Acid Sensing Ion Channel Blockers: A subclass of sodium channel blockers that are specific for ACID-SENSING SODIUM CHANNELS.Ethosuximide: An anticonvulsant especially useful in the treatment of absence seizures unaccompanied by other types of seizures.Ion Channels: 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.Calcium Channel Blockers: A class of drugs that act by selective inhibition of calcium influx through cellular membranes.Ion Channel Gating: 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.Potassium Channel Blockers: 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.Calcium Channels: 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.Acid Sensing Ion Channels: 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 Channel Blockers: 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.Chloride Channels: Cell membrane glycoproteins that form channels to selectively pass chloride ions. Nonselective blockers include FENAMATES; ETHACRYNIC ACID; and TAMOXIFEN.Potassium Channels, Inwardly Rectifying: Potassium channels where the flow of K+ ions into the cell is greater than the outward flow.Potassium Channels, Voltage-Gated: 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.Calcium Channels, L-Type: 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.Membrane Potentials: 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).Electrophysiology: 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 Channels, Calcium-Activated: Potassium channels whose activation is dependent on intracellular calcium concentrations.Patch-Clamp Techniques: 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.KATP 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.Ligand-Gated Ion Channels: A subclass of ion channels that open or close in response to the binding of specific LIGANDS.Calcium: 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.Nifedipine: A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure.Electric Conductivity: The ability of a substrate to allow the passage of ELECTRONS.Potassium: 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.Calcium Channels, T-Type: 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.Shaker Superfamily of Potassium Channels: 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.Cyclic Nucleotide-Gated Cation Channels: 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.Dihydropyridines: Pyridine moieties which are partially saturated by the addition of two hydrogen atoms in any position.Calcium Channels, N-Type: CALCIUM CHANNELS that are concentrated in neural tissue. Omega toxins inhibit the actions of these channels by altering their voltage dependence.Potassium Channels: 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.Ion Transport: 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.Large-Conductance Calcium-Activated Potassium Channels: 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.TRPC Cation Channels: 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.Diltiazem: A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.Verapamil: A calcium channel blocker that is a class IV anti-arrhythmia agent.Xenopus laevis: 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.Oocytes: 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).TRPM Cation Channels: 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.Kv1.3 Potassium Channel: A delayed rectifier subtype of shaker potassium channels that is the predominant VOLTAGE-GATED POTASSIUM CHANNEL of T-LYMPHOCYTES.Tetraethylammonium: A potassium-selective ion channel blocker. (From J Gen Phys 1994;104(1):173-90)TRPV Cation Channels: 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.Sodium Channels: 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.Ether-A-Go-Go Potassium Channels: 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.Kv1.2 Potassium Channel: A delayed rectifier subtype of shaker potassium channels that is selectively inhibited by a variety of SCORPION VENOMS.Calcium Channel Agonists: 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.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.Action Potentials: Abrupt changes in the membrane potential that sweep along the CELL MEMBRANE of excitable cells in response to excitation stimuli.Glyburide: An antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide.Epithelial Sodium Channels: 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.4-Aminopyridine: 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.Nitrobenzoates: Benzoic acid or benzoic acid esters substituted with one or more nitro groups.Transient Receptor Potential Channels: 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.Rats, Sprague-Dawley: 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.Kinetics: The rate dynamics in chemical or physical systems.Neurons: 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.Molecular Sequence Data: 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.KCNQ Potassium Channels: 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.Amino Acid Sequence: 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.Kv1.1 Potassium Channel: A delayed rectifier subtype of shaker potassium channels that is commonly mutated in human episodic ATAXIA and MYOKYMIA.Cells, Cultured: 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.Kv1.5 Potassium Channel: 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.Small-Conductance Calcium-Activated Potassium Channels: 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.Sodium: A member of the alkali group of metals. It has the atomic symbol Na, atomic number 11, and atomic weight 23.Chlorides: Inorganic compounds derived from hydrochloric acid that contain the Cl- ion.Xenopus: An aquatic genus of the family, Pipidae, occurring in Africa and distinguished by having black horny claws on three inner hind toes.Mibefradil: A benzimidazoyl-substituted tetraline that selectively binds and inhibits CALCIUM CHANNELS, T-TYPE.Cell Membrane: The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.Charybdotoxin: A 37-amino acid residue peptide isolated from the scorpion Leiurus quinquestriatus hebraeus. It is a neurotoxin that inhibits calcium activated potassium channels.Barium: 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.Scorpion Venoms: 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.Adenosine Triphosphate: 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.Nicardipine: A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents.Shab Potassium Channels: 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.KCNQ1 Potassium Channel: A voltage-gated potassium channel that is expressed primarily in the HEART.Apamin: 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.Tetrodotoxin: 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.omega-Conotoxin GVIA: 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.Hyperpolarization-Activated Cyclic Nucleotide-Gated Channels: 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.Cell Line: Established cell cultures that have the potential to propagate indefinitely.Cations: Positively charged atoms, radicals or groups of atoms which travel to the cathode or negative pole during electrolysis.Amlodipine: A long-acting dihydropyridine calcium channel blocker. It is effective in the treatment of ANGINA PECTORIS and HYPERTENSION.Angiotensin II Type 1 Receptor Blockers: Agents that antagonize ANGIOTENSIN II TYPE 1 RECEPTOR. Included are ANGIOTENSIN II analogs such as SARALASIN and biphenylimidazoles such as LOSARTAN. Some are used as ANTIHYPERTENSIVE AGENTS.Models, Molecular: Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures.omega-Conotoxins: A family of structurally related neurotoxic peptides from mollusk venom that inhibit voltage-activated entry of calcium into the presynaptic membrane. They selectively inhibit N-, P-, and Q-type calcium channels.Nimodipine: A calcium channel blockader with preferential cerebrovascular activity. It has marked cerebrovascular dilating effects and lowers blood pressure.Niflumic Acid: An analgesic and anti-inflammatory agent used in the treatment of rheumatoid arthritis.Amiloride: 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)Kv1.4 Potassium Channel: A fast inactivating subtype of shaker potassium channels that contains two inactivation domains at its N terminus.Nitrendipine: A calcium channel blocker with marked vasodilator action. It is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive.Intermediate-Conductance Calcium-Activated Potassium Channels: 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.Shaw Potassium Channels: A shaker subfamily that is prominently expressed in NEURONS and are necessary for high-frequency, repetitive firing of ACTION POTENTIALS.Rats, Wistar: A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.Protein Subunits: 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.Protein Structure, Tertiary: 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.Models, Biological: 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.Shal Potassium Channels: 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.Spider Venoms: 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.Ions: 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.Hydrogen-Ion Concentration: 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)Lipid Bilayers: Layers of lipid molecules which are two molecules thick. Bilayer systems are frequently studied as models of biological membranes.Guinea Pigs: 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.4,4'-Diisothiocyanostilbene-2,2'-Disulfonic Acid: An inhibitor of anion conductance including band 3-mediated anion transport.Time Factors: Elements of limited time intervals, contributing to particular results or situations.Tetraethylammonium CompoundsNAV1.5 Voltage-Gated Sodium Channel: 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.Mutation: 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.Delayed Rectifier Potassium Channels: 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.G Protein-Coupled Inwardly-Rectifying Potassium Channels: 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.Electric Stimulation: Use of electric potential or currents to elicit biological responses.Calcium Channels, P-Type: CALCIUM CHANNELS located within the PURKINJE CELLS of the cerebellum. They are involved in stimulation-secretion coupling of neurons.Degenerin Sodium Channels: 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.Large-Conductance Calcium-Activated Potassium Channel alpha Subunits: The pore-forming subunits of large-conductance calcium-activated potassium channels. They form tetramers in CELL MEMBRANES.Ryanodine Receptor Calcium Release Channel: 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.Anions: Negatively charged atoms, radicals or groups of atoms which travel to the anode or positive pole during electrolysis.Binding Sites: The parts of a macromolecule that directly participate in its specific combination with another molecule.Receptors, Nicotinic: One of the two major classes of cholinergic receptors. Nicotinic receptors were originally distinguished by their preference for NICOTINE over MUSCARINE. They are generally divided into muscle-type and neuronal-type (previously ganglionic) based on pharmacology, and subunit composition of the receptors.Peptides: 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.omega-Agatoxin IVA: A neuropeptide toxin from the venom of the funnel web spider, Agelenopsis aperta. It inhibits CALCIUM CHANNELS, P-TYPE by altering the voltage-dependent gating so that very large depolarizations are needed for channel opening. It also inhibits CALCIUM CHANNELS, Q-TYPE.Myocardium: 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.Gramicidin: 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.HEK293 Cells: A cell line generated from human embryonic kidney cells that were transformed with human adenovirus type 5.KCNQ2 Potassium Channel: A very slow opening and closing voltage-gated potassium channel that is expressed in NEURONS and is commonly mutated in BENIGN FAMILIAL NEONATAL CONVULSIONS.Rabbits: 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.Biophysics: The study of PHYSICAL PHENOMENA and PHYSICAL PROCESSES as applied to living things.Cell Membrane Permeability: A quality of cell membranes which permits the passage of solvents and solutes into and out of cells.Calcium Channels, Q-Type: CALCIUM CHANNELS located in the neurons of the brain.Protein Conformation: 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).Calcium Channels, R-Type: CALCIUM CHANNELS located in the neurons of the brain. They are inhibited by the marine snail toxin, omega conotoxin MVIIC.Antihypertensive Agents: Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS.Anti-Arrhythmia Agents: 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.Nerve Tissue ProteinsMembrane Proteins: 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.Cesium: 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.Isradipine: A potent antagonist of CALCIUM CHANNELS that is highly selective for VASCULAR SMOOTH MUSCLE. It is effective in the treatment of chronic stable angina pectoris, hypertension, and congestive cardiac failure.Decanoic Acids: 10-carbon saturated monocarboxylic acids.Pinacidil: 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)Sodium Channel Agonists: A class of drugs that stimulate sodium influx through cell membrane channels.Lidocaine: 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.Voltage-Gated Sodium Channel Blockers: A class of drugs that inhibit the activation of VOLTAGE-GATED SODIUM CHANNELS.Biophysical Phenomena: The physical characteristics and processes of biological systems.Electrophysiological Phenomena: 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.Azetidinecarboxylic Acid: A proline analog that acts as a stoichiometric replacement of proline. It causes the production of abnormal proteins with impaired biological activity.KCNQ3 Potassium Channel: 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.Hydroxy Acids: Organic compounds containing both the hydroxyl and carboxyl radicals.Structure-Activity Relationship: 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.Heart: The hollow, muscular organ that maintains the circulation of the blood.Transfection: 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.Receptors, Drug: 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.Mutagenesis, Site-Directed: Genetically engineered MUTAGENESIS at a specific site in the DNA molecule that introduces a base substitution, or an insertion or deletion.NAV1.2 Voltage-Gated Sodium Channel: 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.Voltage-Gated Sodium Channels: 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.Flufenamic Acid: An anthranilic acid derivative with analgesic, anti-inflammatory, and antipyretic properties. It is used in musculoskeletal and joint disorders and administered by mouth and topically. (From Martindale, The Extra Pharmacopoeia, 30th ed, p16)Signal Transduction: 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.Enzyme Inhibitors: Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.Sulfonylurea Receptors: 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.Calcium Signaling: Signal transduction mechanisms whereby calcium mobilization (from outside the cell or from intracellular storage pools) to the cytoplasm is triggered by external stimuli. Calcium signals are often seen to propagate as waves, oscillations, spikes, sparks, or puffs. The calcium acts as an intracellular messenger by activating calcium-responsive proteins.Magnesium: 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.Membrane Transport Modulators: Agents that affect ION PUMPS; ION CHANNELS; ABC TRANSPORTERS; and other MEMBRANE TRANSPORT PROTEINS.Benzimidazoles: Compounds with a BENZENE fused to IMIDAZOLES.Muscle, Smooth, Vascular: The nonstriated involuntary muscle tissue of blood vessels.Mechanotransduction, Cellular: The process by which cells convert mechanical stimuli into a chemical response. It can occur in both cells specialized for sensing mechanical cues such as MECHANORECEPTORS, and in parenchymal cells whose primary function is not mechanosensory.Quaternary Ammonium Compounds: Derivatives of ammonium compounds, NH4+ Y-, in which all four of the hydrogens bonded to nitrogen have been replaced with hydrocarbyl groups. These are distinguished from IMINES which are RN=CR2.Chelating Agents: Chemicals that bind to and remove ions from solutions. Many chelating agents function through the formation of COORDINATION COMPLEXES with METALS.Myocytes, Cardiac: Striated muscle cells found in the heart. They are derived from cardiac myoblasts (MYOBLASTS, CARDIAC).Acetylcholine: A neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system.Protein Binding: 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.Cromakalim: 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)Dogs: 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)Cricetinae: A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.Adrenergic beta-Antagonists: Drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. Adrenergic beta-antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches, and anxiety.Amantadine: An antiviral that is used in the prophylactic or symptomatic treatment of influenza A. It is also used as an antiparkinsonian agent, to treat extrapyramidal reactions, and for postherpetic neuralgia. The mechanisms of its effects in movement disorders are not well understood but probably reflect an increase in synthesis and release of dopamine, with perhaps some inhibition of dopamine uptake.Recombinant Proteins: Proteins prepared by recombinant DNA technology.Hippocampus: A curved elevation of GRAY MATTER extending the entire length of the floor of the TEMPORAL HORN of the LATERAL VENTRICLE (see also TEMPORAL LOBE). The hippocampus proper, subiculum, and DENTATE GYRUS constitute the hippocampal formation. Sometimes authors include the ENTORHINAL CORTEX in the hippocampal formation.
(1/10) Synthesis, structure-activity relationship, and pharmacological profile of analogs of the ASIC-3 inhibitor A-317567.

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(2/10) Acid sensing ion channel 1 in lateral hypothalamus contributes to breathing control.

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(3/10) The pharmacology and therapeutic potential of small molecule inhibitors of acid-sensing ion channels in stroke intervention.

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(4/10) Cyclisation increases the stability of the sea anemone peptide APETx2 but decreases its activity at acid-sensing ion channel 3.

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(5/10) Functional expression in Escherichia coli of the disulfide-rich sea anemone peptide APETx2, a potent blocker of acid-sensing ion channel 3.

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(6/10) Acid-sensing ion channels contribute to chemosensitivity of breathing-related neurons of the nucleus of the solitary tract.

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(7/10) u-PA inhibitor amiloride suppresses peritoneal metastasis in gastric cancer.

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(8/10) Targeting ASIC1 in primary progressive multiple sclerosis: evidence of neuroprotection with amiloride.

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*  Voltage-gated calcium channel
04, January 2009, 2009 BIOTREND Chemicals AG "Voltage-Gated Ion Channels". IUPHAR Database of Receptors and Ion Channels. ... the R-type channel (R stands for Resistant to the other blockers and toxins, except SNX-482) involved in poorly defined ... The α1 subunit forms the Ca2+ selective pore, which contains voltage-sensing machinery and the drug/toxin-binding sites. A ... Until very recently, the interaction between a highly conserved 18-amino acid region on the α1 subunit intracellular linker ...
*  Ligand-gated ion channel
... calcium channel Calcium-activated potassium channel Cyclic nucleotide-gated ion channel Acid-sensing ion channel Ryanodine ... Many LICs are additionally modulated by allosteric ligands, by channel blockers, ions, or the membrane potential. LICs are ... In contrast to ligand-gated ion channels, there are also receptor systems in which the receptor and the ion channel are ... If these receptors are ligand-gated ion channels, a resulting conformational change opens the ion channels, which leads to a ...
*  Epithelial sodium channel
Jasti J, Furukawa H, Gonzales EB, Gouaux E (2007). "Structure of acid-sensing ion channel 1 at 1.9 Å resolution and low pH". ... Amiloride and triamterene are potassium-sparing diuretics that act as epithelial sodium channel blockers. ... The epithelial sodium channel (short: ENaC, also: amiloride-sensitive sodium channel) is a membrane-bound ion channel that is ... but ENaC is very likely to be a heterotrimeric protein like the recently analyzed acid-sensing ion channel 1 (ASIC1), which ...
*  Three-finger toxin
"Black mamba venom peptides target acid-sensing ion channels to abolish pain". Nature. 490 (7421): 552-555. doi:10.1038/ ... Another class, called the beta-cardiotoxins, causes decreased heart rate and are thought to function as beta blockers, ... the mambalgin family of 3FTx proteins interacts with acid-sensing ion channels to produce analgesia without apparent toxic ... a family of ligand-gated ion channels. 3FTx binding interferes with cholinergic intercellular signaling particularly at ...
*  Pandinus imperator (Pi3) toxin
Pore blockers bind to pore of the ion channel and block the ion flux. Pi3 has a higher dissociation constant than Pi2. Pi3 has ... Lack of three residues in the amino acid terminal has been implicated in the inability of Pi3 and Pi2 to block BK channels. No ... channels in human lymphocytes suggests that the toxin exerts its effect by binding to some external domain and does not sense ... The Pi3 toxin is a potent inhibitor of the Kv1.2 potassium channel, encoded by the KCNA2 gene and a less potent blocker of ...
*  Drug design
... or ion channel openers or blockers) will be designed that are complementary to the binding site of target. Small molecules ( ... In the most basic sense, drug design involves the design of molecules that are complementary in shape and charge to the ... A biomolecular target (most commonly a protein or nucleic acid) is a key molecule involved in a particular metabolic or ...
*  Psychopharmacology
... inhibit voltage-sensitive calcium ion channels, and activate potassium ion channels. Many CB1 receptors are located on axon ... The amino-acid L-tryptophan is also available OTC, and seems to be free of dependence or abuse liability. However, it is not as ... This is followed by a plateau phase, where the subjective sense of time begins to slow and the visual effects increase in ... All proven antipsychotics are postsynaptic dopamine receptor blockers (dopamine antagonists). For an antipsychotic to be ...
*  Nav1.7
... is a sodium ion channel that in humans is encoded by the SCN9A gene. It is usually expressed at high levels in two types ... non-selective Nav channel blocker which is under development for the treatment of pain. Surprisingly, many potent Nav1.7 ... Nav1.7 is present at the endings of pain-sensing nerves, the nociceptors, close to the region where the impulse is initiated. ... erythromelalgia mutations that are observed are missense mutations that change important and highly conserved amino acid ...
*  Hanatoxin
Recovery from the bite usually takes about a week (Tintinalli 2004). Due to its specificity for particular ion-channels, ... voltage-gated potassium channels. The S3-S4 link, where hanatoxin binds, is important for voltage-sensing and gate activation. ... HaTx is a peptide consisting of the following 35 amino-acids: Glu-Cys-Arg-Tyr-Leu-Phe-Gly-Gly-Cys-Lys-Thr-Thr-***-Asp-Cys-Cys- ... Herrington, J. e.a. (2006). "Blockers of the Delayed-Rectifier Potassium Current in Pancreatic β-Cells Enhance Glucose- ...
*  Potassium channel
... blockers inhibit the flow of potassium ions through the channel. They either compete with potassium binding ... "A neuronal two P domain K+ channel stimulated by arachidonic acid and polyunsaturated fatty acids". The EMBO Journal. 17 (12): ... Duprat F, Lesage F, Fink M, Reyes R, Heurteaux C, Lazdunski M (Sep 1997). "TASK, a human background K+ channel to sense ... family Potassium uptake permease Sodium ion channel Calcium channel Littleton JT, Ganetzky B (Apr 2000). "Ion channels and ...
*  Glossary of diabetes
Calcium channel blocker Calcium ions are used in many cells, including beta cells, as a signaling mechanism. Since it does not ... Its amino acid code (DNA triplet --> amino acid incorporation) is identical across all Terrestrial life except for a very few ... In that sense, they are catalysts. Epidemiology the study of the transmission of diseases. One of the first epidemiological ... A Ca+ channel blocker is a drug which interferes with the operation of (some?) such channels. They have widespread effects, ...
*  Transient receptor potential calcium channel family
2F37​ Transient receptor potential cation channel subfamily A member 1: PDB: 3J9P​ Voltage-gated ion channel Ion channel ... Voltage sensing in thermo-TRP channels has been reviewed by Brauchi et al. TRP channels have six TMS helices. These channels ... They found that charged sodium-channel blockers can be targeted into nociceptors by the application of TRPV1 agonists to ... based on their amino acid sequence homology: the canonical or classic TRPs, the vanilloid receptor TRPs, the melastatin or long ...
*  Dysgeusia
There are few case reports claiming calcium channel blockers like Amlodipine also cause dysguesia by blocking calcium sensitive ... The distortion in the sense of taste is the only symptom, and diagnosis is usually complicated since the sense of taste is tied ... Alpha lipoic acid (ALA) is an antioxidant that is made naturally by human cells. It can also be administered in capsules or can ... Metronidazole and chlorhexidine have been found to interact with metal ions that associate with the cell membrane. Drugs that ...
*  Vanillotoxin
ICK toxins are best known as blockers of cation channels. The exact structure of the VaTxs has not yet been deduced, although ... Despite the similar architecture of TRPV1 and Kv2, VaTx1 and VaTx2 bind to the voltage-sensing domain of Kv2 rather than the ... Siemens J (2006). "Ion Spider toxins activate the capsaicin receptor to produce inflammatory pain". Nature. 444 (7116): 208-212 ... VaTxs are 53-82% identical in amino acid sequence. VaTx1 and VaTx2 have an almost identical structure, while VaTx3 shows some ...
*  Aldosterone
... ions into the urine (lumen of collecting duct). Aldosterone upregulates epithelial sodium channels (ENaCs) in the collecting ... which suggests that Ca2+ channel blockers may directly influence the adrenocortical biosynthesis of aldosterone in vivo. The ... An increase in sensed pressure results in an increased rate of firing by the baroreceptors and a negative feedback response, ... Liquorice, which contains glycyrrhetinic acid, can inhibit 11β-HSD and lead to a mineralocorticoid excess syndrome. Angiotensin ...
*  Methamphetamine
... to open the ion channel. Image legend Ion channel G proteins & linked receptors (Text color) Transcription factors United ... benzoic acid, hippuric acid, norephedrine, and phenylacetone, the metabolites of amphetamine. Among these metabolites, the ... Beta blockers with lipophilic properties and CNS penetration such as metoprolol and labetalol may be useful for treating CNS ... decreased sense of fatigue, insomnia or wakefulness, self-confidence, sociability, irritability, restlessness, grandiosity and ...
*  Soluble adenylyl cyclase
The anionic sAC inhibitor 4,4′-diisothiocyanatostilbene-2,2′-disulfonic acid (DIDS) acts as a blocker for the entrance to ... When the second metal - a Mg2+ ion - binds to the α-phosphate of ATP leads to a conformational change of the enzyme: the close ... Bone density experiments in mouse calvaria cultured indicates that HCO−3-sensing sAC is a physiological appropriate regulator ... Calcium enters by voltage-dependent Ca2+ channels or by release from the endoplasmic reticulum. Hydrogencarbonate and calcium ...
*  Neuropsychopharmacology
... resides with the trans-membrane ion channels which control the membrane currents via the ions K+, Na+, and Ca++, and of lesser ... An example is the push for better anti-anxiety agents (anxiolytics) based on GABAA(α2) agonists, CRF1 blockers, and 5HT2c ... each a chain of many amino acids. Transmitters typically bind at the junction between two of these proteins, on the parts that ... can produce confusing or ambiguous secondary effects so that the effects of a lack of receptor can be studied in a purer sense ...
*  TRPM5
... a poor selectivity between TRPM4 and TRPM5 or other ion channels. TPPO or TriPhenylPhosphineOxide is the most selective blocker ... "Extracellular acid block and acid-enhanced inactivation of the Ca2+-activated cation channel TRPM5 involve residues in the S3- ... "Differential effects of bitter compounds on the taste transduction channels TRPM5 and IP3 receptor type 3". Chemical senses. 39 ... Selective blocking agents of TRPM5 ion channels can be used to identify TRPM5 currents in primary cells. Most identified ...
*  Ion channel
... acid sensing ion channels (ASICs), ATP-gated P2X receptors, and the anion-permeable γ-aminobutyric acid-gated GABAA receptor. ... A variety of inorganic and organic molecules can modulate ion channel activity and conductance. Some commonly used blockers ... transport Potassium ion channels Sodium ion channel Synthetic ion channels Transmembrane receptor MeSH entry for Ion channels ... ion channels are a frequent target. There are over 300 types of ion channels just in the cells of the inner ear. Ion channels ...
*  Nav1.8
... is a sodium ion channel subunit that in humans is encoded by the SCN10A gene. Nav1.8-containing channels are ... a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat". Proceedings of ... Nav1.8 and Nav1.9 are both expressed in nociceptors (damage-sensing neurons). Nav1.7, Nav1.8 and Nav1.9 are found in the DRG ... It has been shown using the yeast-two hybrid screening method that p11 binds to a 28-amino-acid fragment at the N terminus of ...
*  Irritable bowel syndrome
... by signaling through a receptor or ligand-gated ion channel that has not been identified as of 2015. A 2015 review noted that ... Bile acid malabsorption is also sometimes missed in patients with diarrhea-predominant IBS. SeHCAT tests suggest around 30% of ... Domperidone, a dopamine receptor blocker and a parasympathomimetic, has been shown to reduce bloating and abdominal pain as a ... Most clinical studies show probiotics do not improve straining, sense of incomplete evacuation, stool consistency, fecal ...
*  Mechanism of anoxic depolarization in the brain
... channels, and acid-sensing ion channels (ASICs). During brain ischemia, glutamate is released in excess from the presynaptic ... and ion channel blockers, to prevent excessive ion fluxes.[citation needed] Brain ischemia Penumbra Weilinger NL, Maslieieva V ... An electrical signal is mediated by the sodium channels and leaky potassium channels in which intracellular K+ ion ... A neuron has a resting membrane potential of -70mV due to the leaky potassium channels. As a neuron depolarizes due to Na+ ion ...
*  Allodynia
They include: Dynamic mechanical allodynia - compounds targeting different ion channels; opioids Mexiletine Lidocaine (IV/ ... sodium channel blockers, opioids Lidocaine (IV) Alfentanil (IV) Adenosine (IV) Ketamine (IV) Glycine antagonist Venlafaxine ... Alique M, Herrero JF, Lucio-Cazana FJ (2007). "All-trans retinoic acid induces COX-2 and prostaglandin E2 synthesis in SH-SY5Y ... In healthy individuals, nociceptors sense information about cell stress or damage and temperature at the skin and transmit it ...
*  Type three secretion system
The bacteria sense such cues as temperature, pH, osmolarity and oxygen levels, and use them to "decide" whether to activate ... This is done in order to define the function of specific amino acids or regions in a protein. The introduction of a gene or a ... Cordes FS, Komoriya K, Larquet E, Yang S, Egelman EH, Blocker A, Lea SM (2003). "Helical structure of the needle of the type ... The bacteria are able to know where they are thanks to the different ions present in these regions; the ileum contains formate ...
*  Natural product
A more recent example is the N-type calcium channel blocker ziconotide analgesic which is based on a cyclic peptide cone snail ... are condensed by fatty acid synthase to produce fatty acids. Fatty acid are essential components of lipid bilayers that form ... ion channels, and enzymes. In some cases, they have also served as leads in the development of novel drugs. For example, ... In the broadest sense, natural products include any substance produced by life. Natural products can also be prepared by ...
Diminazene Is a Slow Pore Blocker of Acid-Sensing Ion Channel 1a (ASIC1a) | Molecular Pharmacology  Diminazene Is a Slow Pore Blocker of Acid-Sensing Ion Channel 1a (ASIC1a) | Molecular Pharmacology
Diminazene Is a Slow Pore Blocker of Acid-Sensing Ion Channel 1a (ASIC1a). Axel Schmidt, Giulia Rossetti, Sylvia Joussen and ... Diminazene Is a Slow Pore Blocker of Acid-Sensing Ion Channel 1a (ASIC1a). Axel Schmidt, Giulia Rossetti, Sylvia Joussen and ... Diminazene Is a Slow Pore Blocker of Acid-Sensing Ion Channel 1a (ASIC1a). Axel Schmidt, Giulia Rossetti, Sylvia Joussen and ... Diminazene Is a Slow Pore Blocker of Acid-Sensing Ion Channel 1a (ASIC1a) ...
more infohttp://molpharm.aspetjournals.org/content/early/2017/10/12/mol.117.110064
Epithelial Sodium Channel (ENaC) as a Novel Mechanism for Hypertension and Volume Expansion in Type 2 Diabetes - Full Text View...  Epithelial Sodium Channel (ENaC) as a Novel Mechanism for Hypertension and Volume Expansion in Type 2 Diabetes - Full Text View...
Acid Sensing Ion Channel Blockers. Sodium Channel Blockers. Membrane Transport Modulators. Molecular Mechanisms of ... Epithelial Sodium Channel (ENaC) as a Novel Mechanism for Hypertension and Volume Expansion in Type 2 Diabetes. The safety and ...
more infohttps://clinicaltrials.gov/ct2/show/NCT01804777?recr=Open&cond=%22Proteinuria%22&rank=11
The Effect of Amiloride and Spironolactone in Healthy Persons - Full Text View - ClinicalTrials.gov  The Effect of Amiloride and Spironolactone in Healthy Persons - Full Text View - ClinicalTrials.gov
Acid Sensing Ion Channel Blockers. Sodium Channel Blockers. Membrane Transport Modulators. Molecular Mechanisms of ...
more infohttps://clinicaltrials.gov/ct2/show/NCT00857909
A Category Names List - Drug Information Portal - U.S. National Library of Medicine  A Category Names List - Drug Information Portal - U.S. National Library of Medicine
Acid Sensing Ion Channel Blockers (2) • A subclass of sodium channel blockers that are specific for ACID-SENSING SODIUM ... CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS. MeSH ... Aromatic Amino Acid Decarboxylase Inhibitors (5) • Compounds and drugs that block or inhibit the enzymatic action of AROMATIC ... Anti-arrhythmia agents are often classed into four main groups according to their mechanism of action: sodium channel blockade ...
more infohttps://druginfo.nlm.nih.gov/drugportal/drug/categories
A Category Names List - Drug Information Portal - U.S. National Library of Medicine  A Category Names List - Drug Information Portal - U.S. National Library of Medicine
Acid Sensing Ion Channel Blockers (2) • A subclass of sodium channel blockers that are specific for ACID-SENSING SODIUM ... CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS. MeSH ... Aromatic Amino Acid Decarboxylase Inhibitors (5) • Compounds and drugs that block or inhibit the enzymatic action of AROMATIC ... Anti-arrhythmia agents are often classed into four main groups according to their mechanism of action: sodium channel blockade ...
more infohttps://druginfo.nlm.nih.gov/drugportal/jsp/drugportal/drugNamesAndCategories.jsp
Blockers | Alomone Labs  Blockers | Alomone Labs
Home › Products › Ion Channels › Na+ ChannelsAcid-Sensing Ion Channels (ASIC) › Blockers ... ASIC channels belong to the ENaC/Degenerin superfamily and are proton-gated ion channels which are not voltage-dependent. Six ... ASIC1 Channel Premium Research Pack. All You Need for ASIC1 Channel Research ... ASIC3 Channel Premium Research Pack. All You Need for ASIC3 Channel Research ...
more infohttps://www.alomone.com/c/blockers-acid-sensing-ion-channels-asic?show=immuno
Psalmotoxin-1 | Abcam  Psalmotoxin-1 | Abcam
... selective ASIC1a blocker. Join researchers using high quality Psalmotoxin-1 from Abcam and achieve your mission… ... Potent, selective acid sensing (proton gated) ion channel 1a (ASIC1a) blocker. Inhibits cation currents mediated by ASICs (IC50 ... The receptor site of the spider toxin PcTx1 on the proton-gated cation channel ASIC1a.. J Physiol 570:339-54 (2006). Read more ... A tarantula peptide against pain via ASIC1a channels and opioid mechanisms.. Nat Neurosci 10:943-5 (2007). Read more (PubMed: ...
more infohttp://www.abcam.com/psalmotoxin-1-ab120483.html
Find Research Outputs
             - UNT Health Science Center  Find Research Outputs - UNT Health Science Center
Basics on the use of acid-sensing ion channels' inhibitors as therapeutics. Dibas, J., Al-Saad, H. & Dibas, A., 1 Mar 2019, In ... Acid Sensing Ion Channel Blockers Acid Sensing Ion Channels Drug Repositioning Neuroprotective Agents ...
more infohttps://experts.unthsc.edu/en/publications/
河南快3开奖号码今天专家推测:Alomone-鈉離子通道  ! 產品專題 樂博生物-試  河南快3开奖号码今天专家推测:Alomone-鈉離子通道 ! 產品專題 樂博生物-試
TTX-Sensitive NaV Channel Blocker Explorer Kit. EK-105. Acid-Sensing Ion Channels (ASIC) Blockers ... 鈉離子通道主要分為電壓門控鈉離子通道(Voltage-Gated Sodium channels, VGSCs) 、酸質子門控鈉離子通道(Acid-Sensitive Ion channels, ASICs)和濃度門控鈉離子通道( ... 我們知道離子通道主要分為電壓門控離子通道(Voltage-Gated channels
more infohttp://www.robtp.com/article.php?id=250
New Products | Alomone Labs  New Products | Alomone Labs
Acid-Sensing Ion Channels (ASIC) / Blockers Release Date: 01/08/2019 * Anti-GLUT1 (extracellular)-FITC Antibody. A Rabbit ... Microglia Ion Channel Antibody Explorer Kit. A Screening Package of Antibodies to Ion Channels Expressed in Microglia ... Voltage-Gated Ca2+ Channels / Blockers Release Date: 09/09/2019 * Neural Stem Cell Culturing Kit. A Neural Stem Cell Culturing ... Voltage-Gated K+ Channels / Blockers Release Date: 11/07/2019 * Anti-N-Cadherin-ATTO-594 Antibody. A Rabbit Polyclonal Antibody ...
more infohttps://www.alomone.com/c/new-products?products=all
David C. Yeomans | Stanford Medicine Profiles  David C. Yeomans | Stanford Medicine Profiles
... acid-sensing ion channels (ASICs), and TRPV1 blocker as well as acidic buffer solutions to investigate and mimic the underlying ... They also used similar techniques to investigate the involvement of acid-sensing ion channels and Nav1.7 sodium channel in ... N-type calcium ion channel blockers, such as omega-conotoxin GVIA (omega-CTX), produce analgesia by impeding flux of calcium ... The combined effects of N-type calcium channel blockers and morphine on A delta versus C fiber mediated nociception ANESTHESIA ...
more infohttps://med.stanford.edu/profiles/david-yeomans
Professor Alan Mark - UQ Researchers  Professor Alan Mark - UQ Researchers
Development of potent and selective blockers of acid sensing ion channels for the treatment of pain ... A dynamic pharmacophore drives the interaction between psalmotoxin-1 and the putative drug target acid-sensing ion channel 1a ... The Binding of the Spider Toxin PcTx1 to the Acid Sensing Ion Channel (ASIC) 1a. Journal of Chemical Information and Modeling, ... A dynamic pharmacophore drives the interaction between psalmotoxin-1 and the putative drug target acid-sensing ion channel 1a. ...
more infohttps://researchers.uq.edu.au/researcher/1469
Professor Glenn King - UQ Researchers  Professor Glenn King - UQ Researchers
Development of selective blockers of acid sensing ion channel 1a for the treatment of stroke ... Developing subtype-selective blockers of acid-sensing ion channels for treating peripheral pain ... Development of potent and selective blockers of acid sensing ion channels for the treatment of pain ... a potent blocker of acid-sensing ion channel 3. Marine Drugs, 10 7: 1605-1618. doi:10.3390/md10071605 ...
more infohttp://researchers.uq.edu.au/researcher/1593
Proton‐independent activation of acid‐sensing ion channel 3 by an alkaloid, lindoldhamine, from Laurus nobilis, British Journal...  Proton‐independent activation of acidsensing ion channel 3 by an alkaloid, lindoldhamine, from Laurus nobilis, British Journal...
... sensing ion channel 3 by an alkaloid, lindoldhamine, from Laurus nobilis, British Journal of Pharmacology" on DeepDyve, the ... Monoamine NMDA receptor channel blockers inhibit and potentiate native and recombinant proton‐gated ion channels ... Nonproton ligand sensing domain is required for paradoxical stimulation of acidsensing ion channel 3 (ASIC3) channels by ... sensing ion channel 3 by an alkaloid, lindoldhamine, from Laurus nobilis. Proton‐independent activation of acidsensing ion ...
more infohttps://www.deepdyve.com/lp/wiley/proton-independent-activation-of-acid-sensing-ion-channel-3-by-an-cQm7jS0sNo
Marine Drugs - ISSN: 1660-3397  Marine Drugs - ISSN: 1660-3397
... a Potent Blocker of Acid-Sensing Ion Channel 3 Author(s): Raveendra Anangi , Lachlan D. Rash , Mehdi Mobli , Glenn F. King. ... Cyclisation Increases the Stability of the Sea Anemone Peptide APETx2 but Decreases Its Activity at Acid-Sensing Ion Channel 3 ... Cytotoxic Anthranilic Acid Derivatives from Deep Sea Sediment-Derived Fungus Penicillium paneum SD-44 Author(s): Chun-Shun Li ... Use of Okadaic Acid to Identify Relevant Phosphoepitopes in Pathology: A Focus on Neurodegeneration Author(s): Miguel Medina , ...
more infohttp://journaldatabase.info/journal/issn1660-3397
Acid-sensing ion channels: potential therapeutic targets for neurologic diseases | Translational Neurodegeneration | Full Text  Acid-sensing ion channels: potential therapeutic targets for neurologic diseases | Translational Neurodegeneration | Full Text
In disease states, tissue acidosis is a common pathologic change causing abnormal activation of acid-sensing ion channels ( ... a potent blocker of acid-sensing ion channel 3. Mar Drugs. 2012;10(7):1605-18.View ArticlePubMed CentralPubMedGoogle Scholar. ... Gonzales EB, Kawate T, Gouaux E. Pore architecture and ion sites in acid-sensing ion channels and P2X receptors. Nature. 2009; ... Structure, function, and pharmacology of acid-sensing Ion channels and the epithelial Na + channel. Pharmacol Rev. 2015;67(1):1 ...
more infohttps://translationalneurodegeneration.biomedcentral.com/articles/10.1186/s40035-015-0031-3
The acid-sensing ion channel ASIC1a mediates striatal synapse remodeling and procedural motor learning | Science Signaling  The acid-sensing ion channel ASIC1a mediates striatal synapse remodeling and procedural motor learning | Science Signaling
Amiloride (500 μM), the nonselective ASIC blocker, inhibited this component (Fig. 1, E and F), which was also largely absent in ... ASIC channels in motor learning. Members of the ASIC family of acid-sensing ion channels are abundant in various regions of the ... Proton-gated acid-sensing ion channels (ASICs) belong to the degenerin/epithelial Na+ channel (DEG/ENaC) superfamily (6) and ... structure, function, and pharmacology of acid-sensing ion channels and the epithelial Na+ channel. Pharmacol. Rev. 67, 1-35 ( ...
more infohttps://stke.sciencemag.org/content/11/542/eaar4481.full
Amiloride-sensitive Na+ channels contribute to regulatory volume increases in human glioma cells.  Amiloride-sensitive Na+ channels contribute to regulatory volume increases in human glioma cells.
This toxin is thought to be a specific peptide inhibitor of acid-sensing ion channel (ASIC1), a member of the Deg/ENaC ... Sodium Channel Blockers / pharmacology*. Sodium Channels / metabolism*. Spider Venoms / pharmacology. Water-Electrolyte Balance ... 0/PcTX1 protein, Psalmopoeus cambridgei; 0/Sodium Channel Blockers; 0/Sodium Channels; 0/Spider Venoms; 2609-46-3/Amiloride; ... In the present study, we investigated the potential role of this ion channel to mediate regulatory volume increase in glioma ...
more infohttp://www.biomedsearch.com/nih/Amiloride-sensitive-Na-channels-contribute/17615161.html
Abundant expression and functional participation of TRPV1 at Zusanli acupoint (ST36) in mice: mechanosensitive TRPV1 as an ...  Abundant expression and functional participation of TRPV1 at Zusanli acupoint (ST36) in mice: mechanosensitive TRPV1 as an ...
... and the acid-sensing ion channel 3 (ASIC3) are regarded as mechanosensitive channels. This study aimed to clarify their role at ... These findings suggest TRPV1 might act as acupuncture-responding channel by sensing physical stimulation from acupuncture and ... Second, immunofluorescence was performed at ST36 to reveal distribution pattern of the channels. Third, agonist of the channels ... and propose possible sensing pathways linking channel activation to neurological signaling. First, tissues from different ...
more infohttps://bmccomplementalternmed.biomedcentral.com/articles/10.1186/1472-6882-14-96
Acid-Sensing Ion Channels | Springer for Research & Development  Acid-Sensing Ion Channels | Springer for Research & Development
... brain sodium channel 1 (BNC1, BNaC1); ASIC2b: mammalian degenerin 2 (MDEG2); ASIC3:... ... brain sodium channel 2 (BNC2, BNaC2); ASIC1b: ASICβ; ASIC2a: mammalian degenerin 1 (MDEG1), ... 2001) Acid-Sensing Ion Channel 3 Matches the Acid-Gated Current in Cardiac Ischemia-Sensing Neurons. Proc Natl Acad Sci USA 98: ... Acid-Sensing Ion Channels (ASICs) are membrane protein complexes that form depolarizing ion channels present on peripheral and/ ...
more infohttps://rd.springer.com/referenceworkentry/10.1007/978-3-540-29805-2_35
Potent neuroprotection after stroke afforded by a double-knot spider-venom peptide that inhibits acid-sensing ion channel 1a |...  Potent neuroprotection after stroke afforded by a double-knot spider-venom peptide that inhibits acid-sensing ion channel 1a |...
Diminazene Is a Slow Pore Blocker of Acid-Sensing Ion Channel 1a (ASIC1a) ... Acid-sensing ion channel 1a (ASIC1a) is the primary acid sensor in mammalian brain and a key mediator of acidosis-induced ... Potent neuroprotection after stroke afforded by a double-knot spider-venom peptide that inhibits acid-sensing ion channel 1a. ... The precipitous drop in brain pH resulting from stroke activates acid-sensing ion channel 1a. We show that inhibition of these ...
more infohttp://www.pnas.org/content/early/2017/03/14/1614728114.short?rss=1
Epithelial sodium channel - Wikipedia  Epithelial sodium channel - Wikipedia
Jasti J, Furukawa H, Gonzales EB, Gouaux E (2007). "Structure of acid-sensing ion channel 1 at 1.9 Å resolution and low pH". ... Amiloride and triamterene are potassium-sparing diuretics that act as epithelial sodium channel blockers. ... The epithelial sodium channel (short: ENaC, also: amiloride-sensitive sodium channel) is a membrane-bound ion channel that is ... but ENaC is very likely to be a heterotrimeric protein like the recently analyzed acid-sensing ion channel 1 (ASIC1), which ...
more infohttps://en.wikipedia.org/wiki/Epithelial_sodium_channel
COMPOSITIONS AND METHODS FOR MODULATING THE ACID-SENSING ION CHANNEL     (ASIC) - Patent application  COMPOSITIONS AND METHODS FOR MODULATING THE ACID-SENSING ION CHANNEL (ASIC) - Patent application
0070] As used herein the term "ASIC receptor blocker" includes any compound which causes inhibition of the ASIC receptor. This ... the opening the acid-sensing ion channels of the DEG/ENaC channel family. In addition to the ASIC channels, it is expected that ... 0036] Acid-sensing ion channels (ASICs) are members of the DEG/ENaC superfamily of Na+ permeable channels, which includes the ... opening and/or closing of the acid-sensing ion channels can be used such as voltage-sensitive dyes or ion-sensitive dyes. An ...
more infohttp://www.patentsencyclopedia.com/app/20120015396
Ion channels | Pharmacology Education Project  Ion channels | Pharmacology Education Project
... diuretics amiloride and triamterene are ENaC channel blockers.. Acid-sensing (proton-gated) ion channels (ASICs) are involved ... Ligand-gated ion channels Ligand-gated ion channels (LGICs) mediate passive ion flux driven by the electrochemical gradient for ... GABAA and glycine receptors as well as acid-sensing (proton-gated) ion channels (ASICs), epithelial sodium channels (ENaC), IP3 ... Other ion channels Other ion channel families include the aquaporins (which also includes aquaglyceroporins), a family of ...
more infohttp://www.pharmacologyeducation.org/pharmacology/ion-channels
Ion channels | Pharmacology Education Project  Ion channels | Pharmacology Education Project
... diuretics amiloride and triamterene are ENaC channel blockers.. Acid-sensing (proton-gated) ion channels (ASICs) are involved ... Ligand-gated ion channels Ligand-gated ion channels (LGICs) mediate passive ion flux driven by the electrochemical gradient for ... GABAA and glycine receptors as well as acid-sensing (proton-gated) ion channels (ASICs), epithelial sodium channels (ENaC), IP3 ... Other ion channels Other ion channel families include the aquaporins (which also includes aquaglyceroporins), a family of ...
more infohttp://pharmacologyeducation.org/pharmacology/ion-channels
  • LICs are classified into three superfamilies which lack evolutionary relationship: cys-loop receptors, ionotropic glutamate receptors and ATP-gated channels. (wikipedia.org)
  • A binding site in the extracellular N-terminal ligand-binding domain gives them receptor specificity for (1) acetylcholine (AcCh), (2) serotonin, (3) glycine, (4) glutamate and (5) γ-aminobutyric acid (GABA) in vertebrates. (wikipedia.org)
  • When the acetylcholine binds it alters the receptor's configuration (twists the T2 helices which moves the leucine residues, which block the pore, out of the channel pathway) and causes the constriction in the pore of approximately 3 angstroms to widen to approximately 8 angstroms so that ions can pass through. (wikipedia.org)
  • Nevertheless, this intracellular loop appears to function in desensitization, modulation of channel physiology by pharmacological substances, and posttranslational modifications. (wikipedia.org)
  • Ligand-gated ion channels (LICs, LGIC), also commonly referred as ionotropic receptors, are a group of transmembrane ion-channel proteins which open to allow ions such as Na+, K+, Ca2+, and/or Cl− to pass through the membrane in response to the binding of a chemical messenger (i.e. a ligand), such as a neurotransmitter. (wikipedia.org)
  • These proteins are typically composed of at least two different domains: a transmembrane domain which includes the ion pore, and an extracellular domain which includes the ligand binding location (an allosteric binding site). (wikipedia.org)
  • With a sufficient number of channels opening at once, the inward flow of positive charges carried by Na+ ions depolarizes the postsynaptic membrane sufficiently to initiate an action potential. (wikipedia.org)
  • The receptors are subdivided with respect to the type of ion that they conduct (anionic or cationic) and further into families defined by the endogenous ligand. (wikipedia.org)
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