiology. 590 ( ...
Additionally, grayanotoxin only binds to the activated conformation of sodium channels. Normally, voltage gated sodium channels ... grayanotoxin is classified as a reversible Nav1.x agonist. Prolonged sodium channel activation and cell depolarization leads to ... At the peak of the action potential, voltage-gated sodium channels are quickly inactivated and are only reset once the cell has ... The toxicity of grayanotoxin is derived from its ability to interfere with voltage-gated sodium channels located in the cell ...
"Sodium Channel NaV1.5 Expression is Enhanced in Cultured Adult Rat Skeletal Muscle Fibers, The Journal of Membrane Biology" on ... Rapid protein kinase C-dependent reduction of rat skeletal muscle voltage-gated sodium channels by ciliary neurotrophic factor ... lp/springer_journal/sodium-channel-nav1-5-expression-is-enhanced-in-cultured-adult-rat-lAZWCBiJ8J ... Beta 3: an additional auxiliary subunit of the voltage-sensitive sodium channel that modulates channel gating with distinct ...
Carvacrol inhibits the neuronal voltage-gated sodium channels Nav1. .2, Nav1. .6, Nav1. .3, Nav1. .7, and Nav1. .8 expressed in ... Receptor Contribute to Channel Function and Ethanol Sensitivity., Popova M., Int J Mol Sci. April 2, 2020; 21 (7): ... Association of A Novel Splice Site Mutation in P/Q-Type Calcium Channels with Childhood Epilepsy and Late-Onset Slowly ... Bupropion Inhibits Serotonin Type 3AB Heteromeric Channels at Clinically Relevant Concentrations., Stuebler AG., Mol Pharmacol ...
VGSCs (voltage-gated sodium channels) are very important for electrogenesis and nerve impulse conduction, and are suggested to ... CC chemokine ligand 2 upregulates the current density and expression of TRPV1 channels and Nav1. 8 sodium channels in dorsal ... Are voltage-gated sodium channels on the dorsal root ganglion involved in the development of neuropathic pain? ... Dysregulation of voltage-gated sodium channels by ubiquitin ligase NEDD4-2 in neuropathic pain ...
This localized concentration of Na+ channels resembles in structure the ion channel organization at the nodes of Ranvier, yet ... anatomically specialized regions which contain very high densities of sodium ion (Na+) channels. Therefore, saltatory ... This localized concentration of Na+ channels resembles in structure the ion channel organization at the Nodes of Ranvier, yet ... By investigating the efficiency of AP propagation over Nav1.8 channels, we find however that the specific inactivation ...
However, studies should further explore the effects of inflammatory cytokines on voltage-gated sodium channels (VGSCs) and ... ligand-5, IL-10, and transforming growth factor-β1, at 6 and 24 h after injury. Incubation in trauma-conditioned medium ... CXCL13/CXCR5 enhances sodium channel Nav1. 8 current density via p38 MAP kinase in primary sensory neurons following ... Voltage-gated sodium channels (VGSCs) are crucial ion channels for the production of action potentials and neuronal ...
The voltage-gated sodium channel NaV1.7 plays a critical role in pain pathways. We generated an epitope-tagged NaV1.7 mouse ... www.readbyqxmd.com/read/29335280/mapping-protein-interactions-of-sodium-channel-nav1-7-using-epitope-tagged-gene-targeted-mice ... Eukaryotic cyclic nucleotide-modulated channels perform their diverse physiological roles by opening and closing their pores to ... Bipolar voltage maps highlight scar as sites of low voltage, but the voltage amplitude of an electrogram depends upon the ...
0003] Voltage-gated sodium channels are found in all excitable cells including myocytes of muscle and neurons of the central ... 0004] There are currently at least nine known members of the family of voltage-gated sodium channel (VGSC) alpha subunits. ... The Nav1.x subfamily can be functionally subdivided into two groups, those which are sensitive to blocking by tetrodotoxin (TTX ... 0008] Certain inhibitors of voltage gated sodium channels useful in the treatment of pain are known. Thus WO-A-2005/013914 ...
The UPS is an important degradation mechanism of cellular proteins including voltage-gated channels [13, 14]. Ubiquitin (Ub) is ... Voltage-gated sodium channel Nav1. Nav1.5, and proteasome inhibitor MG132 blocked the effect of UBC9 overexpression on Nav1.5 ... Voltage-gated sodium channel Nav1. Posted by Louis Fletcher on September 18, 2020 ... We found that UBC9 regulated the ubiquitination of Nav1.5 and cardiac sodium current densities in both a heterologous HEK293 ...
Sequence similarities between voltage-gated sodium channels and voltage-gated calcium channels suggest that the structure of ... Solution NMR structure of Apo-calmodulin in complex with the IQ motif of human cardiac sodium channel NaV1. The function of the ... human voltage-gated sodium channel Na V 1.. 5 is regulated in part by intracellular calcium signals. The ubiquitous calcium ... With Saorview you have the best in Irish TV and with a combo box you can also access the very best free channels from the UK ...
"Voltage-gated", also called "voltage-sensitive" and "voltage-dependent" sodium channel also known as "VGSCs" or "Nav channel" ... Invertebrates possess two Nav channels (Nav1 and Nav2), whereas vertebrate Nav channels are of the Nav1 family. Sodium-channel ... of some voltage gated sodium channels in a very powerful and reversible manner, without affection of other ion channels. " ... April 2012). "Voltage-Gated Sodium Channels at 60: Structure, Function, and Pathophysiology". The Journal of Physiology. 590 ( ...
Your top supplier for voltage-gated sodium channel research! ... Voltage-gated sodium channels (NaV) are essential for the ... Sodium channels in the adult central nervous system and heart contain β1 through β4 subunits, whereas sodium channels in adult ... Alternative Name BII, Brain type II Na+ channel, Sodium channel protein type 2 subunit alpha ... BII, Brain type II Na+ channel, Sodium channel protein type 2 subunit alpha ...
Your top supplier for voltage-gated Na+ channel research! ... Voltage-gated sodium channels (NaV) are essential for the ... biologically active Nav1.7 channel activators & blockers. Lyophilized powder. Economical. Worldwide shipping at room ... Home › Products › Ion Channels › Na+ ChannelsVoltage-Gated Na+ Channels › Antibodies to NaV Channels ... Sodium channels in the adult central nervous system and heart contain β1 through β4 subunits, whereas sodium channels in adult ...
... voltage gated sodium channel subunit alpha Nav1; peripheral sodium channel 1; neuroendocrine sodium channel ... There are a few main classifications of gated ion channels. There are voltage- gated ion channels, ligand- gated, other gating ... voltage-gated sodium channel alpha subunit Nav1.7; voltage-gated sodium channel subunit alpha Nav1.7; sodium channel, voltage- ... voltage-gated sodium channel complex; plasma membrane. Molecular Function: sodium ion binding; voltage-gated sodium channel ...
Both substances were previously demonstrated to quite potently inhibit neuronal voltage-gated Na(+) channels. Thus, a possible ... Propofol (IC50 126 ± 47 μM) and dexmedetomidine (IC50 182 ± 27 μM) blocked the persistent sodium current induced by veratradine ... molecular mechanism for some of their cardiac side effects is an inhibition of cardiac voltage gated Na(+) channels. In this ... Inhibition of the Cardiac Na+ Channel α-subunit Nav1. 5 by Propofol and Dexmedetomidine. ...
Different role of tetrodotoxin-sensitive voltage-gated sodium channel (NaV1) subtypes in action potential initiation and ... The Transient Receptor Potential (TRP) family of ion channels are expressed on sensory nerve terminals, and when activated can ... www.readbyqxmd.com/read/29435993/different-role-of-tetrodotoxin-sensitive-voltage-gated-sodium-channel-nav1-subtypes-in-action- ... Airway sensory nerves are known to express several receptors and channels that are activated by exogenous and endogenous ...
Crystal structure of the C-terminus of voltage-gated sodium channel in complex with FGF13 and CaM. ... Voltage-gated Na(+) (Na(V)) channels initiate neuronal action potentials. Na(V) channels are composed of a transmembrane domain ... Categories: Human , Chung, B C , Lee, S Y , Pitt, G S , Wang, C , Yan, H , Ef-hand , Iq-motif , Nav1 5 ctd binds to fgf13 and ... May regulate voltage-gated sodium channels transport and function.[79] May also play a role in MAPK signaling.[80] ...
B) Conductance-voltage relationship in the absence and presence of 100 μM lidocaine. (C) Voltage-dependence of sodium channel ... Figure 8. Biophysical effects of lidocaine on NaV1. 5-F1760A channels. (A) Current-voltage relationships in the absence and ... Propranolol blocks cardiac and neuronal voltage-gated sodium channels. Dao W. Wang1,2, Akshitkumar M. Mistry1, Kristopher M. ... Voltage-gated sodium channels are established pharmacological targets for local anesthetics and many other drugs with shared ...
CK2 was further found to directly phosphorylate the voltage gated sodium channel NAv1, thereby enhancing its binding to ankyrin ... CK2 activity is required for the interaction of FGF14 with voltage-gated sodium channels and neuronal excitability. FASEB J. ... Another family of membrane proteins that modulate synaptic activity are the voltage gated sodium channels (NAvs). Recently, the ... Protein kinase CK2 is coassembled with small conductance Ca2+-activated K+ channels and regulates channel gating. Neuron. 2004; ...
sodium channel complex. GO:0034706 9.43. SCN2A SCN1B SCN1A 12. voltage-gated sodium channel complex. GO:0001518 9.17. SCN9A ... Tandem of pore domain in a weak inwardly rectifying K+ channels (TWIK) 65 ... voltage-gated sodium channel activity. GO:0005248 9.23. SCN9A SCN8A SCN7A SCN3A SCN2A SCN1B ... Sodium Voltage-Gated Channel Beta Subunit 1. Protein Coding. 800.39. Pathogenic/Likely pathogenic 6 ...
TTX resistant voltage-gated sodium channel Nav1. .. 8, responsible for hyperexcitability of nociceptors. , are expressed. ... resistant voltage-gated sodium channel Nav1.8 is expressed as early as embryonic day 17 (E17) in rat. [42] These channels play ... tetrodotoxin (TTX) resistant voltage-gated sodium channel Nav1.8 is expressed as early as embryonic day 17 (E17) in rat. ,ref ... TTX resistant voltage-gated sodium channel Nav1.8, responsible for hyperexcitability of nociceptors, are expressed [42] ...
"ProTx-I and ProTx-II inhibit all sodium channel (Nav1) subtypes tested with similar potency." (Priest et al. Toxicon. 2007 49: ... 2015) Post-translational modifications of voltage-gated sodium channels in chronic pain syndromes Frontiers in Pharmacology 6: ... 2014) Voltage-gated sodium channel expression in mouse DRG after SNI leads to re-evaluation of projections of injured fibers ... The repertoire of voltage gated sodium channels (VGSCs) in dorsal root ganglia (DRG) and their modulation by inflammatory ...
Such functions include protease inhibitors, membrane pore formation, ion channel blockers and metal binding proteins. Many of ... Toxin-like functions were revealed using ClanTox, a statistical machine-learning predictor trained on ion channel inhibitors ... inhibit the inactivation of voltage-gated sodium channels. These proteins occupy an expanded chromosomal region. Notably, ... The analysis of neurotoxin (Nav1) evolution exposed extensive genomic expansion of this region [42]. Gene expansion has shaped ...
µ and µO-CTX are two isoforms that specifically target voltage-gated sodium channels. These, by inducing the entrance of sodium ... In this review, we describe the current knowledge of µ-CTX interacting with the different sodium channels subtypes, the ... Hyperexcitability and mutations of sodium channels are responsible for perception and transmission of inflammatory and ... Mahdavi, S.; Kuyucak, S. Molecular dynamics study of binding of µ-conotoxin GIIIA to the voltage-gated sodium channel Nav1. 4. ...
ProTx-II is a potent inhibitor for tetrodotoxin-sensitive and tetrodotoxin-resistant voltage-gated sodium channels. The Nav1 ... Na+ Channel (Especially Nav1.7) / Ca2+ Channel Blocker (Gating Modifier) ProTx-II was originally isolated from the venom of the ... SKU: 4450-s Category: Ion Channel Blocker & Toxins Tags: ion channel blocker, Nav1.7 channel, tetrodotoxin, Toxin ... Characterization of Endogenous Sodium Channels in the ND7-23 Neuroblastoma Cell Line: Implications for Use as a Heterologous ...
... also known as sodium channel protein type 9 subunit alpha, neuroendocrine sodium channel, hNE-Na and peripheral sodium channel ... Reduced availability of voltage-gated sodium channels by depolarization or blockade by tetrodotoxin boosts burst firing and ... Peripheral sodium channel 1) (PN1) (Sodium channel protein type IX subunit alpha) (Voltage-gated sodium channel subunit alpha ... also known as sodium channel protein type 9 subunit alpha, neuroendocrine sodium channel, hNE-Na and peripheral sodium channel ...
... venom peptide ProTx-II with lipid membranes is a prerequisite for its inhibition of human voltage-gated sodium channel NaV1. 7 ... In addition, voltage-gated sodium channels play important roles in action potential generation and propagation. Among them, Na ... ProTx II has the potency to inhibit the human voltage-gate sodium channel 1.7 (hNa V1.7), which is involved in nociception and ... Owing to the well-defined three-dimensional structure and ability to inhibit voltage-gated sodium (Na V), potassium (K V) and ...
Reduction of voltage gated sodium channel protein in DRG by vector mediated miRNA reduces pain in rats with painful diabetic ... Nomenclature and structure-function relationships of voltage-gated sodium channels. Pharmacol Rev. 2005;57:397-409.PubMed ... Review of the inherited pain syndromes associated with mutations in the NaV1.7 sodium channel. PubMedCrossRefGoogle Scholar ... Continuous delta-opioid receptor activation reduces neuronal voltage-gated sodium channel (NaV1.7) levels through activation of ...
Intro gene encodes the -subunit of cardiac voltage-gated Na+ channels (Nav1.5), which generate the inward sodium current (INa) ... Introduction We functionally analyzed a frameshift mutation in the gene encoding cardiac Na+ channels (Nav1. that was not ... to CD2 and plays a role as an accessory molecule in g/d T cell recognition and a/b T cell antigen recognition channel gating ... Summary Despite a severe truncation of the C-terminus, the producing mutated channels generate currents, albeit with reduced ...
transient receptor potential a cation channel with 30 transmembrane domains voltage gated sodium channel voltage gated calcium ... noted that many pain syndromes are due to defect in activity of Nav1 type channels caused by mutations in sodium channel genes ... Voltage-gated sodium channels: (NaV)igating the field to determine their contribution to visceral nociception. J Physiol 2018; ... This chromosome region was found to harbor the locus for a voltage gated sodium channel Nav1.7 (SCN9A). Each of the three ...
  • The toxicity of grayanotoxin is derived from its ability to interfere with voltage-gated sodium channels located in the cell membrane of neurons. (wikipedia.org)
  • In vitro PKC kinase assays and autoradiograms suggested that Nav1.8 within DRG neurons was a substrate of PKC and direct phosphorylation of the Na v 1.8 channel by PKC regulates its function in these neurons. (portlandpress.com)
  • The number of ion channels on the surface of neurons' membrane is usually thought to be large enough to justify combining the individual channel conductances into a continuous measure of overall conductivity ( Dayan and Abbott, 2001 ), as originally done by Hodgkin and Huxley (1952) . (frontiersin.org)
  • However, studies should further explore the effects of inflammatory cytokines on voltage-gated sodium channels (VGSCs) and excitability in distal intact neurons. (biomedcentral.com)
  • Thus, like many other neuronal channels and receptors, Nav channels predated neurons. (wikipedia.org)
  • 11 These recent findings highlight the role of this Na V isoform and the subset of DRG neurons that express this channel in physiological pain sensation. (alomone.com)
  • We used the bleomycin-induced pulmonary fibrosis model to investigate the change in TLR expression in pulmonary neurons and the association of TLRs with transient receptor potential (TRP) channels in pulmonary neurons. (readbyqxmd.com)
  • Virtually all the jugular neurons expressed the TTX-sensitive channel Na V 1. (readbyqxmd.com)
  • Available evidence indicates voltage-gated Na + channels (VGSCs) in peripheral sensory neurons are essential for the pain and hypersensitivity associated with tissue injury. (elifesciences.org)
  • However, our understanding of the biophysical and pharmacological properties of the channels in sensory neurons is largely based on the study of heterologous systems or rodent tissue, despite evidence that both expression systems and species differences influence these properties. (elifesciences.org)
  • Nevertheless, virtually all that is known about the biophysical and pharmacological properties of VGSCs comes from the study of these channels in heterologous expression systems and in isolated rodent sensory neurons. (elifesciences.org)
  • Mitochondria-derived superoxide and voltage-gated sodium channels in baroreceptor neurons from chronic heart-failure rats. (nextbio.com)
  • Our iPSC-derived sensory neurons express several voltage-gated sodium ion channels and transient receptor potential (TRP) ion channels that play a key role in nociception. (axolbio.com)
  • Axol Human iPSC-derived Sensory Neurons express Na v 1.7, a key sodium ion channel in DRG sensory neurons that plays an important role in peripheral pain sensation. (axolbio.com)
  • Axol Human iPSC-derived Sensory Neurons express the nociceptive voltage-gated sodium ion channel Na v 1.7 on a multi-electrode array (MEA) (Alpha MED Scientific). (axolbio.com)
  • Mature iPSC-derived sensory neurons express the sodium ion channels, Na v 1.7 and Na v 1.8, and neuronal marker, doublecortin (DCX). (axolbio.com)
  • Nav1.9 is best known for its high expression levels in peripheral sensory neurons and is thought to carry the NaN current, a persistent and tetrodrotoxin (TTX)-resistant voltage-gated Na Current , possibly involved in pain-related signaling [1438] . (epfl.ch)
  • Our study aimed to investigate whether PKC (protein kinase C)-NF-κB (nuclear factor κB) is involved in CCL2-induced regulation of voltage-gated sodium Nav1.8 currents and expression. (portlandpress.com)
  • Summary Despite a severe truncation of the C-terminus, the producing mutated channels generate currents, albeit with reduced amplitude and modified biophysical properties, confirming the key part of the C-terminal website in the manifestation and function of the cardiac Na+ channel. (boothampitheatre.com)
  • Moreover, implementing all the K-A channel equations (for tau n, hinf, and tau h) as cited in Choi Waxman, and calculating I_KA = gKA * n * h * (V-EK) and running a step protocol (-120mV up to various terminal voltages) gives currents that do not agree with those cited in the paper. (yale.edu)
  • Phosphorylation at Ser-1490 by PKC in a highly conserved cytoplasmic loop increases peak sodium currents. (abcam.cn)
  • 2012). Nonetheless, we detected neither voltage-gated whole-cell Ca2+ currents (Figure 9-figure supplement 1A) nor depolarization-induced Ca2+ signals (Figure 9-figure supplement 1B) in starved N2 cells. (pteninhibitor.com)
  • When grayanotoxin is present, binding induces further conformational changes that prevent sodium channel inactivation and lead to a prolonged depolarization. (wikipedia.org)
  • By investigating the efficiency of AP propagation over Nav1.8 channels, we find however that the specific inactivation properties of these channels significantly increase the metabolic cost of signaling in C-fibers. (frontiersin.org)
  • Site 3 binds alpha-scorpion and sea anemone toxins, which slow sodium channel inactivation. (wikipedia.org)
  • The voltage dependencies of fast and slow inactivation as well as the time course of recovery from inactivation were shifted by both propofol and dexmedetomidine. (jpt.com)
  • 7 voltage-sensors to inhibit channel activation and inactivation. (psyclopeptide.com)
  • It has been proposed that C-terminus helices participate in the control of inactivation through stabilization of the closed gate [9,10]. (boothampitheatre.com)
  • Heterologous manifestation of the mutation resulted in a marked decrease of maximum INa density primarily caused by a reduced channel trafficking toward the plasma membrane and in severe alterations in channel activation and inactivation. (boothampitheatre.com)
  • Nav1.9 it is formed of 1765 residues and contains all the hallmarks of Na+ channels, including the inactivation tripeptide Ile-Phe-Met in L3. (epfl.ch)
  • The short intracellular loop connecting homologous domains III and IV serves as the inactivation gate, folding into the channel structure and blocking the pore from the inside during sustained depolarization of the membrane. (epfl.ch)
  • 2. What is meant by Na+ channel inactivation? (alico7.com)
  • More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I): ##STR00001## or a pharmaceutically acceptable salt thereof, wherein Ar.sup.1, X, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined in the description. (patents.com)
  • Toxin-like functions were revealed using ClanTox, a statistical machine-learning predictor trained on ion channel inhibitors from venomous animals. (mdpi.com)
  • Such functions include protease inhibitors, membrane pore formation, ion channel blockers and metal binding proteins. (mdpi.com)
  • Accordingly, inhibitors of voltage-gated Ca2+ channels didn't modify ATP-mediated Ca2+ signals (Figure 9-figure supplement 1C). (pteninhibitor.com)
  • Mapping protein interactions of sodium channel NaV1.7 using epitope-tagged gene-targeted mice. (readbyqxmd.com)
  • The voltage-gated sodium channel NaV1.7 plays a critical role in pain pathways. (readbyqxmd.com)
  • We generated an epitope-tagged NaV1.7 mouse that showed normal pain behaviours to identify channel-interacting proteins. (readbyqxmd.com)
  • Analysis of NaV1.7 complexes affinity-purified under native conditions by mass spectrometry revealed 267 proteins associated with Nav1.7 in vivo The sodium channel β3 (Scn3b), rather than the β1 subunit, complexes with Nav1.7, and we demonstrate an interaction between collapsing-response mediator protein (Crmp2) and Nav1. (readbyqxmd.com)
  • Potent channel blocker with high selectivity for Nav1.7 channel. (peptanova.de)
  • The Nav1 type channels exists in different sub types and ProTx-II shows a special affinity to the Nav1.7 channel which is responsible for pain processing. (peptanova.de)
  • ProTx-II, a selective inhibitor of NaV1.7 sodium channels, blocks action potential propagation in nociceptors. (psyclopeptide.com)
  • Laedermann CJ, Syam N, Pertin M, Decosterd I, Abriel H.. (2013), ' β1- and β3- voltage-gated sodium channel subunits modulate cell surface expression and glycosylation of Nav1.7 in HEK293 cells. . (antibodiesinc.com)
  • 2013), ' Functional expression of the voltage-gated Na⁺-channel Nav1.7 is necessary for EGF-mediated invasion in human non-small cell lung cancer cells. . (antibodiesinc.com)
  • The tetrodotoxin resistant NaV1.5, NaV1.8, and NaV1.9 are closely related ( see phylogenetic tree, fig. 2B in Catterall [817] ), and their amino acid sequences are greater than 64% identical to those of the four sodium channels encoded on chromosome 2 (the highly tertodotoxin sensitive NaV1.1, NaV1.2, NaV1.3, and NaV1.7). (epfl.ch)
  • Paroxysmal Extreme Pain Disorder, also known as familial rectal pain , is related to mucocutaneous ulceration, chronic and brugada syndrome 1 , and has symptoms including pain An important gene associated with Paroxysmal Extreme Pain Disorder is SCN9A (Sodium Voltage-Gated Channel Alpha Subunit 9), and among its related pathways/superpathways are Activation of cAMP-Dependent PKA and Developmental Biology . (malacards.org)
  • Our data evidenced an increase in NaV1.5 channels and the involvement of β subunits in the regulation of sodium current and fiber excitability. (deepdyve.com)
  • Sodium-channel proteins in the mammalian brain are composed of an association that include one alpha subunit and one or more auxiliary beta subunits. (wikipedia.org)
  • Nine types of alpha subunits have been described (Nav1.1 to Nav1.9), and a tenth related isoform (Nax) may also play some role as a Nav channel. (wikipedia.org)
  • 2-3 Mammalian sodium channels are heterotrimers, composed of a central, pore-forming α subunit and two auxiliary β subunits. (alomone.com)
  • Sodium channels in the adult central nervous system and heart contain β 1 through β 4 subunits, whereas sodium channels in adult skeletal muscle have only the β 1 subunit. (alomone.com)
  • Rather, in tsA-201 cells, the beta-subunits drive a rightward shift in the voltage-dependence of channel activation. (elifesciences.org)
  • [817] . These alpha subunits, mediate voltage-dependent gating and conductance, while auxiliary beta subunits regulate the kinetic properties of the channel and facilitate membrane localization of the complex. (epfl.ch)
  • This activated conformation allows for an influx of sodium ions resulting in cell depolarization, followed by the firing of an action potential. (wikipedia.org)
  • Owing to its transient ability to activate channels and increase membrane permeability to sodium ions, grayanotoxin is classified as a reversible Nav1.x agonist. (wikipedia.org)
  • 1 Na V channels are activated in response to depolarization and selectively allow flow of Na + ions. (alomone.com)
  • Ion channels are integral membrane proteins that help establish and control the small voltage gradient across the plasma membrane of living cells by allowing the flow of ions down their electrochemical gradient (1). (mybiosource.com)
  • Whereas some ion channels permit the passage of ions based on charge, others conduct based on a ionic species, such as sodium or potassium. (mybiosource.com)
  • These, by inducing the entrance of sodium ions in the cell, modulate the neuronal excitability by depolarizing plasma membrane and propagating the action potential. (mdpi.com)
  • The passage of ions into cells can be accomplished through specific ionotropic receptors or through specific ion channels that only conduct passage of ions. (kundoc.com)
  • Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient (PubMed:7720699, PubMed:17167479, PubMed:25240195, PubMed:26680203, PubMed:15385606, PubMed:16988069, PubMed:17145499, PubMed:19369487, PubMed:24311784). (abcam.cn)
  • Leak channels- always open allow ions to flow back and fourth across the cell membrane Na cl ,K and Ca ions and they just flow back and fourth without any gate keeper or obstruction, When the neuron is at rest its cytoplasm is Negatively charged. (alico7.com)
  • The Action Potential Graphics are used with permission of: Pearson Education Inc., publishing as Benjamin Cummings (http://www.aw-bc.com) ** If this is not printed in color, it is suggested you color code the ion channels and ions as you go through this topic. (alico7.com)
  • Ions channels and ions should be color coded as follows: Red: Sodium ion channels and sodium ions Blue: Potassium ion channels and potassium ions Page 1. (alico7.com)
  • Ion channels are selective for specific ions. (alico7.com)
  • Normally, voltage gated sodium channels are activated (opened) only when the cell membrane potential reaches a specific threshold voltage. (wikipedia.org)
  • Recent molecular anatomy showed that in C-fibers, the very thin (0.1 μm diameter) axons of the peripheral nervous system, Nav1.8 channels are clustered together on lipid rafts that float in the cell membrane. (frontiersin.org)
  • Propagation of action potentials (AP) in axons relies on the concerted action of membrane-spanning selectively permeable ion channels ( Hodgkin and Huxley, 1952 ). (frontiersin.org)
  • The conceptual transition from conductivity (per surface area) to density of channels, with each channel having only two possible conductance value corresponding to its open and closed states, involves investigating the effects of possible non-uniformities in the distribution of ion channels across the membrane. (frontiersin.org)
  • The first are voltage- gated ion channels which open and close in response to membrane potential. (mybiosource.com)
  • Some studies have pointed out that ProTx-II acts by binding to the membrane-embedded voltage sensor domain of h Na V 1.7, but the exact mechanism of action has not been explored clearly. (psyclopeptide.com)
  • channel gating and membrane expression. (boothampitheatre.com)
  • Optimistic modulation of Ca2+ entry by TRPM5-mediated membrane depolarization has been linked towards the activation of voltage-gated Ca2+ channels (Colsoul et al. (pteninhibitor.com)
  • A sodium channel in a cell membrane whose opening is governed by the membrane potential. (epfl.ch)
  • These residues serve as gating charges and move across the membrane to initiate channel activation in response to depolarization of the membrane. (epfl.ch)
  • 2) If the threshold of excitation is reached, all Na+ channels open and the membrane depolarizes. (alico7.com)
  • The resting potential is due to the sodium potassium pump where 3 Na+ ion move outside the membrane and 2 K+ ion move into the cell ( and this causes the negative potential inside the cell membrane. (alico7.com)
  • What structures in the cell membrane function as ion channels? (alico7.com)
  • The UPS is an important degradation mechanism of cellular proteins including voltage-gated channels [13, 14]. (osi-930.info)
  • Loss of NF-186, NrCAM, Nav channels, or βIV spectrin did not affect other neuronal AIS proteins. (rupress.org)
  • Thus, the clustering of ion channels at nodes of Ranvier is thought to depend on binding to cytoskeletal and scaffolding proteins that are positioned along axons by extracellular, heterophilic interactions between axonal and glial CAMs ( Schafer and Rasband, 2006 ). (rupress.org)
  • ProTx-II is a potent inhibitor for tetrodotoxin-sensitive and tetrodotoxin-resistant voltage-gated sodium channels. (peptanova.de)
  • It is a tetrodotoxin-sensitive Na(+) channel isoform (PubMed:7720699). (abcam.cn)
  • Voltage-gated", also called "voltage-sensitive" and "voltage-dependent" sodium channel also known as "VGSCs" or "Nav channel" are crucial elements of normal physiology in a variety of animals, including flies, leeches, squid and jellyfish, as well as mammalian and non-mammalian vertebrates. (wikipedia.org)
  • It has long been appreciated that voltage-gated Na + channels (VGSCs) underlie the upstroke of the action potential, and therefore play an essential role in the propagation of action potentials along axons ( Hodgkin and Huxley, 1952a , 1952b ). (elifesciences.org)
  • Prolonged sodium channel activation and cell depolarization leads to overstimulation of the central nervous system. (wikipedia.org)
  • Vandael DH, Ottaviani MM, Legros C, Lefort C, Guérineau NC, Allio A, Carabelli V, Carbone E.. (), ' Reduced availability of voltage-gated sodium channels by depolarization or blockade by tetrodotoxin boosts burst firing and catecholamine release in mouse chromaffin cells. . (antibodiesinc.com)
  • Both substances were previously demonstrated to quite potently inhibit neuronal voltage-gated Na(+) channels. (jpt.com)
  • of these channels contributes to the dynamic regulation of neuronal excitability. (elifesciences.org)
  • 7 channel mutation associated with hereditary erythromelalgia contributes to neuronal hyperexcitability and displays reduced lidocaine sensitivity. (yale.edu)
  • NSTX blocks the extracellular portion, the outer vestibule, of some voltage gated sodium channels in a very powerful and reversible manner, without affection of other ion channels. (wikipedia.org)
  • At the peak of the action potential, voltage-gated sodium channels are quickly inactivated and are only reset once the cell has repolarized to resting potential. (wikipedia.org)
  • hypothesized that action potentials could be propagated along thin ( d ≈ 0.2 μm) axons by "jumping" between individual Na + channels placed a few microns apart. (frontiersin.org)
  • Voltage-gated sodium channels (Na V ) are essential for the generation of action potentials and for cell excitability. (alomone.com)
  • Intro gene encodes the -subunit of cardiac voltage-gated Na+ channels (Nav1.5), which generate the inward sodium current (INa) that is critical for the genesis and propagation of action potentials and, subsequently, determines cardiac conduction and excitability speed from the electrical impulse inside the center [1,2]. (boothampitheatre.com)
  • CCL2 [chemokine (C-C motif) ligand 2] contributes to the inflammation-induced neuropathic pain through activating VGSC (voltage-gated sodium channel)-mediated nerve impulse conduction, but the underlying mechanism is currently unknown. (portlandpress.com)
  • Hyperexcitability and mutations of sodium channels are responsible for perception and transmission of inflammatory and neuropathic pain states. (mdpi.com)
  • These channels exhibited increased activation time constant (τm) and reduced conductance, similar to what has been observed in denervated muscles in vivo, where the density of NaV1.5 was increasing progressively after denervation. (deepdyve.com)
  • At day 7, τh was back to normal and τm still increased, in agreement with a decrease in sodium current and conductance at day 4 and normalization at day 7. (deepdyve.com)
  • Touch and pressure on the skin lead to opening of mechanosensitive channels located within the sensory receptors. (kundoc.com)
  • Open channel structure of MscL and the gating mechanism of mechanosensitive channels. (binaryoptionsmembers.com)
  • A proton leak current through the cardiac sodium channel is linked to mixed arrhythmia and the dilated cardiomyopathy phenotype. (ulaval.ca)
  • Thus, a possible molecular mechanism for some of their cardiac side effects is an inhibition of cardiac voltage gated Na(+) channels. (jpt.com)
  • In this review, we describe the current knowledge of µ-CTX interacting with the different sodium channels subtypes, the mechanism of action and their potential therapeutic use as analgesic compounds in the clinical management of pain conditions. (mdpi.com)
  • Airway sensory nerves are known to express several receptors and channels that are activated by exogenous and endogenous mediators that cause coughing. (readbyqxmd.com)
  • Sensory receptors General factors In considering sensory systems it is important to take into account initiating stimuli, cell membranes, cellular receptors, ion channels, ion pumps and intra-cellular signaling systems, particularly G- protein coupled systems. (kundoc.com)
  • Gueret, G. 2010-06-02 00:00:00 This study analyzes changes in the distribution, electrophysiological properties, and proteic composition of voltage-gated sodium channels (NaV) in cultured adult rat skeletal muscle fibers. (deepdyve.com)
  • The action of NSTX produces minimal effect on cardiac Nav, where it exhibits about 20-60 fold lesser affinity than in Nav channels from rat skeletal muscle and rat brain. (wikipedia.org)
  • Former five, but more recently, six neurotoxin receptor sites have been recognized between the seven receptor site located in the vertebrate sodium channel receptor alpha subunit: Site 1 binds the sodium channel blockers tetrodotoxin and saxitoxin. (wikipedia.org)
  • Local anesthetic receptor site binds local anesthetics, antiarrhythmic drugs and antiepileptic drugs NSTX and other site 1 blockers have high affinity (very low dissociation constant) and high specificity for Nav channels. (wikipedia.org)
  • The Research Pack contains all you need for Na V 1.7 research: Antibodies recognizing different domains of the channel, a classical Na V channel activator and Na V 1.7 specific blockers, all in one economical package! (alomone.com)
  • Metoprolol and nadolol did not block Na V 1.5 indicating that sodium channel block is not a class effect of β-blockers. (frontiersin.org)
  • A. S. Aromolaran , Chahine, M. , et Boutjdir, M. , « Regulation of Cardiac Voltage-Gated Sodium Channel by Kinases: Roles of Protein Kinases A and C. » , Handb Exp Pharmacol , 2017. (ulaval.ca)
  • Voltage-gated sodium channels are established pharmacological targets for local anesthetics and many other drugs with shared mechanisms of action including certain anti-arrhythmic and anti-epilepsy agents. (frontiersin.org)
  • The potential problem with this situation is highlighted by evidence that both the biophysical and pharmacological properties of channels are influenced by the expression system and species differences. (elifesciences.org)
  • Site 4 binds beta-scorpion toxins, which affect sodium channel activation. (wikipedia.org)
  • Toxins such as neosaxitoxin and tetrodotoxin have less affinity for most cardiac Nav channels than for most Nav channels in nerve tissue. (wikipedia.org)
  • ProTx-II conforms to the inhibitory cystine knot (ICK) 2 motif, a common structural fold among spider toxins targeting ion channels. (psyclopeptide.com)
  • Owing to the well-defined three-dimensional structure and ability to inhibit voltage-gated sodium (Na V ), potassium (K V ) and calcium (Ca V ) ion channels with high potency and selectivity, disulfide-rich peptide toxins have attracted much attention as potential analgesics. (psyclopeptide.com)
  • The tarantula toxins ProTx-II and HWTX-IV differentially interact with human Nav1. (psyclopeptide.com)
  • Inhibition of the Cardiac Na+ Channel α-subunit Nav1. (jpt.com)
  • Interaction of tarantula venom peptide ProTx-II with lipid membranes is a prerequisite for its inhibition of human voltage-gated sodium channel NaV1. (psyclopeptide.com)
  • The latter include calcium and sodium channels, chloride channels, potassium channels. (kundoc.com)
  • Secondary damages implicate several mechanisms, including influence of inflammatory mediators, mainly cytokines, on excitability of ion channels. (biomedcentral.com)
  • Nav channels form the basis for electrical excitability in animals. (wikipedia.org)
  • Moreover, NSTX is so active on nerve Nav channel than is roughly a million-fold more potent than lidocaine. (wikipedia.org)
  • Name:shasou Exercise 3: Neurophysiology of Nerve Impulses: Activity 5: The Action Potential: Measuring Its Absolute and Relative Refractory Periods Lab Report Pre-lab Quiz Results You scored 50% by answering 2 out of 4 questions correctly. (alico7.com)
  • Interestingly, unlike additional C-terminal website truncating mutations [11], the mutation here presented did not modify INa,L suggesting that deletions of different lengths can differentially impact gating properties of the variants. (boothampitheatre.com)
  • SCN12A) encodes Nav1.9, a voltage-gated sodium channel alpha subunit, type XI. (epfl.ch)
  • Plasmids, mutagenesis, siRNAs and t-CSM peptide The manifestation construct for human being cardiac sodium route gene in vector pcDNA3 (pcDNA3-SCN5A) once was referred to [5, 6, 23C27]. (osi-930.info)
  • An important gene associated with Generalized Epilepsy with Febrile Seizures Plus is SCN1B (Sodium Voltage-Gated Channel Beta Subunit 1), and among its related pathways/superpathways are Developmental Biology and G-Beta Gamma Signaling . (malacards.org)
  • Introduction We functionally analyzed a frameshift mutation in the gene encoding cardiac Na+ channels (Nav1. (boothampitheatre.com)
  • ProTx II has the potency to inhibit the human voltage-gate sodium channel 1.7 (hNa V 1.7), which is involved in nociception and might have potential as a pain therapeutic. (psyclopeptide.com)
  • Physiological interactions between Nav1. (yale.edu)
  • It inhibits multiple sodium channel subtypes but it is reported to be ~100-fold more selective for h Na V 1.7. (psyclopeptide.com)
  • Additionally, grayanotoxin only binds to the activated conformation of sodium channels. (wikipedia.org)
  • Site 2 binds lipid-soluble sodium channel activators such as veratridine. (wikipedia.org)
  • Site 5 binds the polyether ladder brevetoxins and ciguatoxin. (wikipedia.org)
  • ICK peptides are defined by a 1-4, 2-5, 3-6 cystine connectivity and often have limited regular secondary structure. (psyclopeptide.com)
  • Our findings establish sodium channels as targets for propranolol and may help explain some beneficial effects of the drug in treating cardiac arrhythmias, and may explain certain adverse central nervous system effects. (frontiersin.org)
  • Here, we report a new clinical case of debilitating itch and altered pain perception resulting from the heterozygous de novo p.L811P gain-of-function mutation in Na V 1.9, a voltage-gated sodium (Na V ) channel subtype that relays sensory information from the periphery to the spine. (jci.org)
  • Sodium overload due to a persistent current that attenuates the arrhythmogenic potential of a novel LQT3 mutation. (ulaval.ca)
  • Experiments utilizing squid axonal membranes indicate that sodium channel binding likely occurs on the internal face of the neuron. (wikipedia.org)
  • Mediates the voltage-dependent sodium ion permeability of excitable membranes. (abcam.cn)
  • In addition, voltage-gated sodium channels play important roles in action potential generation and propagation. (psyclopeptide.com)
  • Earlier in vitro electrophysiological studies of the effects of propranolol on heart rate and conduction performed in frog atria, rat and canine ventricular myocytes suggested that the drug might be interacting with sodium channels. (frontiersin.org)
  • In the latter axons the AP jumps along the nodes of Ranvier-discrete, anatomically specialized regions which contain very high densities of sodium ion (Na + ) channels. (frontiersin.org)
  • We found that UBC9 regulated the ubiquitination of Nav1.5 and cardiac sodium current densities in both a heterologous HEK293 cell expression system and neonatal cardiomyocytes. (osi-930.info)
  • whereas rapid and efficient action potential conduction along axons depends on high densities of Nav channels located at nodes of Ranvier. (rupress.org)
  • After 4 days of culture, an increase of the NaV1.5 channel type was observed. (deepdyve.com)
  • In this study, we therefore explored the effects of propofol and dexmedetomidine on the cardiac predominant Na(+) channel α-subunit Nav1.5. (jpt.com)
  • Ondansetron is a 5-HT 3 antagonist used to prevent nausea and vomiting associated with cancer treatment and postoperative procedures. (googleteo.com)