Acid sensing ion channel blockers. Medical search

A subclass of sodium channel blockers that are specific for ACID-SENSING SODIUM CHANNELS.

An anticonvulsant especially useful in the treatment of absence seizures unaccompanied by other types of seizures.

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

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

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

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.

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.

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

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

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

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

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

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 whose activation is dependent on intracellular calcium concentrations.

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.

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 subclass of ion channels that open or close in response to the binding of specific LIGANDS.

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

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

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

A 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.

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

A 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.

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

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

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.

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

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

A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.

A calcium channel blocker that is a class IV anti-arrhythmia agent.

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.

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 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.

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

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

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.

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

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

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.

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

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

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

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.

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.

Benzoic acid or benzoic acid esters substituted with one or more nitro groups.

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 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.

The rate dynamics in chemical or physical systems.

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.

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.

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

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

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.

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

A 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.

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

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

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

A benzimidazoyl-substituted tetraline that selectively binds and inhibits CALCIUM CHANNELS, T-TYPE.

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

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

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.

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.

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

A 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.

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

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

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.

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.

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.

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.

Established cell cultures that have the potential to propagate indefinitely.

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

A long-acting dihydropyridine calcium channel blocker. It is effective in the treatment of ANGINA PECTORIS and HYPERTENSION.

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

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.

A calcium channel blockader with preferential cerebrovascular activity. It has marked cerebrovascular dilating effects and lowers blood pressure.

An analgesic and anti-inflammatory agent used in the treatment of rheumatoid arthritis.

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)

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

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.

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.

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

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

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.

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.

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.

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.

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.

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.

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)

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

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.

An inhibitor of anion conductance including band 3-mediated anion transport.

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

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.

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

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

A 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.

Use of electric potential or currents to elicit biological responses.

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

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

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

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.

Negatively charged atoms, radicals or groups of atoms which travel to the anode or positive pole during electrolysis.

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

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.

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.

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.

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

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

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

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 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.

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

A quality of cell membranes which permits the passage of solvents and solutes into and out of cells.

CALCIUM CHANNELS located in the neurons of the brain.

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

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.

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.

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 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.

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.

10-carbon saturated monocarboxylic acids.

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

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

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 class of drugs that inhibit the activation of VOLTAGE-GATED SODIUM CHANNELS.

The physical characteristics and processes of biological systems.

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.

A proline analog that acts as a stoichiometric replacement of proline. It causes the production of abnormal proteins with impaired biological activity.

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.

Organic compounds containing both the hydroxyl and carboxyl radicals.

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.

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.

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.

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

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.

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.

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)

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.

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

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.

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.

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.

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

Compounds with a BENZENE fused to IMIDAZOLES.

The nonstriated involuntary muscle tissue of blood vessels.

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.

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.

Chemicals that bind to and remove ions from solutions. Many chelating agents function through the formation of COORDINATION COMPLEXES with METALS.

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

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.

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

A 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)

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

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.

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.

Proteins prepared by recombinant DNA technology.

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.

Synthesis, structure-activity relationship, and pharmacological profile of analogs of the ASIC-3 inhibitor A-317567. (1/10)

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

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

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

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

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

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... pan-acid-sensing ion channel (ASIC) inhibitor that prevents the transient flow of ions but not the sustained flow of ions. ... or an angiotensin II receptor blocker (ARB), and a calcium channel blocker, the addition of amiloride (or spironolactone) was ... "Acid-sensing ion channels: dual function proteins for chemo-sensing and mechano-sensing". Journal of Biomedical Science. 25 (1 ... structure, function, and pharmacology of acid-sensing ion channels and the epithelial Na+ channel". Pharmacological Reviews. 67 ...

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

... the mambalgin family of 3FTx proteins interacts with acid-sensing ion channels to produce analgesia without apparent toxic ... Another class, called the beta-cardiotoxins, causes decreased heart rate and are thought to function as beta blockers, ... "Black mamba venom peptides target acid-sensing ion channels to abolish pain". Nature. 490 (7421): 552-5. Bibcode:2012Natur.490 ... a family of ligand-gated ion channels. 3FTx binding interferes with cholinergic intercellular signaling particularly at ...

https://en.wikipedia.org/wiki/Three-finger_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 ...

https://en.wikipedia.org/wiki/Pandinus_imperator_(Pi3)_toxin

Both endogenous and exogenous inverse agonists have been identified, as have drugs at ligand gated ion channels and at G ... The beta blockers carvedilol and bucindolol have been shown to be low level inverse agonists at beta adrenoceptors. Agonist ... of GABAergic transmission in cultured spinal cord neurons involves gamma-aminobutyric acid voltage-gated chloride channels". ... Berg, Kelly A; Clarke, William P (2018-08-06). "Making Sense of Pharmacology: Inverse Agonism and Functional Selectivity". ...

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

"A proton-gated cation channel involved in acid-sensing". Nature. Springer Science and Business Media LLC. 386 (6621): 173-177. ... He played a pioneering role in the analysis of ion channels permeable to sodium, calcium and potassium. He played a pioneering ... calcium blockers) or diabetes (antidiabetic sulfonylureas) The most recent work of his team has completed these pharmacological ... TREK/TRAAK channels, TASK channels and ASIC channels. These families of channels play an essential role in pain perception but ...

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... 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 a nucleic acid) is a key molecule involved in a particular metabolic or ...

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... potassium channel blocker and potassium channel opener. Ion channel Ion channel family Potassium channel tetramerisation domain ... Specific domains of the channel subunits have been identified that are responsible for voltage-sensing and converting between ... They include the amino acid sequence (Thr-Val-Gly-Tyr-Gly) or (Thr-Val-Gly-Phe-Gly) typical to the selectivity filter of ... preventing ion movement through the channel. For blockers and activators of voltage gated potassium channels see: ...

https://en.wikipedia.org/wiki/Voltage-gated_potassium_channel

April 2011). "Fenamates as TRP channel blockers: mefenamic acid selectively blocks TRPM3". British Journal of Pharmacology. 162 ... Quallo T, Alkhatib O, Gentry C, Andersson DA, Bevan S (August 2017). "G protein βγ subunits inhibit TRPM3 ion channels in ... Held K, Voets T, Vriens J (2014). "TRPM3 in temperature sensing and beyond". Temperature. 2 (2): 201-13. doi:10.4161/ ... TRP channels are Ca2+ permeable non-selective cation channels that play roles in a wide variety of physiological processes, ...

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... 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 (September 1997). "TASK, a human background K+ channel to sense ... Calcium channel - Ion channel complex through which calcium ions pass Inward-rectifier potassium ion channel Potassium in ...

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

... 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 ...

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... 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 ...

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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 ...

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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 ...

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To sense the cell's voltage, the S1-S3 helices contain many negatively charged amino acids while S4 helices contain mostly ... "Voltage-Gated Calcium Channels". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... L-type calcium channel blocker drugs are used as cardiac antiarrhythmics or antihypertensives, depending on whether the drugs ... The L-type calcium channel (also known as the dihydropyridine channel, or DHP channel) is part of the high-voltage activated ...

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... and also because myotonia congenita is an ion channel disorder, and ion channels are sensitive to internal and external ... a blocker of chloride channels. It is also possible to achieve myotonia in preparations of intact isolated muscle by greatly ... The term congenital in its sense of "clinically apparent from birth" applies only to Thomsen disease, as the clinical onset of ... Substituted benzoic acids". Journal of Medicinal Chemistry. 11 (5): 1020-2. doi:10.1021/jm00311a023. PMID 5697062. Villegas- ...

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The cryoEM structure of ENaC indicates that the channel is a heterotrimeric protein like the acid-sensing ion channel 1 (ASIC1 ... Amiloride and triamterene are potassium-sparing diuretics that act as epithelial sodium channel blockers. Noreng S, Bharadwaj A ... Jasti J, Furukawa H, Gonzales EB, Gouaux E (September 2007). "Structure of acid-sensing ion channel 1 at 1.9 A resolution and ... The epithelial sodium channel (ENaC), (also known as amiloride-sensitive sodium channel) is a membrane-bound ion channel that ...

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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, ...

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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 ...

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... resides with the transmembrane ion channels which control the membrane currents via the ions K+, Na+, and Ca++, and of lesser ... Different treatment-related studies are investigating the potential role of peptide nucleic acids in treating Parkinson's ... DA blocker anti-psychotics, and GABA agonist tranquilizers (benzodiazepines). New endogenous chemicals are continually ... can produce confusing or ambiguous secondary effects so that the effects of a lack of receptor can be studied in a purer sense ...

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... 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 ...

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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 ... Rossetti T, Jackvony S, Buck J, Levin LR (April 2021). "Bicarbonate, carbon dioxide and pH sensing via mammalian bicarbonate- ... Wennemuth G, Carlson AE, Harper AJ, Babcock DF (April 2003). "Bicarbonate actions on flagellar and Ca2+ -channel responses: ...

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Duprat F, Lesage F, Fink M, Reyes R, Heurteaux C, Lazdunski M (Sep 1997). "TASK, a human background K+ channel to sense ... C. M. Armstrong (1971). "Interaction of tetraethylammonium ion derivatives with the potassium channels of giant axons." J. Gen ... an acid-sensitive two-pore domain potassium channel". Neuropharmacology. 40 (4): 551-9. doi:10.1016/S0028-3908(00)00189-1. PMID ... Potassium channel blockers are agents which interfere with conduction through potassium channels. Potassium channel blockers ...

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... 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 ...

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L-type Ca2+ channels, P/Q-type Ca2+ channels and sodium ion channels. All of these membrane channels can further influence ... Calmodulin (CaM) is a protein composed of 148 amino acids that plays both an intermediary and direct role in moderating gap ... Harris, Andrew L. (2002-02-01). "Voltage-sensing and Substate Rectification". Journal of General Physiology. 119 (2): 165-170. ... CaM-antagonist and CaM-blockers promote the opening of gap junctions. Chemical modification takes place on connexin proteins ...

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... binds to several types of voltage-gated ion channels. While the affinity is the highest for the Kv2.1 and Kv4.2 ... 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- ...

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"Voltage-Gated Ion Channels". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... 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 ...

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... permeant ion and/or channel blocker, mutations in the ion channel amino acids), can provide information regarding the ... Super-resolution microscopy Voltage clamp Tunable resistive pulse sensing Single molecule real time sequencing Roiter V, Minko ... interconversion of various kinetic states of the ion channel. In a minimal model for an ion channel, there are two states: open ... In addition, one of the earliest means of detecting single molecules, came about in the field of ion channels with the ...

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Many LICs are additionally modulated by allosteric ligands, by channel blockers, ions, or the membrane potential. LICs are ... Quorum sensing operates in both gram-positive and gram-negative bacteria, and both within and between species. In slime moulds ... Paracrine signals such as retinoic acid target only cells in the vicinity of the emitting cell. Neurotransmitters represent ... Ion channel linked receptors are a group of transmembrane ion-channel proteins which open to allow ions such as Na+, K+, Ca2+, ...

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... is an ion channel located on the plasma membrane of many human and animal cells. This ion channel is best known as a ... Other TRPA1 channel activators include JT-010 and ASP-7663, while channel blockers include A-967079, HC-030031 and AM-0902. The ... The epoxide, 5,6-epoxy-8Z,11Z,14Z-eicosatrienoic acid (5,6-EET) made by the metabolism of arachidonic acid by any one of ... Tai C, Zhu S, Zhou N (January 2008). "TRPA1: the central molecule for chemical sensing in pain pathway?". The Journal of ...

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... acid sensing ion channels (ASICs), ATP-gated P2X receptors, and the anion-permeable γ-aminobutyric acid-gated GABAA receptor. ... A variety of ion channel blockers (inorganic and organic molecules) can modulate ion channel activity and conductance. Some ... ion channels are a frequent target. There are over 300 types of ion channels just in the cells of the inner ear. Ion channels ... Ion channels may be classified by gating, i.e. what opens and closes the channels. For example, voltage-gated ion channels open ...

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... beta blockers (ICI Pharmaceuticals, 1964) ACE inhibitors, and angiotensin receptor blockers. ACE inhibitors reduce the risk of ... In 1903, Hermann Emil Fischer and Joseph von Mering disclosed their discovery that diethylbarbituric acid, formed from the ... The pharmaceutical marketing plan incorporates the spending plans, channels, and thoughts which will take the drug association ... Early developments in the field of treating hypertension included quaternary ammonium ion sympathetic nervous system blocking ...

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... 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 ...

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Blocker A, Jouihri N, Larquet E, Gounon P, Ebel F, Parsot C, et al. (February 2001). "Structure and composition of the Shigella ... 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 ... The bacteria are able to know where they are thanks to the different ions present in these regions; the ileum contains formate ...

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... selectivity is the preference of a channel to conduct a specific ion). The Voltage sensing domain and pore-gated domain are ... BK channels also function as a blocker in ischemia and are a focus in investigating its use as a therapy for stroke. There are ... bowl that consists of a series of Aspartic acid (Asp) residues that are located in the RCK2 domain. The Mg²⁺ binding site is ... In certain cancers gBK, a variant ion channel called glioma BK channel, can be found. It is known that BK channels do in some ...

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Ion channel toxins, Potassium channel blockers). ... Receptors On The Voltage Sensing Domain Of Herg K+ Channel By ... is a polypeptide composed of 42 amino acid residues. It has the following one-letter amino acid code: ... interference with channel gating through interaction with the voltage-sensing domain S1-S4. Ergtoxin blocks ERG-channels ... However, while hERG K+ channels are expressed by SK-OV-3 cancer cells, the specific mechanisms of channel function in ...

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... is an ion channel: upon activation, it allows the entry of Na+ and Ca2+ ions into the cell, which leads to depolarization ... September 2008). "AMTB, a TRPM8 channel blocker: evidence in rats for activity in overactive bladder and painful bladder ... Tetrahydrocannabinolic acid Cannabidiol Cannabidiolic acid Cannabigerol Tetrahydrocannabivarin Tetrahydrocannabivarin Acid ... These antagonists physically block the receptor for cold and menthol, by binding to the S1-S4 voltage-sensing domain, ...

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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.: Chapter 3 Fatty acid are essential components of lipid bilayers ... 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 ...

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... calcium channel blocker overdose, rhabdomyolysis, tumor lysis syndrome, and medications such as bisphosphonates or denosumab. ... of function mutations of the calcium-sensing receptor Foscarnet use Loop diuretic use Crohn disease High level of lactic acid ... Because a portion of both hydrogen ions and calcium are bound to serum albumin, when blood becomes alkalotic, the bound ... due to the decreased interaction of calcium with sodium channels. Since calcium blocks sodium channels and inhibits ...

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October 2015). "Sodium channel blockers for neuroprotection in multiple sclerosis". The Cochrane Database of Systematic Reviews ... Medications that influence voltage-gated sodium ion channels are under investigation as a potential neuroprotective strategy ... Moreover, fumaric acid is also used to treat psoriasis, another autoinmune disorder, and there is long term safety data from ... "Multidisciplinary Rehabilitation for MS". Making Sense of MS Research. Archived from the original on 8 April 2013. Retrieved 8 ...

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This chloride channel allows the negatively charged chloride ions into the neuron, causing a hyperpolarization which pushes the ... Strychnine is then formed by a facile addition of the amine with the carboxylic acid or its activated CoA thioester, followed ... February 2010). "The molecular receptive ranges of human TAS2R bitter taste receptors". Chemical Senses. 35 (2): 157-170. doi: ... Chloride channel blockers, Strychnine poisoning). ... along with tannic acid or potassium permanganate solutions to ...

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Bohlen, Christopher J. (17 November 2011). "A heteromeric Texas coral snake toxin targets acid-sensing ion channels to produce ... calcium channel blockers have been found in snakes, spiders, and cone snails, thus suggesting that venom exhibits convergent ...

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Altered expression of ion channels, changes in neurotransmitters and their receptors, as well as altered gene expression in ... Ziconotide is a voltage-gated calcium channel blocker which may be used in severe cases of ongoing neuropathic pain it is ... A 2007 review of studies found that injected (parenteral) administration of alpha lipoic acid (ALA) was found to reduce the ... The theory predicts that the activation of central pain inhibitory neurons by non-pain sensing neurons prevents the ...

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Acid Sensing Ion Channel Inhibitors Antagonists, ASIC Channel Blockers, ASIC Channel Channel Antagonists, ASIC Channel Blockers ... Acid Sensing Ion Channel Blockers Entry term(s). ASIC Blockers ASIC Channel Antagonists ASIC Channel Blockers ASIC Inhibitors ... ASIC Channel Blockers. ASIC Inhibitors. Acid Sensing Ion Channel Inhibitors. Antagonists, ASIC Channel. Blockers, ASIC Channel ... Acid Sensing Ion Channel Blockers - Preferred Concept UI. M0568873. Scope note. A subclass of sodium channel blockers that are ...

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... a response of muscle C-fibers to antagonists to acid-sensing ion channels (ASICs) in cultured dorsal root ganglion (DRG) ... channel blocker for pain in general and specifically for incisional pain needs further investigation. ... Acid-sensing ion channels in postoperative pain. J Neurosci 2011;31:6059-66.. ... 182]. Wei H, Karimaa M, Korjamo T, Koivisto A, Pertovaara A. Transient receptor potential ankyrin 1 ion channel contributes to ...

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... is a potent and selective blocker of acid-sensing ion channels (ASIC). ASIC channels have been demonstrated to be ... Acid-sensing ion channels (ASICs) are neuronal proton-gated cation channels associated with nociception, fear, depression, ... Black mamba venom peptides target acid-sensing ion channels to abolish pain.. Diochot S., et al. (2012) Black mamba venom ... Acid-sensing ion channels (ASICs) are generally considered principal players in the pain pathway, including in humans. A snake ...

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Influence of acid-sensing ion channel blocker on behavioral responses in a zebrafish model of acute visceral pain. ... Acid-sensing ion channels (ASICs) play significant roles in numerous neurological and pathological conditions, including pain. ... Channelopathies are a large group of systemic disorders whose pathogenesis is associated with dysfunctional ion channels. ... acetic acid 5% (AA), morphine 2.5 mg/kg (MOR) or acetic acid 5% plus morphine 2.5 mg/kg (AA + MOR) in one subject from a four- ...

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... and addressed their possible interaction with acid-sensing ion channels (ASICs) and P2X receptors at the ischaemic site. ... an ASICs blocker)- and TNP-ATP (a P2X antagonist)-induced analgesic effects in TIIP rats. In na{i}ve rats, i.pl. injection of ... and addressed their possible interaction with acid-sensing ion channels (ASICs) and P2X receptors at the ischaemic site. ... and addressed their possible interaction with acid-sensing ion channels (ASICs) and P2X receptors at the ischaemic site. ...

https://experts.umn.edu/en/publications/role-of-peripheral-sigma-1-receptors-in-ischaemic-pain-potential-

There are two general classes: Voltage-gated ion channels for na+, cl-, ca2+, and al2+, are referred to hospital immediately. ... Calcium channel blockers, antidysrhythmics, cyclic antidepressants, quinidine and other pyridoxine -containing enzyme systems. ... Lipid fatty acid mediators may have tests such as metabolism, uid balance, and movement. 173, antidotes in brief: Sodium ... Meets the clients sense of control, and provides a baseline record of your symptoms do not start putting on weight normally ( ...

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A Highly Potent ASIC1a Blocker and ASIC1b Activator ... Acid-Sensing Ion Channels (ASIC) › Blockers ... Acid-sensing ion channels (ASICs) are voltage-independent proton-gated amiloride sensitive sodium channels, belonging to the ... Activity Hm3a Toxin acts as a potent ASIC1a channel blocker with an IC50 value of 1-2 nM and ASIC1b channel activator with an ... and acts as a potent ASIC1a channel blocker with an IC50 value of 1-2 nM and ASIC1b channel activator with an EC50 value of ...

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France Acid-sensing ion channels (ASICs) are voltage-independent cationic channels activated by extracellular protons expressed ... due to ion flux through the voltage-sensing domains at rest. We find that the binding of outer pore blockers such as ... gating behavior of ion channels. Our work has focused on cyclic nucleotide-regulated channels, channels that are gated by the ... The components of these libraries are being tested for the modulation of different ion channels and other ion channel-related ...

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Lighting up the senses: FM1-43 loading of sensory cells through nonselective ion channels. J. Neurosci. 23, 4054-4065 (2003). ... FM1-43 dye behaves as a permeant blocker of the hair-cell mechanotransducer channel. J. Neurosci. 21, 7013-7025 (2001). ... and polysialic acid neural cell adhesion molecule in rat cochlea during development: implications for the nature of Kollikers ... Cell volumes defined in the MYO7A channel (dashed lines) were used to assess fluorescence intensity in the FM1-43 channel as ...

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... calcium ion antagonist or slow-channel blocker) that inhibits the transmembrane influx of calcium ions into vascular smooth ... Special Senses: abnormal vision, conjunctivitis, diplopia, eye pain, tinnitus. Urinary System: micturition frequency, ... uric acid, blood urea nitrogen, or creatinine. ... Amlodipine besylate tablets is a calcium channel blocker and ... Amlodipine besylate is a type of medicine known as a calcium channel blocker (CCB). It is used to treat high blood pressure ( ...

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PGI2 and epoxides of arachidonic acid contributing to control of overlying vascular smooth muscle contractile activity. ... Thus, endothelial cell ion channels importantly participate in several forms of cell-cell communication in the microcirculation ... Endothelial cells are tightly electrically coupled to their neighboring endothelial cells by gap junctions allowing ion channel ... Endothelial cells are tightly electrically coupled to their neighboring endothelial cells by gap junctions allowing ion channel ...

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Although not as sensitive to risky anesthetics as cys-loop ligand-gated ion channels, Na+ channels are inhibited in vitro in a ... blockers or calcium channel blockers). Describes the hemodynamic response to small (5-�g) boluses of epinephrine, including an ... Hypoxia is sensed by glomus type I cells of the carotid bodies by lowered opening of K+ channels, although the particular kind ... Multiple useful results of eicosapentanoic acid and docosa hexaenoic acid in the important care setting. Other significant ...

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N-type Ca2+ channel blocker ω-conotoxin GVIA (0.1 μm) and P/Q-type Ca2+ channel blocker ω-agatoxin IVA (0.2 μm) significantly ... 1982) Simultaneous determination of serotonin, 5-hydroxindoleacetic acid, 3,4-dihydroxyphenylacetic acid and homovanillic acid ... the actin cytoskeleton also modulates ion channel function. For example, voltage-dependent Ca2+ and NMDA channel activities ... The ability of NPCs to intrinsically sense excitatory activity and thereby implement coupling between network activity and ...

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Calcium channel blocker (CCB) toxicity is one of the most lethal prescription drug overdoses; therefore, understanding the ... partially blocking these voltage-gated ion channels, which are responsible for rapid membrane depolarization. There is a ... Perfusion salad: making sense of verapamil overdose. Acad Emerg Med. 1996 Feb. 3(2):99-100. [QxMD MEDLINE Link]. ... Correction of acid-base disturbances and electrolyte abnormalities is also important, to optimize cardiac function. ...

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Calcium Channel Blockers, Others), Angiotensin Converting Enzyme Inhibitors and Angiotensin Blockers, Electrolytes (Potassium, ... Ion Channels and Currents. *Ventricular Function: Frank-Starling Law, Preload and Afterload, Intracardiac Pressure, Force, ... Temperature Regulation: Temperature Sensing (Central, Peripheral), Regulating Centers (Set Point), Heat Production and ... Pharmacology: Diuretics (Mechanism of Action, Comparison of Drugs, Effect on Electrolytes and Acid-Base Balance, Adverse ...

https://anconsultants.com/course/organ-systems/

Sodium channel blockers amplify existing INa+ and possibly other ion channel defects, with a potency inversely proportional to ... The human cardiac Na+ channel α-subunit is a heavily glycosylated protein of ≈260 kDa consisting of 2016 amino acid residues. ... A calcium sensor Calmodulin (CaM), a ubiquitous Ca2+ sensing protein, binds to the carboxy-terminal IQ domain of the human ... ions. The Na+ channel does not normally conduct divalent cations. A powerful blocker of Na+ entry into the channel is TTX ( ...

http://pepsic.bvsalud.org/scielo.php?script=sci_arttext&pid=S0104-12822016000300002

... capsaicin activates ion channels (TRPV1) that are expressed predominantly by nociceptors.19,20,25,26These TRPV1 ion channels ... 77In addition to blocking voltage-gated sodium channels, QX-314 can inhibit potassium channels activated by γ-aminobutyric acid ... Binshtok AM, Bean BP, Woolf CJ: Inhibition of nociceptors by TRPV1-mediated entry of impermeant sodium channel blockers. Nature ... Meyers JR, MacDonald RB, Duggan A, Lenzi D, Standaert DG, Corwin JT, Corey DP: Lighting up the senses: FM1-43 loading of ...

https://pubs.asahq.org/anesthesiology/article/117/2/365/13220/Differential-Effects-of-Peripheral-versus-Central

This study sped up or slowed down specific neuron types in Drosophilas motion detection circuit by manipulating ion channel ... channel, Water witch (Wtrw). Genetic data implicate Wtrw in sound and humidity sensing, although the signaling pathway, which ... Renal NF-κB activation impairs uric acid homeostasis to promote tumor-associated mortality independent of wasting. Immunity 55( ... Feeding young Pink1B9 flies with fluoxetine, a SERT blocker, prevents the loss of dopaminergic neurons and ameliorates motor ...

https://www.sdbonline.org/sites/fly/aimain/model-organisms-october2022.htm

Anthranilic acids with a phenyl group on the nitrogen. Members modulate ION CHANNELS and are used as ANTI-INFLAMMATORY AGENTS. ... HN - 2008 BX - ATP-Sensitive Potassium Channels FX - Potassium Channel Blockers MH - Retinol-Binding Proteins, Cellular UI - ... These hair cells sense the movement of ENDOLYMPH resulting from angular acceleration of the head, and send signals via the ... HN - 2008(1987) BX - Cyclic-Nucleotide Gated Ion Channels MH - KATP Channels UI - D054086 MN - D12.776.157.530.400.600.450.550 ...

https://decs.bvs.br/I/dcsnew2008.txt

New Ability: Ion Dish = (Rain Dish + Plus). Ability Description: This Pokémons Special Attack is raised by 50% during rain. ... Intended Role: Hazard and status blocker. Role Description: A premier Magic Bounce user with an amazing defensive typing. P.S: ... Haze, Spikes, Toxic Spikes, Recover, Toxic, Yawn, Acid Armor. Intended Role: Special wall, hazard setter. Role Justification: ... Voting is mostly done through our discord channel (Linked in the OP), but you can also DM one of the council members your votes ...

https://www.smogon.com/forums/threads/fusion-evolution-gen-9-slate-5-5-results-not-open-for-submissions.3717085/page-4

Srivastava, S. and Agarwal, A. Effect of anion channel blockers on L-arginine action in spermatozoa from asthenospermic men. ... Early postoperative enteral nutrition with arginine-omega-3 fatty acids and ribonucleic acid-supplemented diet vs placebo in ... Coeffier, M. and Dechelotte, P. Combined infusion of glutamine and arginine: does it make sense? Curr.Opin.Clin.Nutr.Metab Care ... potassium ion and 1450 ppm fluoride, and to a control toothpaste with 1450 ppm fluoride: a three-day clinical study in New ...

https://medlineplus.gov/spanish/druginfo/natural/875.html

SARS-CoV- 2s viroporins, such as its Envelope protein, act as calcium ion channels, introducing calcium into infected cells. ... and myeloperoxidase takes hydrogen peroxide and chlorine ions and makes hypochlorous acid, which is many, many times more ... Ranitidine is not only an H2 blocker used as antacid, but also has a powerful antioxidant effect, scavenging hydroxyl radicals ... Society is losing common sense more and more every day.. https://docs.google.com/…/1lNB5VzZaYs2y3n7iEhx0KP91SE…/edit… ...

https://www.auricmedia.net/tag/vaccine-hazards/

Acid sensing ion channel 3 *Actin *Activator Protein-1 *Activin Receptor-like Kinase ... may M2 ion channel blocker play a significant function in shaping the structure from the microbiota as M2 ion channel blocker ... M2 ion channel blocker, monocytes and granulocytes, Mouse monoclonal to CD53.COC53 monoclonal reacts CD53, NK cells, platelets ... of the data is certainly that AMPs suppress but usually do not get rid of the populations of symbiotic M2 ion channel blocker ...

http://researchensemble.com/tag/b-cells/

Then, 39.0 mL of hydrochloric acid (1 M) was added to the solution. Next, 0.278 g of CaCl2, 0.071 g of Na2SO4, and 6.057 g of ... Calcium sensing rceptor function supports osteoblast survival and acts as a co-factor in PTH anabolic actions in bone. J Cell ... This could suggest that the 100CaP obtained by the wet precipitation method did not react with ions from the SBF, what was ... They have used the CaP coating as pore blocker of drug-loaded MSi nanoparticles. Such coating may be dissolved in acidic ...

https://link.springer.com/article/10.1007/s13346-019-00686-3

Acid sensing ion channel 3 *Actin *Activator Protein-1 *Activin Receptor-like Kinase ... β-adrenergic receptor blockers (β-blockers) are the standard of care for myocardial infarction (MI) and ischemic heart disease ... to treatment with β-blockers (atenolol metoprolol carvedilol nebivolol 3 each) Elesclomol AT1R blocker losartan (1μM) and AT2R ... Anti-hypertensive medicines such as β-adrenergic receptor blockers (β-blockers) and inhibitors of angiotensin II type 1 ...

http://www.mdm2-inhibitors.com/2016/08/to-be-able-to-determine-differences-in-cardiovascular-cell-response-during/

A subclass of sodium channel blockers that are specific for ACID-SENSING SODIUM CHANNELS. (nih.gov)
AN - coordinate with SKIN TRANSPLANTATION if appropriate HN - 2013 MH - Acid Sensing Ion Channel Blockers UI - D062646 MN - D27.505.519.562.750.100 MS - A subclass of sodium channel blockers that are specific for ACID-SENSING SODIUM CHANNELS. (nih.gov)
HN - 2013 BX - Proton-Gated Sodium Channel Blockers MH - Acid Sensing Ion Channels UI - D062565 MN - D12.776.157.530.400.875.50 MN - D12.776.543.550.425.875.50 MN - D12.776.543.585.400.875.50 MN - D12.776.641.24 MS - A family of proton-gated sodium channels that are primarily expressed in neuronal tissue. (nih.gov)
HN - 2013 BX - Proton-Gated Sodium Channels MH - Adenomyosis UI - D062788 MN - C13.351.500.852.113 MS - The extension of endometrial tissue (ENDOMETRIUM) into the MYOMETRIUM. (nih.gov)
In vitro studies demonstrated propoxyphene and the metabolite norpropoxyphene inhibit sodium channels (local anesthetic effect) with norpropoxyphene being approximately 2 fold more potent than propoxyphene and propoxyphene approximately 10 fold more potent than lidocaine. (nih.gov)
Recently a technique was developed to selectively inhibit nociceptive inputs by simultaneously applying two drugs: capsaicin, a transient receptor potential vanilloid receptor-1 channel activator, and QX-314, a lidocaine derivative that intracellularly blocks sodium channels. (asahq.org)

HN - 2013 MH - Aminobenzoates UI - D062365 MN - D2.241.223.100.50 MN - D2.455.426.559.389.127.20 MS - Derivatives of BENZOIC ACID that contain one or more amino groups attached to the benzene ring structure. (nih.gov)

7. Enhancement of acid-sensing ion channel activity by metabotropic P2Y UTP receptors in primary sensory neurons. (nih.gov)
8. Potentiation of acid-sensing ion channel activity by the activation of 5-HT₂ receptors in rat dorsal root ganglion neurons. (nih.gov)
As epilepsy is a disorder highlighted by synchronous activation of neurons, it comes as no surprise that most therapeutic approaches to date have focused on neuronal activity (e.g., sodium channel blockers, enhanced inhibition through GABA A receptors, etc. (nih.gov)
Since there is mounting evidence that Sig-1Rs modulate ischaemia-induced pathological conditions, we investigated the role of Sig-1Rs in ischaemia-induced mechanical allodynia (MA) and addressed their possible interaction with acid-sensing ion channels (ASICs) and P2X receptors at the ischaemic site. (umn.edu)
This is a huge collection of various receptors that are either G [guanine nucleotide-binding] protein coupled or ion channels. (nih.gov)
During inflammation, joint nerves become sensitized to mechanical stimuli through the actions of neuropeptides, eicosanoids, proteinase-activated receptors and ion channel ligands. (biomedcentral.com)
Moreover, we are now in a position to expand our protein target list to other classes of channels and receptors, but also to enzymes. (nih.gov)
Arteriolar endothelial cells express inositol 1,4,5 trisphosphate receptors (IP 3 Rs) and transient receptor vanilloid family member 4 (TRPV4) channels that contribute to agonist-induced endothelial Ca 2+ signals. (frontiersin.org)

Mambalgin-1 rapidly and reversibly inhibits recombinant homomeric ASIC1a (IC 50 =55 nM) and heteromeric ASIC1a+ASIC2a (IC 50 =246 nM) or ASIC1a+ASIC2b channels (IC 50 =61 nM) but also human channels hASIC1b (IC 50 =192 nM) and hASIC1a+hASIC1b (IC 50 =72nM). (smartox-biotech.com)
Pharmacological inhibition by mambalgins combined with the use of knockdown and knockout animals indicates that blockade of heteromeric channels made of ASIC1a and ASIC2a subunits in central neurons and of ASIC1b-containing channels in nociceptors is involved in the analgesic effect of mambalgins. (smartox-biotech.com)
Recent studies have revealed that the Acid Sensing Ion Channel 1a (ASIC1a) likely plays a key role in seizure termination. (nih.gov)
Activity Hm3a Toxin acts as a potent ASIC1a channel blocker with an IC 50 value of 1-2 nM and ASIC1b channel activator with an EC 50 value of 46.5 nM 1 . (alomone.com)
Alomone Labs Hm3a Toxin inhibits ASIC1a channels expressed in Xenopus oocytes. (alomone.com)
Hm3a is a 37-amino acid peptide toxin originally isolated from the venom of Togo starburst tarantula ( Heteroscodra maculata ) and acts as a potent ASIC1a channel blocker with an IC 50 value of 1-2 nM and ASIC1b channel activator with an EC 50 value of 46.5 nM 1 . (alomone.com)

1. Inhibition of acid-sensing ion channels by levo-tetrahydropalmatine in rat dorsal root ganglion neurons. (nih.gov)
3. Inhibition of acid-sensing ion channels by chlorogenic acid in rat dorsal root ganglion neurons. (nih.gov)
5. Inhibition of acid-sensing ion channel currents by propofol in rat dorsal root ganglion neurons. (nih.gov)

Carbon is central to the chemistry of life, and in addition to its fundamental roles as a static component of all major biomolecules spanning proteins, nucleic acids, sugars, and lipids, emerging evidence shows that small and transient carbon-based metabolites, termed reactive carbon species (RCS), are dynamic signaling/stress agents that can influence a variety of biological pathways. (nih.gov)

2014) Binding site and inhibitory mechanism of the mambalgin-2 pain-relieving peptide on acid-sensing ion channel 1a. (smartox-biotech.com)

and (c) the balance of Zn 2+ , an ion with a crucial impact on the cardiovascular system. (hindawi.com)

Acid-sensing ion channels (ASICs) are generally considered principal players in the pain pathway, including in humans. (smartox-biotech.com)
Acid-sensing ion channels (ASICs) are neuronal proton-gated cation channels associated with nociception, fear, depression, seizure, and neuronal degeneration, suggesting roles in pain and neurological and psychiatric disorders. (smartox-biotech.com)
BD-1047 synergistically increased amiloride (an ASICs blocker)- and TNP-ATP (a P2X antagonist)-induced analgesic effects in TIIP rats. (umn.edu)

Several other families of ion channels also have this architecture, including calcium-activated potassium (K Ca ) channels, cyclic nucleotide-gated (CNG) and hyperpolarization-activated cyclic nucleotide-modulated (HCN) channels, and transient receptor potential (TRP) channels ( Fig. 1 and see below). (aspetjournals.org)

Glucose and its metabolites are transported from blood vessels to distant neurons through networks of glial cells coupled to each other by gap junctions, which are protein channels that allow small molecules to pass between cells. (nih.gov)
All of these physiological processes are mediated in part by members of the voltage-gated ion channel protein superfamily ( Fig. 1 ) ( Yu and Catterall, 2004 ). (aspetjournals.org)
The inwardly rectifying potassium channels comprise the simplest structural motif in the ion channel protein superfamily. (aspetjournals.org)

The functional elements of the ion channel superfamily of proteins can be divided into three complementary aspects: ion conductance, pore gating, and regulation. (aspetjournals.org)
Influenza A viruses belong to the family Orthomyxoviridae and possess 8 negative-sense RNA segments encoding 11 known proteins. (cdc.gov)

Mambalgin-1 is a potent and selective blocker of acid-sensing ion channels (ASIC). (smartox-biotech.com)
This Account summarizes work from our laboratory on the development of new chemical tools to monitor two important one-carbon RCS, CO and FA, through activity-based sensing (ABS), where we leverage the unique chemical reactivities of these small and transient analytes, rather than lock-and-key binding considerations, for selective detection. (nih.gov)
Capsaicin, by opening channels in pain-related peripheral nerves, allows permanently charged local anesthetics, like the compound QX-314, to enter nerves and produce selective blockade of just those expressing this pain-related channel. (asahq.org)

2. Morphine inhibits acid-sensing ion channel currents in rat dorsal root ganglion neurons. (nih.gov)
4. Gastrodin inhibits the activity of acid-sensing ion channels in rat primary sensory neurons. (nih.gov)
6. Oxytocin inhibits the activity of acid-sensing ion channels through the vasopressin, V1A receptor in primary sensory neurons. (nih.gov)
15. Resveratrol inhibits the activity of acid-sensing ion channels in male rat dorsal root ganglion neurons. (nih.gov)

10. Potentiation of acid-sensing ion channel activity by peripheral group I metabotropic glutamate receptor signaling. (nih.gov)

A site of exclusively notified, secreted ventricular Signs are caused that an Thryoid respiratory Summary( blocker) can lower accurate congestive heart in a alone left function of number effects. (xtenddigital.com)

Black mamba venom peptides target acid-sensing ion channels to abolish pain. (smartox-biotech.com)
We have recently discovered black mamba venom peptides called mambalgin-1 and mambalgin-2, which are new three-finger toxins that specifically inhibit with the same pharmacological profile ASIC channels to exert strong analgesic effects in vivo. (smartox-biotech.com)

Endothelial cells are tightly electrically coupled to their neighboring endothelial cells by gap junctions allowing ion channel-induced changes in membrane potential to be conducted for considerable distances along the endothelial cell tube that lines arterioles and forms capillaries. (frontiersin.org)

The two variant PTL schemes that have already been demonstrated are a blocker of an inhibitory K+ channel pore and an agonist (activator) of an excitatory neurotransmitter receptor. (nih.gov)

18. Electrophysiological and in vivo characterization of A-317567, a novel blocker of acid sensing ion channels. (nih.gov)

The architectures of the ion channel families consist of four variations built upon a common pore-forming structural theme. (aspetjournals.org)

The two main types are respiratory acidosis and metabolic acidosis, due to metabolic acid build up. (lecturio.com)

Recent examples include the identification of carbon monoxide (CO) as an ion channel blocker and endogenous formaldehyde (FA) as a one-carbon metabolic unit formed from the spontaneous degradation of dietary folate metabolites. (nih.gov)

The contraction process is triggered by an initial calcium ion (Ca 2+ ) influx due to the opening of calcium channels located on the plasmatic membrane and activated by the electric signals. (hindawi.com)

In cardiomyocytes, the functional activity is characterized by a rhythmic contraction ensured by an interplay among myofilaments, intracellular Ca 2+ variations (modulated by channels and pumps), and mitochondrial activity. (hindawi.com)

13. Enhancement of acid-sensing ion channel activity by prostaglandin E2 in rat dorsal root ganglion neurons. (nih.gov)
14. Prolactin potentiates the activity of acid-sensing ion channels in female rat primary sensory neurons. (nih.gov)
Activity-Based Sensing Methods for Monitoring the Reactive Carbon Species Carbon Monoxide and Formaldehyde in Living Systems. (nih.gov)
In addition, endothelial cells may be electrically coupled to overlying smooth muscle cells in arterioles and to pericytes in capillaries via heterocellular gap junctions allowing electrical signals generated by endothelial cell ion channels to be transmitted to overlying mural cells to affect smooth muscle or pericyte contractile activity. (frontiersin.org)
This hyperpolarization can be conducted along the endothelium via homocellular gap junctions and transmitted to overlying smooth muscle cells through heterocellular gap junctions to control the activity of voltage-gated Ca 2+ channels and smooth muscle or pericyte contraction. (frontiersin.org)
Endothelial cell IP 3 R- and TRPV4-mediated Ca 2+ signals also control the production of endothelial cell vasodilator autacoids, such as NO, PGI 2 , and epoxides of arachidonic acid contributing to control of overlying vascular smooth muscle contractile activity. (frontiersin.org)
The ability of NPCs to intrinsically sense excitatory activity and thereby implement coupling between network activity and neurogenesis has recently been established. (jneurosci.org)

Mambalgin-1 differs from mambalgin-2 by one amino acid. (smartox-biotech.com)
The synthesis of fluorescent unnatural amino-acid Anap was optimized and the Anap was incorporated into four sites in an acid-pocket or a transmembrane region of human acid-sensing ion channel-1a (hASIC1a). (smartox-biotech.com)

Propoxyphene and norpropoxyphene inhibit the voltage-gated potassium current carried by cardiac rapidly activating delayed rectifier (hERG) channels with approximately equal potency. (nih.gov)

Diovan HCT (valsartan and hydrochlorothiazide, USP) is a combination of valsartan, an orally active, specific angiotensin II receptor blocker (ARB) acting on the AT 1 receptor subtype, and hydrochlorothiazide, a diuretic. (nih.gov)
We have successfully expressed light-gated channels selectively in a subset of ON RGCs using viral delivery and cell-specific promoters. (nih.gov)

For example, to distinguish CO from other biological diatomics of similar shape and size (e.g., nitric oxide and oxygen), we exploit palladium-mediated carbonylation as a synthetic method for CO sensing. (nih.gov)

Polypeptide toxins have played a central part in understanding physiological and physiopathological functions of ion channels. (smartox-biotech.com)

11. TNF-α acutely enhances acid-sensing ion channel currents in rat dorsal root ganglion neurons via a p38 MAPK pathway. (nih.gov)
19. Endothelin-1 enhances acid-sensing ion channel currents in rat primary sensory neurons. (nih.gov)

intracellular portion of the mediator isoenzyme to the diverse acid may investigate in blood of current polypeptide( inducible cell). (siriuspixels.com)

Here we review the molecular and evolutionary relationships among the families within the voltage-gated-like (VGL 1 ) ion channel superfamily. (aspetjournals.org)

The recent identification of mechanogated ion channels on type III and type IV knee joint afferents by electrophysiological means provided the first insight into the physiological mechanisms responsible for mechanotransduction in joints [ 15 ]. (biomedcentral.com)

Voltage-gated potassium (K V ) channels, first identified as the gene encoding the Shaker mutation in the fruit fly Drosophila , exemplify the second structural architecture in the ion channel superfamily. (aspetjournals.org)

And assists the client and family in planning enhances growth and development and maintenance of intravenous hypertonic sodium bicarbonate in situations and feelings about the attack, 278 a d u lt s : M e n 214 painful intercourse in the home health see mental health actions/interventions spend [number] minutes [number] times per day (but as little as 1 g/kg/min in patients with a sense of aloneness. (revivemedicalny.com)

It is unclear if the effects on ion channels occur within therapeutic dose range. (nih.gov)

Human response patterns patterns of daily living adjustment to the number of etiologies have been proposed but never on an abdominal ultrasound scanning (p. 21 positive spiritual connections by: Meets the clients sense of control, and provides a baseline record of your symptoms do not start putting on weight normally (see growth charts, and hemoglobin and increase your calorie intake. (revivemedicalny.com)
This perspective will focus on the function of resistance artery, arteriolar, and capillary endothelial cell ion channels and how they contribute to cell-cell communication involved in control of blood flow in the microcirculation. (frontiersin.org)

Large diameter myelinated nerve fibres encode and transmit proprioceptive signals, which can be interpreted as being either dynamic (movement sensations) or static (position sense). (biomedcentral.com)

Lipid fatty acid mediators may have tests such as metabolism, uid balance, and movement. (revivemedicalny.com)

Endothelial cells in resistance arteries, arterioles, and capillaries express a diverse array of ion channels that contribute to Cell-Cell communication in the microcirculation. (frontiersin.org)

Our approach is to endow the surviving cells with an ability to sense light, using our engineered light-gated ion channels. (nih.gov)
patients can result caudal to user dynamics and may respond compliance with ventricular oxygen cytoplasm and Immunophilin, methylation inducer, tumor of organizations, supply ability hemodialysis, therapist organelles, and acid-base variability. (siriuspixels.com)

There are two general classes: Voltage-gated ion channels for na+, cl-, ca2+, and al2+, are referred to hospital immediately. (revivemedicalny.com)

These Ca 2+ signals then activate intermediate and small conductance Ca 2+ -activated K + (IK Ca and SK Ca ) channels causing vasodilator-induced endothelial hyperpolarization. (frontiersin.org)

Anatomy11

Organisms8

Chemicals and Drugs122

Analytical, Diagnostic and Therapeutic Techniques and Equipment6

Phenomena and Processes23

Disciplines and Occupations2

Technology, Industry, Agriculture1

Information Science2

Synthesis, structure-activity relationship, and pharmacological profile of analogs of the ASIC-3 inhibitor A-317567. (1/10)

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

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

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

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

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

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

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

Acid Sensing Ion Channel Blockers

Ethosuximide

Ion Channels

Calcium Channel Blockers

Ion Channel Gating

Potassium Channel Blockers

Calcium Channels

Acid Sensing Ion Channels

Sodium Channel Blockers

Chloride Channels

Potassium Channels, Inwardly Rectifying

Potassium Channels, Voltage-Gated

Calcium Channels, L-Type

Membrane Potentials

Electrophysiology

Potassium Channels, Calcium-Activated

Patch-Clamp Techniques

KATP Channels

Ligand-Gated Ion Channels

Calcium

Nifedipine

Electric Conductivity

Potassium

Calcium Channels, T-Type

Shaker Superfamily of Potassium Channels

Cyclic Nucleotide-Gated Cation Channels

Dihydropyridines

Calcium Channels, N-Type

Potassium Channels

Ion Transport

Large-Conductance Calcium-Activated Potassium Channels

TRPC Cation Channels

Diltiazem

Verapamil

Xenopus laevis

Oocytes

TRPM Cation Channels

Kv1.3 Potassium Channel

Tetraethylammonium

TRPV Cation Channels

Sodium Channels

Ether-A-Go-Go Potassium Channels

Kv1.2 Potassium Channel

Calcium Channel Agonists

Dose-Response Relationship, Drug

Action Potentials

Glyburide

Epithelial Sodium Channels

4-Aminopyridine

Nitrobenzoates

Transient Receptor Potential Channels

Rats, Sprague-Dawley

Kinetics

Neurons

Molecular Sequence Data

KCNQ Potassium Channels

Amino Acid Sequence

Kv1.1 Potassium Channel

Cells, Cultured

Kv1.5 Potassium Channel

Small-Conductance Calcium-Activated Potassium Channels

Sodium

Chlorides

Xenopus

Mibefradil

Cell Membrane

Charybdotoxin

Barium

Scorpion Venoms

Adenosine Triphosphate

Nicardipine

Shab Potassium Channels

KCNQ1 Potassium Channel

Apamin

Tetrodotoxin

omega-Conotoxin GVIA

Hyperpolarization-Activated Cyclic Nucleotide-Gated Channels

Cell Line

Cations

Amlodipine