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 class of drugs that act by selective inhibition of calcium influx through cellular membranes.
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.
Gated, ion-selective glycoproteins that traverse membranes. The stimulus for ION CHANNEL GATING can be due to a variety of stimuli such as LIGANDS, a TRANSMEMBRANE POTENTIAL DIFFERENCE, mechanical deformation or through INTRACELLULAR SIGNALING PEPTIDES AND PROTEINS.
CALCIUM CHANNELS that are concentrated in neural tissue. Omega toxins inhibit the actions of these channels by altering their voltage dependence.
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.
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.
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 opening and closing of ion channels due to a stimulus. The stimulus can be a change in membrane potential (voltage-gated), drugs or chemical transmitters (ligand-gated), or a mechanical deformation. Gating is thought to involve conformational changes of the ion channel which alters selective permeability.
Potassium channels where the flow of K+ ions into the cell is greater than the outward flow.
CALCIUM CHANNELS located within the PURKINJE CELLS of the cerebellum. They are involved in stimulation-secretion coupling of neurons.
CALCIUM CHANNELS located in the neurons of the brain.
Pyridine moieties which are partially saturated by the addition of two hydrogen atoms in any position.
CALCIUM CHANNELS located in the neurons of the brain. They are inhibited by the marine snail toxin, omega conotoxin MVIIC.
A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure.
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.
Cell membrane glycoproteins that form channels to selectively pass chloride ions. Nonselective blockers include FENAMATES; ETHACRYNIC ACID; and TAMOXIFEN.
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.
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.
Calcium compounds used as food supplements or in food to supply the body with calcium. Dietary calcium is needed during growth for bone development and for maintenance of skeletal integrity later in life to prevent osteoporosis.
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).
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.
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.
A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.
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 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 calcium channel blocker that is a class IV anti-arrhythmia agent.
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.
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.
Potassium channels whose activation is dependent on intracellular calcium concentrations.
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 benzimidazoyl-substituted tetraline that selectively binds and inhibits CALCIUM CHANNELS, T-TYPE.
The ability of a substrate to allow the passage of ELECTRONS.
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.
An element of the alkaline earth group of metals. It has an atomic symbol Ba, atomic number 56, and atomic weight 138. All of its acid-soluble salts are poisonous.
A calcium channel blockader with preferential cerebrovascular activity. It has marked cerebrovascular dilating effects and lowers blood pressure.
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.
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.
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.
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.
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 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.
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.
Carbonic acid calcium salt (CaCO3). An odorless, tasteless powder or crystal that occurs in nature. It is used therapeutically as a phosphate buffer in hemodialysis patients and as a calcium supplement.
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.
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).
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 salt used to replenish calcium levels, as an acid-producing diuretic, and as an antidote for magnesium poisoning.
A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.
A 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.
The relationship between the dose of an administered drug and the response of the organism to the drug.
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.
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.
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 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.
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 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.
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.
Calcium salts of phosphoric acid. These compounds are frequently used as calcium supplements.
Established cell cultures that have the potential to propagate indefinitely.
Sodium channels found on salt-reabsorbing EPITHELIAL CELLS that line the distal NEPHRON; the distal COLON; SALIVARY DUCTS; SWEAT GLANDS; and the LUNG. They are AMILORIDE-sensitive and play a critical role in the control of sodium balance, BLOOD VOLUME, and BLOOD PRESSURE.
A delayed rectifier subtype of shaker potassium channels that is the predominant VOLTAGE-GATED POTASSIUM CHANNEL of T-LYMPHOCYTES.
A family of voltage-gated potassium channels that are characterized by long N-terminal and C-terminal intracellular tails. They are named from the Drosophila protein whose mutation causes abnormal leg shaking under ether anesthesia. Their activation kinetics are dependent on extracellular MAGNESIUM and PROTON concentration.
Stable calcium atoms that have the same atomic number as the element calcium, but differ in atomic weight. Ca-42-44, 46, and 48 are stable calcium isotopes.
A delayed rectifier subtype of shaker potassium channels that is selectively inhibited by a variety of SCORPION VENOMS.
A delayed rectifier subtype of shaker potassium channels that is commonly mutated in human episodic ATAXIA and MYOKYMIA.
Unstable isotopes of calcium that decay or disintegrate emitting radiation. Ca atoms with atomic weights 39, 41, 45, 47, 49, and 50 are radioactive calcium isotopes.
Single chains of amino acids that are the units of multimeric PROTEINS. Multimeric proteins can be composed of identical or non-identical subunits. One or more monomeric subunits may compose a protomer which itself is a subunit structure of a larger assembly.
A long-acting dihydropyridine calcium channel blocker. It is effective in the treatment of ANGINA PECTORIS and HYPERTENSION.
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 class of polyamine and peptide toxins which are isolated from the venom of spiders such as Agelenopsis aperta.
An aquatic genus of the family, Pipidae, occurring in Africa and distinguished by having black horny claws on three inner hind toes.
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 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.
Abrupt changes in the membrane potential that sweep along the CELL MEMBRANE of excitable cells in response to excitation stimuli.
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 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.
Elements of limited time intervals, contributing to particular results or situations.
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.
Venoms from mollusks, including CONUS and OCTOPUS species. The venoms contain proteins, enzymes, choline derivatives, slow-reacting substances, and several characterized polypeptide toxins that affect the nervous system. Mollusk venoms include cephalotoxin, venerupin, maculotoxin, surugatoxin, conotoxins, and murexine.
A 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 family of delayed rectifier voltage-gated potassium channels that share homology with their founding member, KCNQ1 PROTEIN. KCNQ potassium channels have been implicated in a variety of diseases including LONG QT SYNDROME; DEAFNESS; and EPILEPSY.
A 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 strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
A voltage-gated potassium channel that is expressed primarily in the HEART.
A chelating agent relatively more specific for calcium and less toxic than EDETIC ACID.
Use of electric potential or currents to elicit biological responses.
The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.
A shaker subfamily that is prominently expressed in NEURONS and are necessary for high-frequency, repetitive firing of ACTION POTENTIALS.
A fast inactivating subtype of shaker potassium channels that contains two inactivation domains at its N terminus.
An aminoperhydroquinazoline poison found mainly in the liver and ovaries of fishes in the order TETRAODONTIFORMES, which are eaten. The toxin causes paresthesia and paralysis through interference with neuromuscular conduction.
The 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.
The calcium salt of oxalic acid, occurring in the urine as crystals and in certain calculi.
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.
Chemicals that bind to and remove ions from solutions. Many chelating agents function through the formation of COORDINATION COMPLEXES with METALS.
Coronary vasodilator that is an analog of iproveratril (VERAPAMIL) with one more methoxy group on the benzene ring.
A family of inwardly-rectifying potassium channels that are activated by PERTUSSIS TOXIN sensitive G-PROTEIN-COUPLED RECEPTORS. GIRK potassium channels are primarily activated by the complex of GTP-BINDING PROTEIN BETA SUBUNITS and GTP-BINDING PROTEIN GAMMA SUBUNITS.
The calcium salt of gluconic acid. The compound has a variety of uses, including its use as a calcium replenisher in hypocalcemic states.
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.
The distal terminations of axons which are specialized for the release of neurotransmitters. Also included are varicosities along the course of axons which have similar specializations and also release transmitters. Presynaptic terminals in both the central and peripheral nervous systems are included.
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.
A fluorescent calcium chelating agent which is used to study intracellular calcium in tissues.
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 sesquiterpene lactone found in roots of THAPSIA. It inhibits CA(2+)-TRANSPORTING ATPASE mediated uptake of CALCIUM into SARCOPLASMIC RETICULUM.
The hollow, muscular organ that maintains the circulation of the blood.
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 parts of a macromolecule that directly participate in its specific combination with another molecule.
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.
The uptake of naked or purified DNA by CELLS, usually meaning the process as it occurs in eukaryotic cells. It is analogous to bacterial transformation (TRANSFORMATION, BACTERIAL) and both are routinely employed in GENE TRANSFER TECHNIQUES.
A 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.
The nonstriated involuntary muscle tissue of blood vessels.
A potassium-selective ion channel blocker. (From J Gen Phys 1994;104(1):173-90)
A trace element with the atomic symbol Ni, atomic number 28, and atomic weight 58.69. It is a cofactor of the enzyme UREASE.
Substances used for their pharmacological actions on any aspect of neurotransmitter systems. Neurotransmitter agents include agonists, antagonists, degradation inhibitors, uptake inhibitors, depleters, precursors, and modulators of receptor function.
The study of PHYSICAL PHENOMENA and PHYSICAL PROCESSES as applied to living things.
An antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide.
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.
Lanthanum. The prototypical element in the rare earth family of metals. It has the atomic symbol La, atomic number 57, and atomic weight 138.91. Lanthanide ion is used in experimental biology as a calcium antagonist; lanthanum oxide improves the optical properties of glass.
An element with atomic symbol Cd, atomic number 48, and atomic weight 114. It is a metal and ingestion will lead to CADMIUM POISONING.
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.
Contractile tissue that produces movement in animals.
A dihydropyridine calcium channel antagonist that acts as a potent arterial vasodilator and antihypertensive agent. It is also effective in patients with cardiac failure and angina.
A voltage-gated sodium channel subtype that mediates the sodium ion PERMEABILITY of CARDIOMYOCYTES. Defects in the SCN5A gene, which codes for the alpha subunit of this sodium channel, are associated with a variety of CARDIAC DISEASES that result from loss of sodium channel function.
A 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.
Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures.
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.
Proteins which are found in membranes including cellular and intracellular membranes. They consist of two types, peripheral and integral proteins. They include most membrane-associated enzymes, antigenic proteins, transport proteins, and drug, hormone, and lectin receptors.
The communication from a NEURON to a target (neuron, muscle, or secretory cell) across a SYNAPSE. In chemical synaptic transmission, the presynaptic neuron releases a NEUROTRANSMITTER that diffuses across the synaptic cleft and binds to specific synaptic receptors, activating them. The activated receptors modulate specific ion channels and/or second-messenger systems in the postsynaptic cell. In electrical synaptic transmission, electrical signals are communicated as an ionic current flow across ELECTRICAL SYNAPSES.
A very slow opening and closing voltage-gated potassium channel that is expressed in NEURONS and is closely related to KCNQ2 POTASSIUM CHANNEL. It is commonly mutated in BENIGN FAMILIAL NEONATAL CONVULSIONS.
The pore-forming subunits of large-conductance calcium-activated potassium channels. They form tetramers in CELL MEMBRANES.
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.
Sensory ganglia located on the dorsal spinal roots within the vertebral column. The spinal ganglion cells are pseudounipolar. The single primary branch bifurcates sending a peripheral process to carry sensory information from the periphery and a central branch which relays that information to the spinal cord or brain.
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)
Positively charged atoms, radicals or groups of atoms which travel to the cathode or negative pole during electrolysis.
Intracellular receptors that bind to INOSITOL 1,4,5-TRISPHOSPHATE and play an important role in its intracellular signaling. Inositol 1,4,5-trisphosphate receptors are calcium channels that release CALCIUM in response to increased levels of inositol 1,4,5-trisphosphate in the CYTOPLASM.
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 process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.
A methylpyrrole-carboxylate from RYANIA that disrupts the RYANODINE RECEPTOR CALCIUM RELEASE CHANNEL to modify CALCIUM release from SARCOPLASMIC RETICULUM resulting in alteration of MUSCLE CONTRACTION. It was previously used in INSECTICIDES. It is used experimentally in conjunction with THAPSIGARGIN and other inhibitors of CALCIUM ATPASE uptake of calcium into SARCOPLASMIC RETICULUM.
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 heat-stable, low-molecular-weight activator protein found mainly in the brain and heart. The binding of calcium ions to this protein allows this protein to bind to cyclic nucleotide phosphodiesterases and to adenyl cyclase with subsequent activation. Thereby this protein modulates cyclic AMP and cyclic GMP levels.
RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.
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.
Inorganic compounds derived from hydrochloric acid that contain the Cl- ion.
Striated muscle cells found in the heart. They are derived from cardiac myoblasts (MYOBLASTS, CARDIAC).
A quality of cell membranes which permits the passage of solvents and solutes into and out of cells.
A 37-amino acid residue peptide isolated from the scorpion Leiurus quinquestriatus hebraeus. It is a neurotoxin that inhibits calcium activated potassium channels.
Layers of lipid molecules which are two molecules thick. Bilayer systems are frequently studied as models of biological membranes.
The physical characteristics and processes of biological systems.
Proteins prepared by recombinant DNA technology.
The fluid inside CELLS.
Refers to animals in the period of time just after birth.
Intracellular fluid from the cytoplasm after removal of ORGANELLES and other insoluble cytoplasmic components.
An element of the alkaline earth family of metals. It has the atomic symbol Sr, atomic number 38, and atomic weight 87.62.
Flunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity. It is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy.
An ionophorous, polyether antibiotic from Streptomyces chartreusensis. It binds and transports CALCIUM and other divalent cations across membranes and uncouples oxidative phosphorylation while inhibiting ATPase of rat liver mitochondria. The substance is used mostly as a biochemical tool to study the role of divalent cations in various biological systems.
A cell line generated from human embryonic kidney cells that were transformed with human adenovirus type 5.
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
Regulatory proteins that act as molecular switches. They control a wide range of biological processes including: receptor signaling, intracellular signal transduction pathways, and protein synthesis. Their activity is regulated by factors that control their ability to bind to and hydrolyze GTP to GDP. EC 3.6.1.-.
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).
Agents that emit light after excitation by light. The wave length of the emitted light is usually longer than that of the incident light. Fluorochromes are substances that cause fluorescence in other substances, i.e., dyes used to mark or label other compounds with fluorescent tags.
Inorganic compounds that contain calcium as an integral part of the molecule.
Different forms of a protein that may be produced from different GENES, or from the same gene by ALTERNATIVE SPLICING.
A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.
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.
Body organ that filters blood for the secretion of URINE and that regulates ion concentrations.
An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH.
Specialized junctions at which a neuron communicates with a target cell. At classical synapses, a neuron's presynaptic terminal releases a chemical transmitter stored in synaptic vesicles which diffuses across a narrow synaptic cleft and activates receptors on the postsynaptic membrane of the target cell. The target may be a dendrite, cell body, or axon of another neuron, or a specialized region of a muscle or secretory cell. Neurons may also communicate via direct electrical coupling with ELECTRICAL SYNAPSES. Several other non-synaptic chemical or electric signal transmitting processes occur via extracellular mediated interactions.
Positively charged atoms, radicals or groups of atoms with a valence of plus 2, which travel to the cathode or negative pole during electrolysis.
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 serine-threonine protein kinase that requires the presence of physiological concentrations of CALCIUM and membrane PHOSPHOLIPIDS. The additional presence of DIACYLGLYCEROLS markedly increases its sensitivity to both calcium and phospholipids. The sensitivity of the enzyme can also be increased by PHORBOL ESTERS and it is believed that protein kinase C is the receptor protein of tumor-promoting phorbol esters.
The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.
A group of enzymes that are dependent on CYCLIC AMP and catalyze the phosphorylation of SERINE or THREONINE residues on proteins. Included under this category are two cyclic-AMP-dependent protein kinase subtypes, each of which is defined by its subunit composition.
Proteins to which calcium ions are bound. They can act as transport proteins, regulator proteins, or activator proteins. They typically contain EF HAND MOTIFS.
A white crystal or crystalline powder used in BUFFERS; FERTILIZERS; and EXPLOSIVES. It can be used to replenish ELECTROLYTES and restore WATER-ELECTROLYTE BALANCE in treating HYPOKALEMIA.
A methylxanthine naturally occurring in some beverages and also used as a pharmacological agent. Caffeine's most notable pharmacological effect is as a central nervous system stimulant, increasing alertness and producing agitation. It also relaxes SMOOTH MUSCLE, stimulates CARDIAC MUSCLE, stimulates DIURESIS, and appears to be useful in the treatment of some types of headache. Several cellular actions of caffeine have been observed, but it is not entirely clear how each contributes to its pharmacological profile. Among the most important are inhibition of cyclic nucleotide PHOSPHODIESTERASES, antagonism of ADENOSINE RECEPTORS, and modulation of intracellular calcium handling.
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.
The degree of similarity between sequences of amino acids. This information is useful for the analyzing genetic relatedness of proteins and species.
A dihydropyridine calcium antagonist with positive inotropic effects. It lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels.
Genetically engineered MUTAGENESIS at a specific site in the DNA molecule that introduces a base substitution, or an insertion or deletion.
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.
Unstriated and unstriped muscle, one of the muscles of the internal organs, blood vessels, hair follicles, etc. Contractile elements are elongated, usually spindle-shaped cells with centrally located nuclei. Smooth muscle fibers are bound together into sheets or bundles by reticular fibers and frequently elastic nets are also abundant. (From Stedman, 25th ed)
The part of brain that lies behind the BRAIN STEM in the posterior base of skull (CRANIAL FOSSA, POSTERIOR). It is also known as the "little brain" with convolutions similar to those of CEREBRAL CORTEX, inner white matter, and deep cerebellar nuclei. Its function is to coordinate voluntary movements, maintain balance, and learn motor skills.
A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.
The excitable plasma membrane of a muscle cell. (Glick, Glossary of Biochemistry and Molecular Biology, 1990)
The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.
A voltage-gated sodium channel subtype that mediates the sodium ion PERMEABILITY of SKELETAL MYOCYTES. Defects in the SCN4A gene, which codes for the alpha subunit of this sodium channel, are associated with several MYOTONIC DISORDERS.
A family of voltage-gated eukaryotic porins that form aqueous channels. They play an essential role in mitochondrial CELL MEMBRANE PERMEABILITY, are often regulated by BCL-2 PROTO-ONCOGENE PROTEINS, and have been implicated in APOPTOSIS.
The processes whereby the internal environment of an organism tends to remain balanced and stable.
Interstitial space between cells, occupied by INTERSTITIAL FLUID as well as amorphous and fibrous substances. For organisms with a CELL WALL, the extracellular space includes everything outside of the CELL MEMBRANE including the PERIPLASM and the cell wall.
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 proline analog that acts as a stoichiometric replacement of proline. It causes the production of abnormal proteins with impaired biological activity.
Cellular release of material within membrane-limited vesicles by fusion of the vesicles with the CELL MEMBRANE.
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.
The lower right and left chambers of the heart. The right ventricle pumps venous BLOOD into the LUNGS and the left ventricle pumps oxygenated blood into the systemic arterial circulation.

Functional consequences of mutations in the human alpha1A calcium channel subunit linked to familial hemiplegic migraine. (1/8682)

Mutations in alpha1A, the pore-forming subunit of P/Q-type calcium channels, are linked to several human diseases, including familial hemiplegic migraine (FHM). We introduced the four missense mutations linked to FHM into human alpha1A-2 subunits and investigated their functional consequences after expression in human embryonic kidney 293 cells. By combining single-channel and whole-cell patch-clamp recordings, we show that all four mutations affect both the biophysical properties and the density of functional channels. Mutation R192Q in the S4 segment of domain I increased the density of functional P/Q-type channels and their open probability. Mutation T666M in the pore loop of domain II decreased both the density of functional channels and their unitary conductance (from 20 to 11 pS). Mutations V714A and I1815L in the S6 segments of domains II and IV shifted the voltage range of activation toward more negative voltages, increased both the open probability and the rate of recovery from inactivation, and decreased the density of functional channels. Mutation V714A decreased the single-channel conductance to 16 pS. Strikingly, the reduction in single-channel conductance induced by mutations T666M and V714A was not observed in some patches or periods of activity, suggesting that the abnormal channel may switch on and off, perhaps depending on some unknown factor. Our data show that the FHM mutations can lead to both gain- and loss-of-function of human P/Q-type calcium channels.  (+info)

Ionic currents underlying spontaneous action potentials in isolated cerebellar Purkinje neurons. (2/8682)

Acutely dissociated cell bodies of mouse Purkinje neurons spontaneously fired action potentials at approximately 50 Hz (25 degrees C). To directly measure the ionic currents underlying spontaneous activity, we voltage-clamped the cells using prerecorded spontaneous action potentials (spike trains) as voltage commands and used ionic substitution and selective blockers to isolate individual currents. The largest current flowing during the interspike interval was tetrodotoxin-sensitive sodium current (approximately -50 pA between -65 and -60 mV). Although the neurons had large voltage-dependent calcium currents, the net current blocked by cobalt substitution for calcium was outward at all times during spike trains. Thus, the electrical effect of calcium current is apparently dominated by rapidly activated calcium-dependent potassium currents. Under current clamp, all cells continued firing spontaneously (though approximately 30% more slowly) after block of T-type calcium current by mibefradil, and most cells continued to fire after block of all calcium current by cobalt substitution. Although the neurons possessed hyperpolarization-activated cation current (Ih), little current flowed during spike trains, and block by 1 mM cesium had no effect on firing frequency. The outward potassium currents underlying the repolarization of the spikes were completely blocked by 1 mM TEA. These currents deactivated quickly (<1 msec) after each spike. We conclude that the spontaneous firing of Purkinje neuron cell bodies depends mainly on tetrodotoxin-sensitive sodium current flowing between spikes. The high firing rate is promoted by large potassium currents that repolarize the cell rapidly and deactivate quickly, thus preventing strong hyperpolarization and restoring a high input resistance for subsequent depolarization.  (+info)

Somatic recording of GABAergic autoreceptor current in cerebellar stellate and basket cells. (3/8682)

Patch-clamp recordings were performed from stellate and basket cells in rat cerebellar slices. Under somatic voltage clamp, short depolarizing pulses were applied to elicit action potentials in the axon. After the action potential, a bicuculline- and Cd2+-sensitive current transient was observed. A similar response was obtained when eliciting axonal firing by extracellular stimulation. With an isotonic internal Cl- solution, the peak amplitude of this current varied linearly with the holding potential, yielding an extrapolated reversal potential of -20 to 0 mV. Unlike synaptic or autaptic GABAergic currents obtained in the same preparation, the current transient had a slow rise-time and a low variability between trials. This current was blocked when 10 mM BAPTA was included in the recording solution. In some experiments, the current transient elicited axonal action potentials. The current transient was reliably observed in animals aged 12-15 d, with a mean amplitude of 82 pA at -70 mV, but was small and rare in the age group 29-49 d. Numerical simulations could account for all properties of the current transient by assuming that an action potential activates a distributed GABAergic conductance in the axon. The actual conductance is probably restricted to release sites, with an estimated mean presynaptic current response of 10 pA per site (-70 mV, age 12-15 d). We conclude that in developing rats, stellate and basket cell axons have a high density of GABAergic autoreceptors and that a sizable fraction of the corresponding current can be measured from the soma.  (+info)

Activation of human D3 dopamine receptor inhibits P/Q-type calcium channels and secretory activity in AtT-20 cells. (4/8682)

The D3 dopamine receptor is postulated to play an important role in the regulation of neurotransmitter secretion at both pre- and postsynaptic terminals. However, this hypothesis and the underlying mechanisms remain untested because of the lack of D3-selective ligands, paucity of appropriate model secretory systems, and the weak and inconsistent coupling of D3 receptors to classical signal transduction pathways. The absence of ligands that selectively discriminate between D3 and D2 receptors in vivo precludes the study of D3 receptor function in the brain and necessitates the use of heterologous expression systems. In this report we demonstrate that activation of the human D3 dopamine receptor expressed in the AtT-20 neuroendocrine cell line causes robust inhibition of P/Q-type calcium channels via pertussis toxin-sensitive G-proteins. In addition, using the vesicle trafficking dye FM1-43, we show that D3 receptor activation significantly inhibits spontaneous secretory activity in these cells. Our results not only support the hypothesis that the D3 receptor can regulate secretory activity but also provide insight into the underlying signaling mechanisms. We propose a functional model in which the D3 receptor tightly regulates neurotransmitter release at a synapse by only allowing the propagation of spikes above a certain frequency or burst-duration threshold.  (+info)

Voltage and calcium use the same molecular determinants to inactivate calcium channels. (5/8682)

During sustained depolarization, voltage-gated Ca2+ channels progressively undergo a transition to a nonconducting, inactivated state, preventing Ca2+ overload of the cell. This transition can be triggered either by the membrane potential (voltage-dependent inactivation) or by the consecutive entry of Ca2+ (Ca2+-dependent inactivation), depending on the type of Ca2+ channel. These two types of inactivation are suspected to arise from distinct underlying mechanisms, relying on specific molecular sequences of the different pore-forming Ca2+ channel subunits. Here we report that the voltage-dependent inactivation (of the alpha1A Ca2+ channel) and the Ca2+-dependent inactivation (of the alpha1C Ca2+ channel) are similarly influenced by Ca2+ channel beta subunits. The same molecular determinants of the beta subunit, and therefore the same subunit interactions, influence both types of inactivation. These results strongly suggest that the voltage and the Ca2+-dependent transitions leading to channel inactivation use homologous structures of the different alpha1 subunits and occur through the same molecular process. A model of inactivation taking into account these new data is presented.  (+info)

Calmodulin mediates calcium-dependent activation of the intermediate conductance KCa channel, IKCa1. (6/8682)

Small and intermediate conductance Ca2+-activated K+ channels play a crucial role in hyperpolarizing the membrane potential of excitable and nonexcitable cells. These channels are exquisitely sensitive to cytoplasmic Ca2+, yet their protein-coding regions do not contain consensus Ca2+-binding motifs. We investigated the involvement of an accessory protein in the Ca2+-dependent gating of hIKCa1, a human intermediate conductance channel expressed in peripheral tissues. Cal- modulin was found to interact strongly with the cytoplasmic carboxyl (C)-tail of hIKCa1 in a yeast two-hybrid system. Deletion analyses defined a requirement for the first 62 amino acids of the C-tail, and the binding of calmodulin to this region did not require Ca2+. The C-tail of hSKCa3, a human neuronal small conductance channel, also bound calmodulin, whereas that of a voltage-gated K+ channel, mKv1.3, did not. Calmodulin co-precipitated with the channel in cell lines transfected with hIKCa1, but not with mKv1. 3-transfected lines. A mutant calmodulin, defective in Ca2+ sensing but retaining binding to the channel, dramatically reduced current amplitudes when co-expressed with hIKCa1 in mammalian cells. Co-expression with varying amounts of wild-type and mutant calmodulin resulted in a dominant-negative suppression of current, consistent with four calmodulin molecules being associated with the channel. Taken together, our results suggest that Ca2+-calmodulin-induced conformational changes in all four subunits are necessary for the channel to open.  (+info)

Characterization of elementary Ca2+ release signals in NGF-differentiated PC12 cells and hippocampal neurons. (7/8682)

Elementary Ca2+ release signals in nerve growth factor- (NGF-) differentiated PC12 cells and hippocampal neurons, functionally analogous to the "Ca2+ sparks" and "Ca2+ puffs" identified in other cell types, were characterized by confocal microscopy. They either occurred spontaneously or could be activated by caffeine and metabotropic agonists. The release events were dissimilar to the sparks and puffs described so far, as many arose from clusters of both ryanodine receptors (RyRs) and inositol 1,4,5-trisphosphate receptors (InsP3Rs). Increasing either the stimulus strength or loading of the intracellular stores enhanced the frequency of and coupling between elementary release sites and evoked global Ca2+ signals. In the PC12 cells, the elementary Ca2+ release preferentially occurred around the branch points. Spatio-temporal recruitment of such elementary release events may regulate neuronal activities.  (+info)

Control and assessment of the uterus and cervix during pregnancy and labour. (8/8682)

Preterm labour and resultant preterm birth are the most important problems in perinatology. Countless efforts have failed to establish a single effective treatment of preterm labour, partly because the mechanisms regulating the uterus and cervix during pregnancy are not well understood. New knowledge is needed to inhibit early progression of labour (uterine contractility and cervical ripening), and adequate quantitative tools to evaluate the uterus and cervix during pregnancy are lacking. In this review, we outline studies showing that the uterus (myometrium) and cervix pass through a conditioning step in preparation for labour. This step is not easily identifiable with present methods to assess the uterus or cervix. In the uterus, this seemingly irreversible step consists of changes in the electrical properties to make muscle more excitable and responsive to produce forceful contractions. In the cervix, the step consists of softening of the connective tissue components. Progesterone appears to have a dominant role in controlling both the uterus and cervix, as antiprogestins induce early, preterm conditioning leading to preterm labour. Apparently, nitric oxide (NO) also controls conditioning of the uterus and cervix. In the uterus, NO, in concert with progesterone, inhibits uterine contractility. At term, NO production by the uterus and placenta are decreased and allow labour to progress. In contrast, NO in the cervix increases at the end of pregnancy and it may be the final pathway for stimulating cervical ripening by activation of metalloenzymes. The progress of labour can be assessed non-invasively using electromyographic (EMG) signals from the uterus (the driving force for contractility) recorded from the abdominal surface. Uterine EMG bursts detected in this manner characterize uterine contractile events during human and animal pregnancy. A low uterine EMG activity, measured transabdominally throughout most of pregnancy, rises dramatically during labour. EMG activity also increases substantially during preterm labour in humans and rats. This method may be used one day to predict impending preterm labour and identify control steps and treatments. A quantitative method also assesses the cervix, using an optical device which measures collagen fluorescence in the cervix. The collascope estimates cervical collagen content from a fluorescent signal generated when collagen cross-links are illuminated with excitation light of about 340 nm. The system has proved useful in rats and humans at various stages of pregnancy, and indicates that cervical softening occurs progressively in the last one-third of pregnancy. In rats, collascope readings correlate with resistance measurements made in the isolated cervix, which may help to assess cervical function during pregnancy, and indicate control and treatments.  (+info)

Voltage Dependent T Type Calcium Channel Subunit Alpha 1G (Voltage Gated Calcium Channel Subunit Alpha Cav3.1 or CACNA1G) - Drugs in Development, 2021 provides in depth analysis on Voltage Dependent T Type Calcium Channel Subunit Alpha 1G (Voltage Gated Calcium Channel Subunit Alpha Cav3.1 or CACNA1G) targeted pipeline therapeutics. The report provides comprehensive information complete with Analysis by Indications, Stage of Development, Mechanism of Action (MoA), Route of Administration (RoA) and Molecule Type. The report also covers the descriptive pharmacological action of the therapeutics, its complete research and development history and latest news and press releases. Additionally, the report provides an overview of key players involved in Voltage Dependent T Type Calcium Channel Subunit Alpha 1G (Voltage Gated Calcium Channel Subunit Alpha Cav3.1 or CACNA1G) targeted therapeutics development and features dormant and discontinued projects. The report analyses the pipeline products across ...
Live-cell imaging allows for the in-depth study of activities occurring within living cells. The understanding of these complex interactions has wide ranging implications to many biomedical applications [1]. As the techniques used in live-cell imaging have improved, they have become an important component of monitoring the interactions within and among cells throughout their lifecycle [2, 3] . Several probes have been developed in relation to these endeavors, [4-6], and in turn, we have created T-Time, a repository of T cell images using a novel tag developed in [7].. T cells are lymphocytes that play a central role in cell-mediated immunity to foreign pathogens. Dysregulated T cell responses are implicated in numerous chronic conditions ranging from severe combined immunodeficiency (SCID) to autoimmunity and cancer. T cells migrate extensively throughout the body to enable proper immune function. This migration is the focus of extensive research and has motivated the development of ...
In the present study we have investigated the role of inositol 1,4,5-trisphosphate (IP3), functional IP3 receptors (IP3Rs) and the human homologue of the Drosophila transient receptor potential (Trp) channel, human Trp1 (hTrp1), in store-mediated Ca2+ entry (SMCE) in human platelets. Inhibition of IP3 recycling using Li+, or the inhibition of IP3Rs using xestospongin C, both resulted in the inhibition of SMCE activation following Ca2+ store depletion using thapsigargin. Co-immunoprecipitation experiments indicated that endogenously expressed hTrp1 couples with IP3R type II, but not types I or III, in platelets with depleted intracellular Ca2+ stores, but not in control, undepleted cells. These results provide strong evidence for the activation of SMCE by conformational coupling involving de novo association between IP3Rs and a plasma membrane channel in normal human cells.. ...
A calcium channel opener is a type of drug which facilitates ion transmission through calcium channels. An example is Bay K8644, which is an analogue of nifedipine that specifically and directly activates L-type voltage-dependent calcium channels. In contrast to Bay K8644, which is not for clinical use, Ambroxol is a frequently used mucolytic drug that triggers lysosomal secretion by mobilizing calcium from acidic calcium stores. This effect does most likely not occur by a direct interaction between the drug and a lysosomal calcium channel, but indirectly by neutralizing the acidic pH within lysosomes. Calcium permeable ion channels in lysosomal membranes that may be activated by a luminal pH increase include two pore channels (TPCs), mucolipin TRP channels (TRPMLs) and purinergic receptors of the P2X channel type. Calcium channel blocker Schramm M, Thomas G, Towart R, Franckowiak G (1983). Activation of calcium channels by novel 1,4-dihydropyridines. A new mechanism for positive inotropics or ...
Voltage-dependent calcium channels represent a major pathway of calcium entry into neurons, where they participate actively to cell excitability and to the molecular processes of synaptic transmission. For that reason, they have been the direct or indirect pharmacological targets of analgesics and this long before their implication in the physiology of nociception had been demonstrated. These last years, the still more refined molecular characterization of these channels and their associated regulatory subunits and the demonstration of their implication in nociceptive processes indicates that these structures are prime pharmacological targets for the management of pain. Herein, we detail the recent breakthroughs on calcium channel structure, function and pharmacology, review the implication of calcium channels in the transmission of nociception, and evaluate their importance as targets for the treatment of pain perception. The search for specific inhibitors of voltage-dependent calcium channels appears
Calcium release-activated calcium channels (CRAC) control influx of calcium in human T lymphocytes. Hour-long calcium elevations are necessary for efficient gene expression during T cell activation and proliferation. We report here that, the time course for store-operated Ca2+ entry is short-lived (3-4 min) and therefore, cannot account for the prolonged Ca2+ elevations necessary for NFAT translocation into nucleus. Previous findings strongly suggest that T cell activation is accompanied by cytosolic alkalinization. Here, we show that pH changes in Jurkat T cells following activation with mitogenic lectin, phytohemagglutinin (PHA), depends on the length of time of exposure and the concentration (potency) of the mitogen. For full understanding of ion fluxes involved in this process, it is important to distinguish CRAC channel subtype functions in these cells during activation as well as elucidate the pH mediated changes in Ca2+. In some experiments we show low pH with high concentrations of PHA. We also
Shop Muscle calcium channel ELISA Kit, Recombinant Protein and Muscle calcium channel Antibody at MyBioSource. Custom ELISA Kit, Recombinant Protein and Antibody are available.
TY - JOUR. T1 - Molecular pharmacology of store-operated CRAC channels. AU - Jairaman, Amit. AU - Prakriya, Murali. PY - 2013/9/1. Y1 - 2013/9/1. N2 - Calcium influx through store-operated Ca2+ release-activated Ca2+ channels (CRAC channels) is a well-defined mechanism of generating cellular Ca2+ elevations that regulates many functions including gene expression, exocytosis, and cell proliferation. The identifications of the ER Ca2+ sensing proteins, STIM1-2 and the CRAC channel proteins, Orai1-3, have led to improved understanding of the physiological roles and the activation mechanism of CRAC channels. Defects in CRAC channel function are associated with serious human diseases such as immunodeficiency and auto-immunity. In this review, we discuss several pharmacological modulators of CRAC channels, focusing specifically on the molecular mechanism of drug action and their utility in illuminating the mechanism of CRAC channel operation and their physiological roles in different cells.. AB - ...
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Shop Store-operated calcium entry regulator ELISA Kit, Recombinant Protein and Store-operated calcium entry regulator Antibody at MyBioSource. Custom ELISA Kit, Recombinant Protein and Antibody are available.
TY - JOUR. T1 - Restoration of motor defects caused by loss of drosophila TDP-43 by expression of the voltage-gated calcium channel, cacophony, in central neurons. AU - Lembke, Kayly M.. AU - Scudder, Charles. AU - Morton, David. PY - 2017/9/27. Y1 - 2017/9/27. N2 - Defects in the RNA-binding protein, TDP-43, are known to cause a variety of neurodegenerative diseases, including amyotrophic lateral sclerosis and frontotemporal lobar dementia. A variety of experimental systems have shown that neurons are sensitive to TDP-43 expression levels, yet the specific functional defects resulting from TDP-43 dysregulation have not been well described. Using the Drosophila TDP-43 ortholog TBPH, we previously showed that TBPH-null animals display locomotion defects as third instar larvae. Furthermore, loss of TBPH caused a reduction in cacophony, a Type II voltage-gated calcium channel, expression and that genetically restoring cacophony in motor neurons in TBPH mutant animals was sufficient to rescue the ...
Voltage-dependent calcium channel subunit alpha-2/delta-1 (CA2D1) antibody | P54289 | Voltage-dependent calcium channel subunit alpha-2/delta-1, Voltage-gated calcium channel subunit alpha-2/delta-1, CACNL2A, CCHL2A, MHS3
RecName: Full=Voltage-dependent calcium channel subunit alpha-2/delta-4;AltName: Full=Voltage-gated calcium channel subunit alpha-2/delta-4;Contains: RecName: Full=Voltage-dependent calcium channel subunit alpha-2-4;Contains: RecName: Full=Voltage-depen ...
Voltage-gated calcium channels (VGCCs), also known as voltage-dependent calcium channels (VDCCs), are a group of voltage-gated ion channels found in the membrane of excitable cells (e.g., muscle, glial cells, neurons, etc.) with a permeability to the calcium ion Ca2+. These channels are slightly permeable to sodium ions, so they are also called Ca2+-Na+ channels, but their permeability to calcium is about 1000-fold greater than to sodium under normal physiological conditions. At physiologic or resting membrane potential, VGCCs are normally closed. They are activated (i.e., opened) at depolarized membrane potentials and this is the source of the voltage-gated epithet. The concentration of calcium (Ca2+ ions) is normally several thousand times higher outside the cell than inside. Activation of particular VGCCs allows Ca2+ to rush into the cell, which, depending on the cell type, results in activation of calcium-sensitive potassium channels, muscular contraction, excitation of neurons, ...
Voltage-gated calcium channels are multi-subunit membrane proteins which transduce depolarization into cellular functions like excitation-contraction coupling in muscle or neurotransmitter release in neurons. The auxiliary β subunits function in membrane targeting of the channel and modulation of its gating properties. However, whether β subunits can reversibly interact with, and thus differentially modulate channels in the membrane is still unresolved. Here we applied fluorescence recovery after photobleaching (FRAP) of GFP-tagged α1 and β subunits expressed in dysgenic myotubes to study the relative dynamics of these calcium channel subunits for the first time in a native functional signaling complex. Identical fluorescence recovery rates of both subunits indicate stable interactions, distinct rates dynamic interactions. Whereas the skeletal muscle β1a isoform formed stable complexes with CaV1.1 and CaV1.2, the non-skeletal muscle β2a and β4b isoforms dynamically interacted with both ...
Frequency of genetic polymorphism of calcium channels gene CACNA1C in healthy individuals and patients with arterial hypertension
Complementary DNAs were isolated and used to deduce the primary structures of the alpha 1 and alpha 2 subunits of the dihydropyridine-sensitive, voltage-dependent calcium channel from rabbit skeletal muscle. The alpha 1 subunit, which contains putative binding sites for calcium antagonists, is a hydrophobic protein with a sequence that is consistent with multiple transmembrane domains and shows structural and sequence homology with other voltage-dependent ion channels. In contrast, the alpha 2 subunit is a hydrophilic protein without homology to other known protein sequences. Nucleic acid hybridization studies suggest that the alpha 1 and alpha 2 subunit mRNAs are expressed differentially in a tissue-specific manner and that there is a family of genes encoding additional calcium channel subtypes. ...
Definition of calcium channel blocking agent in the Financial Dictionary - by Free online English dictionary and encyclopedia. What is calcium channel blocking agent? Meaning of calcium channel blocking agent as a finance term. What does calcium channel blocking agent mean in finance?
Voltage-dependent N-type calcium channel subunit alpha-1B (Brain calcium channel III) (BIII) (Calcium channel; L type; alpha-1 polypeptide isoform 5) (Voltage-gated calcium channel subunit alpha Cav2.2 ...
N-type calcium channels belong to the family of voltage gated calcium channels , which open in response to membrane depolarisation. These channels are responsible for the calcium influx that triggers neurotransmitter release at presynaptic terminals. N - type channels are particularly important in mediating neurotransmitter release at the presynaptic terminals of peripheral sensory neurons and have been implicated i n neuropathic pain. Understanding the regulation of N - type channels is critical to the development of treatments that target these channels. Until now it has been difficult to directly investigate the regulation of their expression at the cell surface due to the inability to selectively visualise channels at the surface. Although N - type channels are thought to consist of a Ca v 2.2, α 2 δ and β subunits, there is uncertainty over whether the pore forming Ca v 2.2 subunit does indeed interact with α 2 δ at the cell surface. The work in this thesis has yielded two tagged ...
Alternative splicing of a pair of mutually exclusive exons (exon 37a and 37b) of the P/Q-type Ca2+ channels produces two different splice variants in the EF-hand region, namely Cav2.1[EFa] and Cav2.1[EFb] channels. Using isoform-specific antibodies against Cav2.1[EFa] and Cav2.1[EFb] channels, we show that Cav2.1[EFa] and Cav2.1[EFb] channels are differentially localized in subcellular compartments of hippocampal, cerebellar and cortical neurons. Cav2.1[EFb] channels show somatic, proximal and distal dendritic localization while Cav2.1[EFa] channels are expressed in the cell bodies, proximal dendrites as well as presynaptic terminals. The distinct subcellular localization of Cav2.1[EFa] and Cav2.1[EFb] channels suggests compartmentalized roles of voltage-gated Ca2+ channels in neurotransmitter release and generation of synaptic plasticity. In addition, a yeast-two-hybrid screen was performed to find potential interacting proteins with the EF-hand of the Cav2.1[EFa] channel. The screen reveals ...
Foto: MUI/Presseabteilung; Gerald Obermair mit seinem Team PhD - Student Clemens Schöpf und Stefanie Geisler ,, Presseartikel mypoint. The family of α1 subunits consists of 10 genes, seven of which constitute the high-voltage-activated calcium channels of the CaV1 and CaV2 subgroups (α1A to α1F and α1S). With the exception of two specific α1 subunits expressed in skeletal muscle (see research by The Flucher Lab) and in the retina all isoforms are expressed in the nervous system.. Regarding the auxiliary subunits all of the four β subunits and three of the four α2δ subunits are found in the brain. Because all α1, β, and α2δ subunits can form functional channel complexes with each other, this yields the theoretical number of 60 different brain calcium channels (5 α1 X 4 β X 3 α2δ) not considering the existence of multiple splices of each protein! In our research we address the question why nerve cells express so many different calcium channels subunits and whether individual ...
Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1C gives rise to L-type calcium currents. Long-lasting (L-type) calcium channels belong to the high-voltage activated (HVA) group. They are blocked by dihydropyridines (DHP), phenylalkylamines, benzothiazepines, and by omega-agatoxin-IIIA (omega-Aga-IIIA). They are however insensitive to omega-conotoxin-GVIA (omega-CTx-GVIA) and omega-agatoxin-IVA (omega-Aga-IVA). Calcium channels containing the alpha-1C subunit play an important role in excitation-contraction coupling in the heart. The various isoforms display marked differences in the sensitivity to DHP compounds. Binding of calmodulin or CABP1 at the same regulatory sites results in an opposit effects on the channel function ...
Background Antigen stimulation of immune cells triggers Ca2+ entry through Ca2+ release-activated Ca2+(CRAC) channels, promoting an immune response to pathogens. Defects in a CRAC (Orai) channel in...
voltage-gated calcium channel complex, high voltage-gated calcium channel activity, voltage-gated calcium channel activity, calcium ion transmembrane transport, calcium-mediated signaling, chemical synaptic transmission, neuromuscular junction development, neuron remodeling, regulation of voltage-gated calcium channel activity
Mast cell activation involves cross-linking of IgE receptors followed by phosphorylation of the non-receptor tyrosine kinase Syk. This results in activation of the plasma membrane-bound enzyme phospholipase Cgamma1, which hydrolyzes the minor membrane phospholipid phosphatidylinositol 4,5-bisphosphate to generate diacylglycerol and inositol trisphosphate. Inositol trisphosphate raises cytoplasmic Ca2+ concentration by releasing Ca2+ from intracellular stores. This Ca2+ release phase is accompanied by sustained Ca2+ influx through store-operated Ca2+ release-activated Ca2+ (CRAC) channels. Here, we find that engagement of IgE receptors activates Syk, and this leads to Ca2+ release from stores followed by Ca2+ influx. The Ca2+ influx phase then sustains Syk activity. The Ca2+ influx pathway activated by these receptors was identified as the CRAC channel, because pharmacological block of the channels with either a low concentration of Gd3+ or exposure to the novel CRAC channel blocker 3-fluoropyridine-4
TY - JOUR. T1 - Store-independent activation of orai1 by SPCA2 in mammary tumors. AU - Feng, Mingye. AU - Grice, Desma M.. AU - Faddy, Helen M.. AU - Nguyen, Nguyen. AU - Leitch, Sharon. AU - Wang, Yingyu. AU - Muend, Sabina. AU - Kenny, Paraic A.. AU - Sukumar, Saraswati. AU - Roberts-Thomson, Sarah J.. AU - Monteith, Gregory R.. AU - Rao, Rajini. PY - 2010/10/1. Y1 - 2010/10/1. N2 - Ca2+ is an essential and ubiquitous second messenger. Changes in cytosolic Ca2+ trigger events critical for tumorigenesis, such as cellular motility, proliferation, and apoptosis. We show that an isoform of Secretory Pathway Ca2+-ATPase, SPCA2, is upregulated in breast cancer-derived cells and human breast tumors, and suppression of SPCA2 attenuates basal Ca2+ levels and tumorigenicity. Contrary to its conventional role in Golgi Ca2+ sequestration, expression of SPCA2 increased Ca2+ influx by a mechanism dependent on the store-operated Ca2+ channel Orai1. Unexpectedly, SPCA2-Orai1 signaling was independent of ER ...
Elevation in cytosolic calcium, [Ca2+]i, is an essential step in numerous physiological and pathophysiological signal transduction events. Ion channels allowing for the entry of extracellular Ca2+ into the cytosol are the principal source of increased [Ca2+]i. In nonexcitable cells, store-operated calcium (SOC), and to a lesser extent, receptor-operated calcium (ROC), entry channels represent the main source of calcium entry.1,2 Although it is generally recognized that SOC entry occurs through Ca2+-selective and nonselective channels, the molecular makeup, regulation, and downstream targets of specific channels remain to be determined.. In endothelial cells, activation of SOC entry contributes to the formation of intercellular gaps, leading to endothelial barrier disruption,3-5 a common factor in the development and progression of systemic and pulmonary diseases, including hypertension, atherosclerosis, and acute respiratory distress syndrome. It is therefore therapeutically desirable to ...
Synaptic vesicle exocytosis in primary cultures of baroreceptor neurons is reduced during high-frequency stimulation. Calcium influx through voltage-gated calcium channels (VGCC) is a key step in neurotransmitter release. With the help of FM2-10, a marker of synaptic vesicle recycling, the present s …
Reduced pancreatic b-cell function or mass is the critical problem in developing diabetes. Insulin release from b-cells depends on Ca2+ influx through high voltage- gated Ca2+ channels (HVCCs). Ca2+ influx also regulates insulin synthesis and insulin granule priming and contributes to β-cell electrical activity. The HVCCs aremultisubunit protein complexes composed of a pore-forming a1 and auxiliary β and α2δ subunits. α2δ is a key regulator of membrane incorporation and function of HVCCs. Here we show that genetic deletion of α2δ-1, the dominant α 2δ subunit in pancreatic islets, results in glucose intolerance and diabetes without affecting insulin sensitivity. Lack of the α 2δ-1 subunit reduces the Ca2+ currents through all HVCC isoforms expressed in b-cells equally in male and female mice. The reduced Ca2+ influx alters the kinetics and amplitude of the global Ca2+ response to glucose in pancreatic islets and significantly reduces insulin release in both sexes. The progression of ...
Store-operated Ca2+ channels in the plasma membrane (PM) are activated by the depletion of Ca2+ from the endoplasmic reticulum (ER) and constitute a widespread and highly conserved Ca2+ influx pathway. After store emptying, the ER Ca2+ sensor STIM1 forms multimers, which then migrate to ER-PM junctions where they activate the Ca2+ release-activated Ca2+ channel Orai1. Movement of an intracellular protein to such specialized sites where it gates an ion channel is without precedence, but the fundamental question of how STIM1 migrates remains unresolved. Here, we show that trafficking of STIM1 to ER-PM junctions and subsequent Ca2+ release-activated Ca2+ channel activity is impaired following mitochondrial depolarization. We identify the dynamin-related mitochondrial protein mitofusin 2, mutations of which causes the inherited neurodegenerative disease Charcot-Marie-Tooth IIa in humans, as an important component of this mechanism. Our results reveal a molecular mechanism whereby a mitochondrial fusion
Voltage-gated calcium (Cav) channels, which are regulated by membrane potential, cytosolic Ca2+, phosphorylation, and membrane phospholipids, govern Ca2+ entry into excitable cells. Cav channels contain a pore-forming α1 subunit, an auxiliary α2δ subunit, and a regulatory β subunit, each encoded by several genes in mammals. In addition to a domain that interacts with the α1 subunit, β2e and β2a also interact with the cytoplasmic face of the plasma membrane through an electrostatic interaction for β2e and posttranslational acylation for β2a. We found that an increase in cytosolic Ca2+ promoted the release of β2e from the membrane without requiring substantial depletion of the anionic phospholipid phosphatidylinositol 4,5-bisphosphate (PIP2) from the plasma membrane. Experiments with liposomes indicated that Ca2+ disrupted the interaction of the β2e amino-terminal peptide with membranes containing PIP2. Ca2+ binding to calmodulin (CaM) leads to CaM-mediated inactivation of Cav currents. ...
Calcium (Ca2+) is an essential signaling messenger in every eukaryotic cell, regulating diverse and kinetically distinct cellular phenomena in health and disease. Sarco/endoplasmic reticulum (SR/ER) luminal store-dependent Ca2+ influx through plasma membrane (PM) Ca2+ release activated Ca2+ (CRAC) channels is a vital Ca2+ entry pathway mediating sustained cytosolic Ca2+ elevations. The molecular players that mediate this store-operated Ca2+ entry (SOCE) include the stromal interaction molecules (STIM)s which sense changes in SR/ER luminal Ca2+ levels and the Orai proteins which constitute the PM Ca2+ channel pore. Upon luminal Ca2+ store depletion, STIMs oligomerize and translocate to the SR/ER-PM junctions where they recruit and activate the Orai channels, forming a CRAC channel complex. My research applies structural biology (i.e. solution nuclear magnetic resonance spectroscopy and X-ray crystallography), biophysical methodologies (i.e. optical spectroscopies, calorimetry, chromatography, ...
Ca2+ flux into mitochondria is an important regulator of cytoplasmic Ca2+ signals, energy production and cell death pathways. Ca2+ uptake can occur through the recently discovered mitochondrial uniporter channel (MCU) but whether the MCU is involved in shaping Ca2+ signals and downstream responses to physiological levels of receptor stimulation is unknown. Here, we show that modest stimulation of leukotriene receptors with the pro-inflammatory signal LTC4 evokes a series of cytoplasmic Ca2+ oscillations that are rapidly and faithfully propagated into mitochondrial matrix. Knockdown of MCU or mitochondrial depolarisation, to reduce the driving force for Ca2+ entry into the matrix, prevents the mitochondrial Ca2+ rise and accelerates run down of the oscillations. The loss of cytoplasmic Ca2+ oscillations appeared to be a consequence of enhanced Ca2+-dependent inactivation of InsP3 receptors, which arose from the loss of mitochondrial Ca2+ buffering. Ca2+ dependent gene expression in response to
6/28/2020. Colchicine in COVID 19 improved time to clinical deterioration.. 6/24/2020. Tocilizumab improves survival in mechanically ventilated COVID 19 patients with cytokine storm.. 6/20/2020. Covid-19: Low dose steroid dexamethasone cuts death in ventilated patients.. 6/15/2020. Auxora( inhibitor of calcium release-activated calcium (CRAC) channels) and Acalabrutinib(Bruton tyrosine kinase BTK inhibitor) may work against COVID.. 6/9/2020. Rifabutin may be useful against Acinetobacter baumannii.. 6/1/2020. Artificial Intelligence as good as radiologists in detecting Lung Infection in Supine Chest Radiographs of Critically Ill Patients. 5/22/2020. High-Dose Vitamin C Therapy in Adult Patients is not associated with any harm.. 5/18/2020. Operative Surgery Is Rarely Required in the Acute Management of Diverticulitis.. 5/1/2020. Remdesivir accelerates recovery in COVID 19.. 4/11/2020. Cytokine absorbing filter in patients with pneumococcal sepsis undergoing ECMO may reduce mortality. ...
The beta subunit of voltage-dependent calcium channels contributes to the function of the calcium channel by increasing peak calcium current, shifting the voltage dependencies of activation and inactivation, modulating G protein inhibition and controlling the alpha-1 subunit membrane targeting.
Orai1 antibody (ORAI calcium release-activated calcium modulator 1) for ELISA, ICC/IF, IHC-P, WB. Anti-Orai1 pAb (GTX85057) is tested in Human, Mouse samples. 100% Ab-Assurance.
There is a new publication out in the Journal of Neuroscience (cover story) from Moran Eye Center scientists, Store-Operated Calcium Entry In Müller Glia Is Controlled By Synergistic Activation Of TRPC And Orai Channels authored by Tünde Molnár, Oleg Yarishkin, Peter Barabas, Anthony Iuso, Bryan William Jones, Robert Marc, Tam Phuong, and David Krizaj.. Continue reading Store-Operated Calcium Entry In Müller Glia Is Controlled By Synergistic Activation Of TRPC And Orai Channels. ...
Ca(2+)-dependent gene expression is critical for cell growth, proliferation, plasticity, and adaptation [1-3]. Because a common mechanism in vertebrates linking cytoplasmic Ca(2+) signals with activation of protein synthesis involves the nuclear factor of activated T cells (NFAT) family of transcription factors [4, 5], we have quantified protein expression in single cells following physiological Ca(2+) signals by using NFAT-driven expression of a genetically encoded fluorescent protein. We find that gene expression following CRAC channel activation is an all-or-nothing event over a range of stimulus intensities. Increasing agonist concentration recruits more cells but each responding cell does so in an essentially digital manner. Furthermore, Ca(2+)-dependent gene expression shows both short-term memory and strong synergy, where two pulses of agonist, which are ineffectual individually, robustly activate gene expression provided that the time interval between them is short. Such temporal filtering
RGK regulation of voltage-gated calcium channels. . Biblioteca virtual para leer y descargar libros, documentos, trabajos y tesis universitarias en PDF. Material universiario, documentación y tareas realizadas por universitarios en nuestra biblioteca. Para descargar gratis y para leer online.
We hypothesized that the store-operated calcium entry (SOCE) channel, Orai1, participates in the activation of Th17 cells and influences renal injury. In rats, following renal ischemia/reperfusion (I/R), there was a rapid and sustained influx of Orai1+ CD4 T cells and IL-17 expression was restricted to Orai1+ cells. When kidney CD4+ cells of post-acute kidney injury (post-AKI) rats were stimulated with angiotensin II and elevated Na+ (10-7 M/170 mM) in vitro, there was an enhanced response in intracellular Ca2+ and IL-17 expression, which was blocked by SOCE inhibitors 2APB, YM58483/BTP2, or AnCoA4. In vivo, YM58483/BTP2 (1 mg/kg) attenuated IL-17+ cell activation, inflammation, and severity of AKI following either I/R or intramuscular glycerol injection. Rats treated with high-salt diet (5-9 weeks after I/R) manifested progressive disease indicated by enhanced inflammation, fibrosis, and impaired renal function. These responses were significantly attenuated by YM58483/BTP2. In peripheral blood ...
We hypothesized that the store-operated calcium entry (SOCE) channel, Orai1, participates in the activation of Th17 cells and influences renal injury. In rats, following renal ischemia/reperfusion (I/R), there was a rapid and sustained influx of Orai1+ CD4 T cells and IL-17 expression was restricted to Orai1+ cells. When kidney CD4+ cells of post-acute kidney injury (post-AKI) rats were stimulated with angiotensin II and elevated Na+ (10-7 M/170 mM) in vitro, there was an enhanced response in intracellular Ca2+ and IL-17 expression, which was blocked by SOCE inhibitors 2APB, YM58483/BTP2, or AnCoA4. In vivo, YM58483/BTP2 (1 mg/kg) attenuated IL-17+ cell activation, inflammation, and severity of AKI following either I/R or intramuscular glycerol injection. Rats treated with high-salt diet (5-9 weeks after I/R) manifested progressive disease indicated by enhanced inflammation, fibrosis, and impaired renal function. These responses were significantly attenuated by YM58483/BTP2. In peripheral blood ...
We hypothesized that the store-operated calcium entry (SOCE) channel, Orai1, participates in the activation of Th17 cells and influences renal injury. In rats, following renal ischemia/reperfusion (I/R), there was a rapid and sustained influx of Orai1+ CD4 T cells and IL-17 expression was restricted to Orai1+ cells. When kidney CD4+ cells of post-acute kidney injury (post-AKI) rats were stimulated with angiotensin II and elevated Na+ (10-7 M/170 mM) in vitro, there was an enhanced response in intracellular Ca2+ and IL-17 expression, which was blocked by SOCE inhibitors 2APB, YM58483/BTP2, or AnCoA4. In vivo, YM58483/BTP2 (1 mg/kg) attenuated IL-17+ cell activation, inflammation, and severity of AKI following either I/R or intramuscular glycerol injection. Rats treated with high-salt diet (5-9 weeks after I/R) manifested progressive disease indicated by enhanced inflammation, fibrosis, and impaired renal function. These responses were significantly attenuated by YM58483/BTP2. In peripheral blood ...
The IUPHAR/BPS Guide to Pharmacology. Cav1.3 - Voltage-gated calcium channels. Detailed annotation on the structure, function, physiology, pharmacology and clinical relevance of drug targets.
ENCODES a protein that exhibits low voltage-gated calcium channel activity (ortholog); INVOLVED IN neuronal action potential; sleep; calcium ion import (ortholog); PARTICIPATES IN calcium transport pathway; calcium/calcium-mediated signaling pathway; mitogen activated protein kinase signaling pathway; INTERACTS WITH bisphenol A; raloxifene; tetraphene
Our research focuses on how intracellular Ca2+, the ultimate signal of membrane excitability, regulates membrane excitability and the consequent function of excitable cells. We have discovered and described multiple mechanisms that control Ca2+ influx through voltage-gated Ca2+ channels and feedback mechanisms by which internal calcium regulates other channels that influence
Insulin-like growth factor 1 (IGF-1) rapidly potentiates N and L calcium channel currents in cerebellar granule neurons by an unknown mechanism. Here, we show that the L channel alpha1C subunit is tyrosine phosphorylated in response to IGF-1. Moreover, expression of kinase-dead c-Src in neurons or a …
Concentrations of calcium within mitochondria are tightly regulated and modulate physiological mitochondrial functions, including control of metabolism and cell death. Sancak et al. complete the molecular characterization of the mitochondrial calcium uniporter (MCU), the multicomponent channel that allows concentration of calcium within the organelle. They identified a small protein termed essential MCU regulator-or EMRE-which was required for calcium transport activity of the fully assembled uniporter.. Y. Sancak, A. L. Markhard, T. Kitami, E. Kovács-Bogdán, K. J. Kamer, N. D. Udeshi, S. A. Carr, D. Chaudhuri, D. E. Clapham, A. A. Li, S. E. Calvo, O. Goldberger, V. K. Mootha, EMRE is an essential component of the mitochondrial calcium uniporter complex. Science 342, 1379-1382 (2013). [Abstract] [Full Text] ...
Changes in the cytoplasm free Ca2+ concentration [Ca2+]in regulate a large number of relevant physiological processes and have a major impact on cell development and function. The identification of STIM, the endoplasmic reticulum (ER) Ca2+ sensor, and Orai, a key subunit of the Ca2+ release-activated Ca2+ (CRAC) channel pore, have provided the tools to illuminate the mechanisms of CRAC channel regulation, that play an important role in modulation of the free Ca2+ concentration in non-excitable cells. Store-operated Ca2+ entry (SOCE) is a common and ubiquitous mechanism for regulating Ca2+ influx into cells and is widely expressed in most tissues. ...
To unravel the evolutionarily conserved genetic network underlying energy homeostasis, we performed a systematic in vivo gene knockdown screen in D...
This gene encodes an alpha-1 subunit of a voltage-dependent calcium channel. Calcium channels mediate the influx of calcium ... calcium channel activity. • metal ion binding. • voltage-gated ion channel activity. • ion channel activity. • protein binding ... high voltage-gated calcium channel activity. • voltage-gated calcium channel activity involved in AV node cell action potential ... voltage-gated calcium channel activity. • voltage-gated calcium channel activity involved in cardiac muscle cell action ...
ion channel activity. • protein binding. • actin binding. • calcium channel activity. • cation channel activity. • protein ... cation channel complex. Biological process. • regulation of cytosolic calcium ion concentration. • positive regulation of ... store-operated calcium channel activity. • clathrin binding. • inositol 1,4,5 trisphosphate binding. • ... Heiner I, Eisfeld J, Lückhoff A (2004). "Role and regulation of TRP channels in neutrophil granulocytes". Cell Calcium. 33 (5-6 ...
See also: Ryanodine-Inositol 1,4,5-triphosphate receptor calcium channels. inositol 1,4,5-trisphosphate receptor, type 1[1]. ... Inositol trisphosphate receptor (InsP3R) is a membrane glycoprotein complex acting as a Ca2+ channel activated by inositol ...
Cl−: Chloride channel. *Calcium-activated chloride channels *Anoctamin *ANO1. *Bestrophin *1. *2 ... gap junction channel activity. Cellular component. • cytoplasm. • integral component of membrane. • gap junction. • cell ... Connexins are membrane-spanning proteins that assemble to form gap junction channels that facilitate the transfer of ions and ... Typically the GJB1 protein forms channels through the myelin to the internal Schwann cell or oligodendrocyte, allowing ...
Cl−: Chloride channel. *Calcium-activated chloride channels *Anoctamin *ANO1. *Bestrophin *1. *2 ... Channel composition influences the function of gap junction channels. Before innexins and connexins were well characterized, ... When two identical hemichannel proteins come together to form a Gap junction channel, it is called a homotypic GJ channel. When ... 3) and calcium (Ca2+. ),[7] although different hemichannel subunits can impart different selectivity for particular small ...
channel regulator activity. • calcium channel activity. • voltage-gated calcium channel activity. • calcium channel regulator ... Voltage-dependent calcium channel gamma-4 subunit is a protein that in humans is encoded by the CACNG4 gene.[5][6] ... CACNG4, calcium voltage-gated channel auxiliary subunit gamma 4. External IDs. OMIM: 606404 MGI: 1859167 HomoloGene: 8674 ... voltage-gated calcium channel complex. • integral component of membrane. • integral component of plasma membrane. • AMPA ...
ion channel activity. • store-operated calcium channel activity. • protein binding. • calcium channel activity. • clathrin ... regulation of cytosolic calcium ion concentration. • calcium ion transmembrane transport. • calcium ion transport. • nervous ... calcium channel complex. • membrane. • cytoplasm. • growth cone. • neuronal cell body. • dendrite. • membrane raft. • cation ... Beech DJ (2007). "Bipolar phospholipid sensing by TRPC5 calcium channel". Biochem. Soc. Trans. 35 (Pt 1): 101-4. doi:10.1042/ ...
"Functional coupling of intracellular calcium and inactivation of voltage-gated Kv1.1/Kvbeta1.1 A-type K+ channels". Proc. Natl ... channel), voltage gated potassium channel HBK1, voltage gated potassium channel subunit Kv1.1, voltage-gated K+ channel HuKI ... potassium channel activity. • delayed rectifier potassium channel activity. • voltage-gated ion channel activity. • GO:0015388 ... Potassium voltage-gated channel subfamily A member 1 also known as Kv1.1 is a shaker related voltage-gated potassium channel ...
calcium channel activity. • metal ion binding. • voltage-gated ion channel activity. • voltage-gated calcium channel activity. ... a protein in the voltage-dependent calcium channel complex. Calcium channels mediate the influx of calcium ions into the cell ... Voltage-dependent calcium channel subunit alpha2delta-2 is a protein that in humans is encoded by the CACNA2D2 gene.[5] ... CACNA2D2, CACNA2D, calcium voltage-gated channel auxiliary subunit alpha2delta 2. External IDs. OMIM: 607082 MGI: 1929813 ...
... is an antihistamine and calcium channel blocker of the diphenylmethylpiperazine group.[1] It is prescribed for ... Cinnarizine is classified as a selective antagonist of T-type voltage-operated calcium ion channels, because its binding blocks ... due to calcium channel blockade), which happen mostly in brain and the fact that it is also used as a labyrinthine sedative.[14 ... and it has been shown that this drug preferentially binds to its target calcium channels when they are in an open, as opposed ...
Calcium channel. Voltage-gated. *CACNA1A *Familial hemiplegic migraine 1. *Episodic ataxia 2 ...
The main ones are the L-type calcium channel α1-subunit[1] and potassium inward rectifier 2.6;[3] it is therefore classified as ... Genetic mutations in the L-type calcium channel α1-subunit (Cav1.1) have been described in Southern Chinese with TPP. The ... The condition has been linked with genetic mutations in genes that code for certain ion channels that transport electrolytes ( ... Furthermore, mutations have been reported in the genes coding for potassium voltage-gated channel, Shaw-related subfamily, ...
Calcium channel. Voltage-gated. *CACNA1A *Familial hemiplegic migraine 1. *Episodic ataxia 2 ...
CaVβ2B - β-2 subunit of the voltage-gated calcium channel carrying the L-type calcium current ICa(L).[17] ... CaV1.2 - α subunit of voltage-dependent calcium channel carrying the L-type calcium current ICa(L). [17] ... α2δ subunit of the voltage-gated calcium channel carrying the L-type calcium current ICa(L).[6] ... while others form different types of sodium channel (SCN10A). Some genes encode ion channels that carry calcium or potassium ...
The calcium channels are used for cell signaling and triggering apoptosis. The calcium uniporter transports calcium across the ... Hoppe, U. (2010). "Mitochondrial Calcium Channels". FEBS Letters: 1975-1981. OpenStax College (2013). Chapter 12.4 The Action ... Uniporter channels open in response to a stimulus and allow the free flow of specific molecules. There are several ways in ... Voltage-gated potassium channels are also uniporters that can be found in neurons and are essential for action potentials. This ...
... works as a calcium antagonist by blocking voltage-dependent calcium channels. A study using [3H]Nitrendipine showed ... and apoptotic death is reduced through the reduction of calcium-dependent apoptotic agents. While some calcium-channel blockers ... Lomerizine (INN) (also known as KB-2796) is a diphenylpiperazine class L-type and T-type calcium channel blocker. This drug is ... However, its antimigraine effects are believed to be due not to the blocking of calcium channels, but to the antagonizing ...
... , a bis-benzylisoquinoline alkaloid, is a calcium channel blocker. It has anti-inflammatory, immunologic and ... doi:10.1016/S0031-9422(00)91024-0. Tetrandrine(Fanchinine) , CAS 518-34-3 , calcium channel Inhibitor , Fanchinine, Hanfangchin ... "Two-pore channels control Ebola virus host cell entry and are drug targets for disease treatment". Science. 347 (6225): 995-998 ...
"Calcium Channel Blockers". livertox.nih.gov. Retrieved 2015-12-22. "Calcium channel blockers are not recommended for the ... A variety of medications have been developed to relax the blood vessels in the lung, calcium channel blockers are used but only ...
Medications that are probably associated with gynecomastia include calcium channel blockers such as verapamil, amlodipine, and ... calcium channel blockers; antifungal medications such as ketoconazole; antibiotics such as metronidazole; tricyclic ...
Most frequent side effects are nausea, orthostatic hypotension, headaches, and vomiting through stimulation of the brainstem vomiting centre.[9] Vasospasms with serious consequences such as myocardial infarction and stroke that have been reported in connection with the puerperium, appear to be extremely rare events.[10] Peripheral vasospasm (of the fingers or toes) can cause Raynaud's Phenomenon. Bromocriptine use has been anecdotally associated with causing or worsening psychotic symptoms (its mechanism is in opposition of most antipsychotics, whose mechanisms generally block dopamine).[11] Pulmonary fibrosis has been reported when bromocriptine was used in high doses for the treatment of Parkinson's disease.[12] Use to suppress milk production after childbirth was reviewed in 2014 and it was concluded that in this context a causal association with serious cardiovascular, neurological or psychiatric events could not be excluded with an overall incidence rate estimated to range between 0.005% ...
InChI=1S/C25H29N3O2/c1-27-14-18(13-26-25(29)30-16-17-7-4-3-5-8-17)11-21-20-9-6-10-22-24(20)19(12-23(21)27)15-28(22)2/h3-10,15,18,21,23H,11-14,16H2,1-2H3,(H,26,29)/t18-,21+,23+/m0/s1 ...
Calcium channel. 7. Exocytosis of a vesicle. 8. Recaptured neurotransmitter. ... Amino acid neurotransmitter release (exocytosis) is dependent upon calcium Ca2+ and is a presynaptic response. There are ...
Calcium sulfate. Strontium sulfate. Barium sulfate Except where otherwise noted, data are given for materials in their standard ... Channel blockers. class I. (Na+ channel blockers). class Ia (Phase 0→ and Phase 3→). *Ajmaline ... Other inorganic sulfate salts such as sodium sulfate and calcium sulfate may be used in the same way. ... In a magnesium-deficient marine aquarium, calcium and alkalinity concentrations are very difficult to control because not ...
Dihydropyrimidinones, the products of the Biginelli reaction, are widely used in the pharmaceutical industry as calcium channel ... "Dihydropyrimidine calcium channel blockers. 4. Basic 3-substituted-4-aryl-1,4-dihydropyrimidine-5-carboxylic acid esters. ...
... cell biology and biochemistry of store-operated calcium channel proteins. Opening of these channels leads to calcium entry into ... Too much or too little calcium entry can lead to disease and tissue damage which makes the Calcium release activated channels ( ... Parekh's research investigates the physiology of Calcium signalling and Calcium release activated channels (CRACs). He ... Anant Parekh's ORCID 0000-0002-4860-1644 Parekh, Anant B.; Putney, James W. (2005). "Store-Operated Calcium Channels". ...
"Calcium channel blocker poisoning". UpToDate. Retrieved 2019-07-09. https://calpoison.org/news/cardiac-glycoside-poisoning. ... a calcium transporting ATPase, as one host factor required for box jellyfish venom cytotoxicity. Antitoxin Antivenom Snakebite ...
... sensor protein responsible for sensing calcium changes in internal calcium stores and communicate with ORAI calcium channels in ... STIM-ORAI Interactions That Control the CRAC Channel. Current Topics in Membranes. Store-Operated Calcium Channels. 71. ... "STIM1 gates the store-operated calcium channel ORAI1 in vitro". Nature Structural & Molecular Biology. 17 (1): 112-116. doi: ... Hogan, Patrick G.; Lewis, Richard S.; Rao, Anjana (2010-01-01). "Molecular Basis of Calcium Signaling in Lymphocytes: STIM and ...
"Neuronal Calcium Channel Antagonists. Discrimination between Calcium Channel Subtypes Using .omega.-conotoxin from Conus Magus ... and are capable of inhibiting the activity of a number of ion channels such as calcium, sodium, or potassium channels. In many ... Choi, D (1988). "Calcium-mediated Neurotoxicity: Relationship to Specific Channel Types and Role in Ischemic Damage". Trends in ... Significantly, ω-CgTx is capable of long term binding to and inhibition of voltage-dependent calcium channels located in the ...
The resultant products bind to inositol triphosphate (IP3) receptors through calcium ion channels. The calcium comes from ... They can also block calcium ion channels to hyperpolarize postsynaptic cells. Significance[edit]. There are many applications ... DSIs can be blocked by ionotropic receptor calcium ion channel antagonists on the somata and proximal apical dendrites of CA1 ... These depolarizations activate voltage-dependent calcium channels. They later become hyperpolarizing as the mammal matures. To ...
With the emergence of two-photon microscopy and calcium imaging, we now have powerful experimental methods with which to test ... Voltage sensitive ion channels are glycoprotein molecules which extend through the lipid bilayer, allowing ions to traverse ... "Intracellular Calcium Dynamics Permit a Purkinje Neuron Model to Perform Toggle and Gain Computations Upon its Inputs" ... "Intracellular Calcium Dynamics Permit a Purkinje Neuron Model to Perform Toggle and Gain Computations Upon its Inputs" ...
Veins sunken below the surface, resulting in a rounded channel. Sometimes confused with "guttered" because the channels may ... Cote, G. G. (2009). "Diversity and distribution of idioblasts producing calcium oxalate crystals in Dieffenbachia seguine ( ... Vein is sunk below the surface, more prominent than surrounding tissues but more sunken in channel than with impressed veins. e ... Veins partly prominent, the crest above the leaf lamina surface, but with channels running along each side, like gutters. ...
Other research has also suggested that calcium flow through N-type calcium channels is essential for normal breathing, and is ... Other potassium channels like large conductance calcium-dependent potassium channels and sodium chloride dependent potassium ... voltage gated calcium channels become activated and calcium is able to flow into the cell which usually leads to the release of ... L-type calcium channels are known to increase the frequency of action potentials in some neurons, which might be the reason ...
... and an enzyme in the toxic saliva is used to dissolve the calcium carbonate of the shell. It takes about three hours for O. ...
See also: Receptor/signaling modulators • Ion channel modulators. Taxon identifiers. *Wikidata: Q146217 ...
... which opens ion channels (largely sodium channels, though calcium can enter through these channels as well). The positive ... This change in the cell's membrane potential causes voltage-gated calcium channels to close. This leads to a decrease in the ... A decrease in the intracellular calcium concentration means that less glutamate is released via calcium-induced exocytosis to ... Thus, the random opening or closing of sodium channels will not affect the membrane potential of the cell; only the closing of ...
The eggs hatch in about 2 weeks, and the tiny larvae tunnel to the wood and score its surface with their feeding channels. With ... calcium, magnesium, and sulfur, all used in relatively large amounts (Buckman and Brady 1969).[31] Nutrient concentrations in ... when larvae occasionally return to the surface of the wood and extend the feeding channels generally in a U-shaped ...
Calcium Scandium Titanium Vanadium Chromium Manganese Iron Cobalt Nickel Copper Zinc Gallium Germanium Arsenic Selenium Bromine ... Hellgren, Mikko; Sandberg, Lars; Edholm, Olle (2006). "A comparison between two prokaryotic potassium channels (KirBac1.1 and ... Similar solutions are formed by the heavy divalent alkaline earth metals calcium, strontium, barium, as well as the divalent ... calcium (1.5%), and aluminium (1.4%); with the remaining 1.2% consisting of trace amounts of other elements. Due to planetary ...
265-268 "(...) the equality of the two channels is known to be preserved from high energy through 20 keV and down to about 5 ... Several medium and heavy elements like calcium, titanium, chromium, manganese, iron, cobalt, copper and zinc have been reported ... where the first channel predominates due to 'molecular resonance excitation']", Huizenga 1993, pp. 6-7, 35-36, 75, 108-109, 112 ...
The link was a single nucleotide polymorphism of two genes involved in calcium channel signaling with neurons. One of these ... Both males and females with larger combs have higher bone density and strength, which allows females to deposit more calcium ... the part of the bone that transfers calcium into developing eggshells) are located at the same locus as the gene affecting comb ...
"Mitochondrial Ion Channels: Gatekeepers of Life and Death". Physiology. 20 (5): 303-315. doi:10.1152/physiol.00020.2005. ISSN ...
性鈣通道(英語:Voltage-dependent calcium channel). 突觸後致. 密物質(英語:Postsynaptic density) ... 鉀離子通道阻滯劑(英語:Potassium channel blocker) (PCB) ... 鈉離子通道阻滯劑(英語:Sodium channel blocker) (SCB
Mark Akeson joined the research effort in 1997, and in 1999 published a paper showing that the hemolysin channel, now referred ... His advisor was David Cornwell, a lipid biochemist, so Deamer focused on calcium interactions with fatty acid and phospholipid ... the two established methods for monitoring proton permeation through ion channels such as gramicidin. In 1989, while returning ... "Characterization of individual polynucleotide molecules using a membrane channel". Proceedings of the National Academy of ...
calcium channel activity. • aspartic-type endopeptidase activity. • endopeptidase activity. • hydrolase activity. • aspartic ... endoplasmic reticulum calcium ion homeostasis. • response to oxidative stress. • autophagosome assembly. • positive regulation ... smooth endoplasmic reticulum calcium ion homeostasis. • synaptic vesicle targeting. • Cajal-Retzius cell differentiation. • ... cellular calcium ion homeostasis. • epithelial cell proliferation. • neuron migration. • negative regulation of apoptotic ...
States in which ginger is exported follow the marketing channels of vegetable marketing in India, and the steps are similar to ... water channels are made 60-80 ft apart to irrigate the crop.[29] ... Calcium (intracellular). *Cold. *Coolact P. *Cooling Agent 10. ...
Calcium Channel Blockers. CCB. 降血壓. 鈣質. Calcium. -. 骨骼細胞營養所需 ... Better Health Channel. [2011-07-21]. (原始内容存档于2011-
GABA receptors contain a binding site for the chemical, GABA, a chloride ion channel, and an additional binding site for ... Disulfiram-like drugs: disulfiram, calcium carbimide, cyanamide. Sulfonic acids: Acamprosate. Religion and alcohol. *Christian ...
Wnt signaling pathway, calcium modulating pathway. • Wnt signaling pathway, planar cell polarity pathway. • beta-catenin ... "IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.. ...
Calcium supports child growth in many varying ways. Common sources of calcium are found in dates, grapefruit,oranges, celery, ... Better Health Channel. 2015-02-09. Retrieved 03/04/2015. Check date values in: ,access-date= (help) "Healthy Kids Association ... A diet rich with Calcium, Vitamin C, B Vitamins, Iodine and Zinc ensures a growing child receives the most benefits from the ... Foundation for strong healthy bones and teeth - majority of the calcium consumed as a child is deposited onto collagen bone ...
Epithelial sodium channel blockers: amiloride and triamterene.. Calcium-sparing diureticsEdit. The term "calcium-sparing ... The reduced concentration of calcium in the urine can lead to an increased rate of calcium in serum. The sparing effect on ... calcium chloride, ammonium chloride 1. Arginine vasopressin. receptor 2 antagonists amphotericin B, lithium[13][14]. Inhibits ... The potassium-sparing diuretics cause a net increase in calcium lost in urine, but the increase is much smaller than the ...
See also: Receptor/signaling modulators • Ion channel modulators. Taxon identifiers. *Wikidata: Q122679 ...
See also: Receptor/signaling modulators • Ion channel modulators. Retrieved from "https://en.wikipedia.org/w/index.php?title= ...
NMDA receptor activation by rapid successive firing allows calcium influx in addition to sodium. The calcium influx triggered ... will communicate regularly and maintain the synapse structure and function long after the initial activation of NMDA channels. ... Promoter IV activity, leading to the translation of exon IV-containing mRNA, is strongly stimulated by calcium and is primarily ... triggering a calcium influx. Through a protein signaling cascade requiring Erk, CaM KII/IV, PI3K, and PLC, NMDA receptor ...
It is made up of 70% inorganic materials (mainly hydroxylapatite and some non-crystalline amorphous calcium phosphate), 20% ... Dentine consists of microscopic channels, called dentinal tubules, which radiate outward through the dentine from the pulp to ...
Inhibition of voltage-gated sodium channels and voltage-gated calcium channels (by kavain and methysticin). ...
... voltage-gated calcium channels) ବିରୁଦ୍ଧରେ ଆଣ୍ଟିବଡି ପ୍ରସ୍ତୁତ ହେବା ଯୋଗୁ ଏହି ରୋଗ ହୁଏ । ଆଉ ମଧ୍ୟ ମାଂସପେଶୀକୁ ସଂଯୋଗ କରୁଥିବା ...
Calcium concentrations falling below the needs of some freshwater organisms. *The additive-and possibly synergistic-effects of ... which underlies many larger rivers and can contain substantially more water than is seen in the open channel. It may also be in ...
Ion channel. modulators. Calcium blockers. *Gabapentin. *Gabapentin enacarbil. *Mirogabalin. *Pregabalin. *Ziconotide. Sodium ...
... calcium channel blockers) ବା ବିଟା ବ୍ଲକର (beta blockers) ଦିଆଯାଏ । ଦୀର୍ଘକାଳୀନ ଭିତ୍ତିରେ କେତେକ ଲୋକଙ୍କର ଆସ୍ପିରିନ (aspirin) ବା ...
Taking a calcium supplement of up to 1,000 mg per day can help women live longer, according to a study whose lead author was ... Calcium supplements linked to longer lifespans in women Published: 22May2013 ... McGill research team studies how calcium compounds accumulate in the arteries Published: 31Jan2018 ... UAlberta and McGill scientists uncover a hidden calcium cholesterol connection Published: 27Jul2017 ...
... opening of the L-type calcium channel permits influx of calcium into the cell. The calcium binds to the calcium release ... High-voltage-gated calcium channels include the neural N-type channel blocked by ω-conotoxinGVIA, the R-type channel (R stands ... Voltage-gated calcium channels (VGCCs), also known as voltage-dependent calcium channels (VDCCs), are a group of voltage-gated ... In skeletal muscle, the actual opening of the channel, which is mechanically gated to a calcium-release channel (a.k.a. ...
P-type calcium channel ("Purkinje") /Q-type calcium channel. HVA (high voltage activated). Cav2.1 (CACNA1A). α2δ, β, possibly γ ... Voltage-gated calcium channels (VGCCs), also known as voltage-dependent calcium channels (VDCCs), are a group of voltage-gated ... opening of the L-type calcium channel permits influx of calcium into the cell. The calcium binds to the calcium release ... High-voltage-gated calcium channels include the neural N-type channel blocked by ω-conotoxin GVIA, the R-type channel (R stands ...
Calcium permeability of ligand-gated channels.. Burnashev N1.. Author information. 1. Max-Planck-Institut für medizinische ... Ligand-gated channels activated by excitatory neurotransmitters: glutamate, acetylcholine, ATP or serotonin are cation channels ... The functional role of the Ca2+ entry mediated by various ligand-gated channels in mammalian central nervous system is less ... Many of them have different Ca2+ permeability providing immense diversity in Ca2+ entry mediated by ligand-gated channels ...
... This learning resource is a 5-minute animation about calcium channel blocker in YouTube. Learning ... pharmacology, calcium channel blockers, heart medication, pharmacy, nursing Disciplines:. * Science and Technology / Health ... You just viewed Calcium Channel Blockers. Please take a moment to rate this material. ... about calcium channel blockers is easy and fun at Rutgers University, School of Nursing in Stratford, NJ. ...
Single channel studies have identified two types of calcium-activated potassium channel which can also be separated on ... In neurons, these currents are largely activated following calcium influx via voltage gated calcium channels active during the ... It is now clear that BK channels underlie I(c) whereas SK channels underlie I(AHP). The identity of the channels underlying I( ... Channels underlying neuronal calcium-activated potassium currents.. Sah P1, Faber ES. ...
they block the small pores in cells that let calcium pass through, and widen blood vessels as well as affect the activity o ... What are calcium channel blockers?. NEXT QUESTION: Which calcium channel blockers have been studied to treat bipolar disorder? ... How do calcium channel blockers work?. ANSWER These drugs are usually used to treat high blood pressure or heart problems. They ... So calcium channel blockers have been studied as a treatment for bipolar disorder, but there isnt enough evidence yet that ...
They prevent the calcium ions needed for muscle contraction from entering the cells of smooth and cardiac muscle. This causes ... calcium-channel blocker calcium-channel blocker. calcium-channel blocker, any of a class of drugs used in treating hypertension ... Cardizem (diltiazem) is a common calcium-channel blocker. The Columbia Electronic Encyclopedia, 6th ed. Copyright © 2012, ... Some calcium-channel blockers, such as Procardia (nifedipine), slow the electrical impulses that run through heart muscle, thus ...
... also called calcium antagonists, are a newer category of medications which are used to treat heart disease and hypertension. ... Calcium channel blockers, also called calcium antagonists, are a newer category of medications which are used to treat heart ... the calcium channel. The more calcium that gets through the door before the electrical signal comes, the more strongly the ... Calcium channel blockers, like verapamil and its cousins, do not quite lock the revolving door, but they significantly slow ...
Calcium-channel blockers are a type of medicine used to treat high blood pressure and heart rhythm disturbances. They are one ... The specific ingredients in each type of calcium-channel blocker vary. However, the main ingredient is called a calcium-channel ... Calcium-channel blockers are a type of medicine used to treat high blood pressure and heart rhythm disturbances. They are one ... Calcium channel blockers. In: Aronson JK, ed. Meylers Side Effects of Drugs. 16th ed. Waltham, MA: Elsevier; 2016:23-39. ...
A type of blood pressure lowering medication, called a calcium-channel blocker, may be linked with an increased risk of a type ... Atomic level analysis reveals how two classes of calcium channel blockers produce different effects An atomic level analysis ... Tau Therapeutics presents data of T-type calcium channel inhibitors in treatment of pancreatic cancer Tau Therapeutics LLC ... Two-drug combinations containing calcium channel blocker significantly lowers BP In the largest randomized controlled trial of ...
Calcium channel blockers are a common type of medication for high blood pressure and heart conditions. We discuss how these ... What is a calcium channel blocker?. Share on Pinterest. A doctor may prescribe calcium channel blockers to treat high blood ... Calcium channel blockers reduce the amount of calcium that can enter muscle cells in the heart and blood vessel walls via these ... Calcium channel blockers are a type of medication that people take to increase the flow of blood and oxygen to the heart. ...
... what calcium channel blocker did you try and did you have any side-effects? Did it help your migraines? I am... ... I was wondering if anyone here has tried a calcium channel blocker before? If so, ... I was wondering if anyone here has tried a calcium channel blocker before? If so, what calcium channel blocker did you try and ... I hope the Calcium Channel Blockers work for you! I dont think the Beta Blocker is working for me either at this point (we ...
Calcium channel blockers are used to treat high blood pressure. Theyre as effective as ACE inhibitors in reducing blood ... How calcium channel blockers work. CCBs reduce blood pressure by limiting the amount of calcium or the rate at which calcium ... What are calcium channel blockers?. Calcium channel blockers (CCBs) are a class of medications used to treat high blood ... Natural calcium channel blockers. Magnesium is an example of a nutrient that acts as a natural CCB. Research has shown that ...
Calcium-activated potassium channels mediate prejunctional inhibition of peripheral sensory nerves. D Stretton, M Miura, M G ... Calcium-activated potassium channels mediate prejunctional inhibition of peripheral sensory nerves. D Stretton, M Miura, M G ... Calcium-activated potassium channels mediate prejunctional inhibition of peripheral sensory nerves. D Stretton, M Miura, M G ... Calcium-activated potassium channels mediate prejunctional inhibition of peripheral sensory nerves Message Subject (Your Name) ...
Calcium channel blocking agents and the heart. Br Med J (Clin Res Ed) 1985; 291 :1150 ... Calcium channel blocking agents and the heart.. Br Med J (Clin Res Ed) 1985; 291 doi: https://doi.org/10.1136/bmj.291.6503.1150 ...
... was 90 Units (Defined Daily Dosage) Per Thousand Persons Per Day. Discover more ... How does Sweden rank in Calcium Channel Blocking Medicine Use?. #. 28 Countries. Units (Defined Daily Dosage) Per Thousand ... Since 2014, Sweden Calcium Channel Blocking Medicine Use rose 3% year on year. In 2019, the country was number 3 comparing ... Sweden - Calcium Channel Blocking Medicine Use Units (Defined Daily Dosage) Per Thousand Persons Per Day - 2000 to 2019 ...
... was 55 Units (Defined Daily Dosage) Per Thousand Persons Per Day. Discover ... How does Iceland rank in Calcium Channel Blocking Medicine Use?. #. 28 Countries. Units (Defined Daily Dosage) Per Thousand ... Since 2014, Iceland Calcium Channel Blocking Medicine Use increased 3.5% year on year. With 54.6 Units (Defined Daily Dosage) ... Iceland - Calcium Channel Blocking Medicine Use Units (Defined Daily Dosage) Per Thousand Persons Per Day - 1989 to 2019 ...
Channels were inhibited by verapamil and lanthanum. These channels could participate in the regulation of cytoplasmic Ca2+ by ... Free calcium (Ca2+) in the cytoplasm of plant cells is important for the regulation of many cellular processes and the ... The patch-clamp technique was used to study Ca2+ channels in the vacuole of sugar beet cells. Vacuolar currents showed inward ... Control of cytoplasmic Ca2+ involves the activity of pumps, carriers, and possibly ion channels. ...
Here we have elucidated the role of R-type Ca(V)2.3 channels in that process. A 20% reduction in glucose-evoked insulin ... channel isoforms may determine the kinetics of insulin release from pancreatic islets. ... CaV2.3 calcium channels control second-phase insulin release J Clin Invest. 2005 Jan;115(1):146-54. doi: 10.1172/JCI22518. ... We propose a specific role for Ca(V)2.3 Ca(2+) channels in second-phase insulin release, that of mediating the Ca(2+) entry ...
... Jason Kennerly jkenner at cello.gina.calstate.edu Fri Sep 1 20:06:46 EST 1995 *Previous ...
P-type calcium channel ("Purkinje") /Q-type calcium channel. HVA (high voltage activated). Cav2.1 (CACNA1A). α2δ, β, possibly γ ... "calcium channel" at Dorlands Medical Dictionary *^ Striggow F, Ehrlich BE (August 1996). "Ligand-gated calcium channels inside ... A calcium channel is an ion channel which shows selective permeability to calcium ions. It is sometimes synonymous as voltage- ... Calcium Induced Calcium Release - CICR). RYR1, RYR2, RYR3. ER/SR. Calcium-induced calcium release in myocytes[4]. ...
Calcium channel blockers and cancer. . . and other stories BMJ 2018; 361 :k2529 ... There has been some anxiety that calcium channel blockers might encourage growth of malignant cells by reducing intracellular ... mortality from breast cancer was no higher in women who had taken calcium channel blockers than in women who had never used ... Calcium channel blockers and cancer. . . and other stories. BMJ 2018; 361 doi: https://doi.org/10.1136/bmj.k2529 (Published 14 ...
... calcium channel blockers (sometimes called ccbs for short, or calcium antagonists) dont let calcium into certain muscle cells ... How do calcium channel blockers work for high blood pressure?. ANSWER To treat blood high blood pressure, calcium channel ... blockers (sometimes called CCBs for short, or calcium antagonists) dont let calcium into certain muscle cells in your heart ...
Calcium channel synonyms, Calcium channel pronunciation, Calcium channel translation, English dictionary definition of Calcium ... channel. n. 1. The bed of a stream or river. 2. The deeper part of a river or harbor, especially a deep navigable passage. 3. A ... tr.v. chan·neled, chan·nel·ing, chan·nels also chan·nelled or chan·nel·ling 1. To make or cut channels in. ... Calcium channel - definition of Calcium channel by The Free Dictionary https://www.thefreedictionary.com/Calcium+channel ...
This overload was due to the overproduction of the gene encoding a channel, known as the L-type channel, which allows calcium ... Calcium channel blockers may be effective in treating memory loss associated with Alzheimers. Treating diseased brain cells ... More of these channels means more calcium ions are able to flow into the cell, disrupting memory formation. Using a drug to ... This shows that memory loss is likely due to calcium overload because too many L-type channels are made and, if this is ...
... donderdag, 05 september 2019 - Categorie: Onderzoeken. Bron: www.ncbi.nlm.nih.gov/pmc/articles/ ... Voltage-gated calcium (Ca2+) channels are key transducers of membrane potential changes into intracellular Ca2+ transients that ... There are ten members of the voltage-gated Ca2+ channel family in mammals, and they serve distinct roles in cellular signal ... This article presents the molecular relationships and physiological functions of these Ca2+ channel proteins and provides ...
Calcium Channels. Some articles on calcium channel, calcium channels, calcium, channels, channel:. Cilnidipine. ... Cilnidipine ... INN) is a calcium channel blocker ... is a dual blocker of L-type voltage-gated calcium channels in vascular smooth muscle and ... as a selective antagonist of T-type voltage-operated calcium ion channels, because its binding blocks the channels and keeps ... it causes a calcium ion influx through voltage-gated calcium channels ... Activation of the nicotinic receptor opens its ...
One such class of medications is calcium channel blockers, or CCBs. Because untreated GERD can cause serious medical problems, ... British Journal of Clinical Pharmacology: Do Calcium Antagonists Contribute to Gastro-oesophageal Reflux Disease and ...
Calcium Channel Blockers Question:What is the risk of mortality with calcium channel blockers? Answer: There has been a lot of ... Doctors Answers to "Frequently Asked Questions" - Calcium Channel Blockers. These comments are made for the purpose of ... review by the Food and Drug Administration has recently stated that there appears to be no excess risk with calcium channel ... This was initiated after a presentation of data which compared relative mortality of beta-blockers and calcium blockers. This ...
  • This learning resource is a 5-minute animation about calcium channel blocker in YouTube. (merlot.org)
  • calcium-channel blocker, any of a class of drugs used in treating hypertension , angina pectoris , and certain arrhythmias . (factmonster.com)
  • Cardizem (diltiazem) is a common calcium-channel blocker. (factmonster.com)
  • Calcium-channel blocker overdose occurs when someone takes more than the normal or recommended amount of this medicine. (medlineplus.gov)
  • The specific ingredients in each type of calcium-channel blocker vary. (medlineplus.gov)
  • Taking too much of a calcium-channel blocker can be very dangerous. (medlineplus.gov)
  • A type of blood pressure lowering medication, called a calcium-channel blocker, may be linked with an increased risk of a type of bowel condition called diverticulosis. (news-medical.net)
  • In the largest randomized controlled trial of treatment for high blood pressure ever conducted in sub-Saharan Africa, two frontline two-drug combinations that included the long-acting calcium channel blocker, amlodipine, were able to drive down blood pressure levels more than a third two-drug combination that did not include amlodipine, according to research presented at the American College of Cardiology's 68th Annual Scientific Session. (news-medical.net)
  • What is the definition of calcium-channel blocker? (webmd.com)
  • Doctors may prescribe a calcium channel blocker to treat high blood pressure or a variety of heart conditions. (medicalnewstoday.com)
  • What is a calcium channel blocker? (medicalnewstoday.com)
  • A doctor may sometimes prescribe an ACE inhibitor with a calcium channel blocker. (medicalnewstoday.com)
  • There are two different types of calcium channel blocker, which are called dihydropyridines and nondihydropyridines. (medicalnewstoday.com)
  • I was wondering if anyone here has tried a calcium channel blocker before? (medhelp.org)
  • If so, what calcium channel blocker did you try and did you have any side-effects? (medhelp.org)
  • since I have not tried a calcium channel blocker, I realized that maybe I should suggest this to my neurologist as our next step before the 'slightly controversial' next step. (medhelp.org)
  • so, maybe I will talk to my neurologist about the possibility of trying a Calcium Channel Blocker for me too. (medhelp.org)
  • If your neurologist does end up putting you on a blood pressure medication, and it turns out to be a Calcium Channel Blocker instead of a Beta Blocker. (medhelp.org)
  • They tried all the preventatives on me, Imipramine(anti-depressant), Nadolol ( beta blocker) and a few others nothing worked so we thought we had to do something as I have had a migraine now for months---from about the 5th Oct till yesterday I was migraine free with the Diltiazem CD (calcium blocker for blood pressure), so it does help me. (medhelp.org)
  • A 20% reduction in glucose-evoked insulin secretion was observed in Ca(V)2.3-knockout (Ca(V)2.3(-/-)) islets, close to the 17% inhibition by the R-type blocker SNX482 but much less than the 77% inhibition produced by the L-type Ca(2+) channel antagonist isradipine. (nih.gov)
  • The team's findings, published in Frontiers in Cellular Neuroscience , found treating a diseased brain cell with a blocker of the L-type channel reduced the number of calcium ions able to flow into the brain cell. (bris.ac.uk)
  • Ziconotide , a peptide compound derived from the omega- conotoxin , is a selective N-type calcium channel blocker that has potent analgesic properties that are equivalent to approximate 1,000 times that of morphine . (wikipedia.org)
  • These images are a random sampling from a Bing search on the term "Dihydropyridine Calcium Channel Blocker. (fpnotebook.com)
  • NBC News , 9 July 2018 Among the 4,338 women who had taken a short-acting calcium channel blocker for high blood pressure, 45 (or about 1%) were diagnosed with pancreatic cancer. (merriam-webster.com)
  • These example sentences are selected automatically from various online news sources to reflect current usage of the word 'calcium channel blocker. (merriam-webster.com)
  • New pharmaceutical products may have both a calcium channel blocker and a second antihypertensive such as an angiotensin-converting enzyme inhibitor or an angiotensin receptor blocker. (medscape.com)
  • When calcium channel blocker (CCB) ingestion is suspected, specifically question the patient or family about symptoms that may indicate cardiac or pulmonary manifestations of calcium channel blocker toxicity. (medscape.com)
  • The cardiac, vascular, and neurologic examinations deserve particular attention, because calcium channel blocker (CCB) toxicity manifests most physical findings in these systems. (medscape.com)
  • Posicor has a long half-life of 17 to 25 hours and a prolonged washout period may be required after discontinuation of the calcium channel blocker prior to initiation of other antihypertensive agents. (mercola.com)
  • The calcium channel blocker amlodipine decreases the risk of cardiovascular events (such as heart attack or heart-disease related deaths) in patients with coronary artery disease and normal blood pressure, as does the ACE inhibitor enalapril, but to a lesser extent, according to a study in the November 10 issue of JAMA. (eurekalert.org)
  • Angiotensin II inhibitors with calcium channel blocking agents is a combination medicine containing both an angiotensin II inhibitor and a calcium channel blocker. (drugs.com)
  • So some people have a spasm in their artery, calcium channel blocker as a joint is more likely to relax that and prevent that from happening. (sharecare.com)
  • Side effects of these drugs may include but are not limited to: Constipation Peripheral edema, which can occur in as much as 70% of people receiving calcium channel blocker, is caused by calcium channel blockers' preferential arteriolar or precapillary dilation without commensurate dilation in the venous or postcapillary circulation. (wikipedia.org)
  • Alcohol, combined with a calcium channel blocker, can cause severe side effects and may also affect the way the medication works. (everydayhealth.com)
  • CAMBRIDGE, Mass.--( BUSINESS WIRE )-- Zalicus Inc. (Nasdaq Capital Market: ZLCS) a biopharmaceutical company that discovers and develops novel treatments for patients suffering from pain, today announced that it is advancing Z944, its novel oral T-type calcium channel blocker, into further clinical development in the third quarter of 2013. (aol.com)
  • T-type calcium channels are known to be widely implicated in the frequency and intensity of pain signals, and we believe Z944 is the most advanced T-type calcium channel blocker currently in clinical development,' commented Mark H.N. Corrigan, MD, President and CEO of Zalicus. (aol.com)
  • Z944 is a novel, oral, state-dependent, selective T-type calcium channel blocker that has demonstrated preclinical efficacy in multiple inflammatory pain models. (aol.com)
  • DALLAS, July 7 -- Boston researchers say they have evidence that supports the safety of nifedipine, a calcium channel blocker used to treat high blood pressure. (eurekalert.org)
  • However, two large studies in the past five years have generated concerns that they may be dangerous for some individuals, The two studies included an investigation that pooled data from 15 trials involving about 10,000 patients with unstable angina pectoris or heart attack and found an increase in deaths among patients taking a short-acting form of the calcium channel blocker nifedipine. (eurekalert.org)
  • Some evidence suggests that the bioflavonoid naringen may interact with medications in the calcium channel blocker family, increasing blood levels of the drug. (medicalcityhospital.com)
  • The report covers forecast and analysis for the calcium channel blocker market on a global and regional level. (researchandmarkets.com)
  • The study includes drivers and restraints for the Calcium channel blocker market along with the impact they have on the demand in the forecast period. (researchandmarkets.com)
  • Additionally, the report includes the study of opportunities available in the calcium channel blocker market on a global level. (researchandmarkets.com)
  • In order to give the users a comprehensive view on the calcium channel blocker market and to understand the competitive landscape in the market, an analysis of Porter's Five Forces model for the calcium channel blocker market has also been included. (researchandmarkets.com)
  • Our findings on short-acting calcium channel blocker use and pancreatic cancer risk are novel and of potential broad medical and public health significance if confirmed," Wang said in a press release. (healio.com)
  • Your doctor will offer you the calcium-channel blocker that is most suitable for you. (bupa.co.uk)
  • According to expert consensus recommendations, first-line therapies for symptomatic calcium channel blocker (CCB) poisoning include which of the following? (the-hospitalist.org)
  • Combining an ACE inhibitor with a calcium channel blocker more effectively reduces the risk of cardiovascular events than an ACE inhibitor with a diuretic, a major new trial concludes. (pulsetoday.co.uk)
  • ACCOMPLISH was stopped early after finding clear benefits for the calcium channel blocker combination, and the results were published in the New England Journal of Medicine last week. (pulsetoday.co.uk)
  • Current guidance from NICE and the British Hypertension Society recommends combining a calcium channel blocker or a diuretic with an ACE inhibitor as second-line treatment of hypertension, but the best combination has not been established. (pulsetoday.co.uk)
  • But the ACCOMPLISH study, of more than 11,000 hypertensive patients at high risk of cardiovascular events, found treatment with an ACE inhibitor plus a calcium-channel blocker produced better outcomes than an ACE inhibitor plus a diuretic. (pulsetoday.co.uk)
  • Mean blood pressure in the calcium channel blocker group was 131.6/73.3 mmHg, compared with 132.5/74.7 mm Hg in the diuretic group. (pulsetoday.co.uk)
  • The calcium channel blocker group also had fewer recorded adverse events, with a total of 552 (9.6%), compared with 679 (11.8%) with the diuretic. (pulsetoday.co.uk)
  • Patients treated with an ACE inhibitor and a calcium channel blocker were 21% less likely to suffer a cardiovascular disease-related death or non-fatal heart attack or stroke than those in the diuretic group. (pulsetoday.co.uk)
  • Though calcium channel blocker mood regulation effects are smaller in magnitude than those produced by lithium or the anticonvulsant mood stabilizers, they are nevertheless useful for some patients, and thus are deserving of mention. (mentalhelp.net)
  • Excessive activation of VGCCs is a major component of excitotoxicity, as severely elevated levels of intracellular calcium activates enzymes which, at high enough levels, can degrade essential cellular structures. (wikipedia.org)
  • There has been some anxiety that calcium channel blockers might encourage growth of malignant cells by reducing intracellular calcium concentrations and inhibiting apoptotic gene expression. (bmj.com)
  • In plant cells, the vacuole serves as an intracellular calcium store and buffer. (sciencemag.org)
  • have identified the TPC1 gene as encoding the cation channel responsible for Ca 2+ -dependent Ca 2+ release in response to micromolar concentrations of intracellular calcium. (sciencemag.org)
  • The tau inact was also longer with BAPTA in the whole-cell pipette compared to EGTA, suggesting that tau inact reflects primarily the rate of accumulation of intracellular calcium. (jneurosci.org)
  • Recent findings identified intracellular calcium as an important regulator of both basal and induced autophagy. (frontiersin.org)
  • These channels are slightly permeable to sodium ions, so they are also called Ca2+-Na+ channels, but their permeability to calcium is about 1000-fold greater than to sodium under normal physiological conditions. (wikipedia.org)
  • The concentration of calcium (Ca2+ ions) is normally several thousand times higher outside the cell than inside. (wikipedia.org)
  • They prevent the calcium ions needed for muscle contraction from entering the cells of smooth and cardiac muscle. (factmonster.com)
  • A calcium channel is an ion channel which shows selective permeability to calcium ions. (wikipedia.org)
  • The researchers used fruit flies to study AD, using a fluorescent molecule called GCaMP6f, which reports the amount of calcium ions inside brain cells. (bris.ac.uk)
  • They found that diseased brain cells become overloaded with calcium ions, which at normal levels are important for memory formation. (bris.ac.uk)
  • This overload was due to the overproduction of the gene encoding a channel, known as the L-type channel, which allows calcium ions to flow into the cell from outside. (bris.ac.uk)
  • More of these channels means more calcium ions are able to flow into the cell, disrupting memory formation. (bris.ac.uk)
  • Using a drug to block the L-type channel reversed the effect of disease and reduced the flow of calcium ions to a normal level. (bris.ac.uk)
  • However, if the overproduction of L-type channels was corrected in the diseased flies, their brain cells were no longer overloaded with calcium ions and their memory was just as good as healthy flies. (bris.ac.uk)
  • Voltage-gated calcium channels open in unison, rather than independently, to allow calcium ions into and activate excitable cells such as neurons and muscle cells, researchers with UC Davis Health System and the University of Washington have found. (biologynews.net)
  • Any of a class of drugs that inhibit the movement of calcium ions across the cell membranes of cardiac and smooth muscle and are used to treat cardiovascular disorders. (thefreedictionary.com)
  • Medicine) any drug that prevents the influx of calcium ions into cardiac and smooth muscle: used to treat high blood pressure and angina. (thefreedictionary.com)
  • The opening and closing of these channels by depolarizing stimuli, such as action potentials, allows Ca2+ ions to enter neurons down a steep electrochemical gradient, producing transient intracellular Ca2+ signals. (ebi.ac.uk)
  • The alpha-1 subunit forms the pore for the import of extracellular calcium ions and, though regulated by the other subunits, is primarily responsible for the pharmacological properties of the channel [ PMID: 11031246 ]. (ebi.ac.uk)
  • Voltage-gated calcium channels swing open with passing action potentials, allowing calcium ions into the cell, and slide shut when the membrane depolarization has passed. (alzforum.org)
  • Voltage-activated calcium channels open in response to membrane depolarization allowing the entry of calcium ions into excitable cells that in turn triggers multiple cellular events including neurotransmission, excitation-contraction coupling, gene expression and hormone secretion. (fz-juelich.de)
  • The α1 subunit pore (~190 kDa in molecular mass) is the primary subunit necessary for channel functioning in the HVGCC, and consists of the characteristic four homologous I-IV domains containing six transmembrane α-helices each. (wikipedia.org)
  • Gabapentinoids , such as gabapentin and pregabalin , are selective blockers of α2δ subunit -containing voltage-gated calcium channels . (wikipedia.org)
  • Rojas CV, Wang J, Schwartz LS, et al (1991) A Met-to-Val mutation in the skeletal muscle Na+ channel a subunit in hyperkalemic periodic paralysis. (springer.com)
  • The 1 subunit is the ion conduction channel and contains the binding sites for calcium channel blockers and toxins. (uni-muenchen.de)
  • The pore is formed by the alpha-1 subunit which incorporates the conduction pore, the voltage sensor and gating apparatus, and the known sites of channel regulation by second messengers, drugs, and toxins [ PMID: 14657414 ]. (ebi.ac.uk)
  • Recent findings of TMEM16B in photoreceptor terminals ( 10 ) and olfactory neuron cilia ( 11 ) suggest that calcium-activated chloride channels containing the TMEM16B subunit likely fulfill the negative and positive feedback regulation, respectively, in these sensory neurons. (pnas.org)
  • We found that unc-2 encodes a homologue of a voltage-sensitive calcium-channel α-1 subunit. (nature.com)
  • Movements of individual Ca 2+ channels were tracked by coupling quantum dots to an antibody against the extracellular α 2 δ 4 Ca 2+ channel subunit. (jneurosci.org)
  • L-type Ca V channels are composed of a pore-forming α subunit, with accessory β, α 2 δ and γ subunits ( Catterall, 2000 ). (jneurosci.org)
  • we therefore chose the α 2 δ 4 subunit as a target for labeling Ca V channels in living tissue. (jneurosci.org)
  • This book reviews the influence of α2/β subunit in setting the biophysical properties of calcium channels, the connection of α2/β with diseases, and the functions of α2/β that are now being unraveled. (novapublishers.com)
  • Belongs to the calcium channel alpha-1 subunit (TC 1.A.1.11) family. (abcam.com)
  • Calcium channel blockers, like verapamil and its cousins, do not quite 'lock' the revolving door, but they significantly slow it down. (healthcentral.com)
  • Channels were inhibited by verapamil and lanthanum. (sciencemag.org)
  • Korin Miller, SELF , 12 July 2018 Verapamil is a drug that lowers blood pressure and in a class called calcium channel blockers . (merriam-webster.com)
  • The cardiovascular drugs that have the most favorable profile would be the class of alpha-blockers, ACE inhibitors and ARBs--venodilators, nitrates and slow calcium channel blockers (with the exception of verapamil, which may cause a significant decrease in heart rate response at peak exercise. (thefreedictionary.com)
  • Cranefield PF, Aronson RS, Wit AL (1974) Effect of verapamil on the normal action potential and on calcium-dependent slow response canine cardiac Purkinje fibers. (springer.com)
  • Fendiline Gallopamil Verapamil (Calan, Isoptin) Benzothiazepine calcium channel blockers belong to the benzothiazepine class of compounds and are an intermediate class between phenylalkylamine and dihydropyridines in their selectivity for vascular calcium channels. (wikipedia.org)
  • Bar-Or D and Gasiel Y. Calcium and calciferol antagonise effect of verapamil in atrial fibrillation. (medicalcityhospital.com)
  • Reversal of the cardiovascular effects of verapamil by calcium and sodium: differences between electrophysiologic and hemodynamic responses. (medicalcityhospital.com)
  • Treatment of severe left ventricular dysfunction with calcium chloride in patients receiving verapamil. (medicalcityhospital.com)
  • Intravenous verapamil for treatment of multifocal atrial tachycardia with and without calcium pretreatment. (medicalcityhospital.com)
  • Calcium gluconate in severe verapamil intoxication. (medicalcityhospital.com)
  • Low-dose calcium pretreatment to prevent verapamil-induced hypotension. (medicalcityhospital.com)
  • non-dihydropyridines, or 'rate-limiting' calcium-channel blockers (for example diltiazem and verapamil). (bupa.co.uk)
  • Voltage-gated calcium channels are formed as a complex of several different subunits: α1, α2δ, β1-4, and γ. (wikipedia.org)
  • This arrangement is analogous to a homo-tetramer formed by single-domain subunits of voltage-gated potassium channels (that also each contain 6 TM helices). (wikipedia.org)
  • Molecular cloning revealed a large variety of the ligand-gated channel subunits differentially expressed in mammalian brain. (nih.gov)
  • In situ hybridization revealed the presence of different BK channel splice variants (X1 +24 , X2 +92 , SS2 +174 and SS4 +81 ) in combination with β 1, β 2, and β 4 subunits in rat cerebral arteries [ 13 ]. (hindawi.com)
  • Members of a previously unidentified family of potassium channel subunits were cloned from rat and human brain. (sciencemag.org)
  • The channels that formed from the various subunits displayed differential sensitivity to apamin and tubocurare. (sciencemag.org)
  • The high-voltage-activated calcium channel is a multimeric protein complex containing 1, 2/δ, β, and γ subunits. (uni-muenchen.de)
  • The smooth and cardiac muscle L-type calcium channel 1 subunits are splice variants of the same gene. (uni-muenchen.de)
  • L-type calcium channels are formed from alpha-1S, alpha-1C, alpha-1D, and alpha-1F subunits. (ebi.ac.uk)
  • The TMEM16A expression pattern established in this study thus provides a roadmap for the analyses of physiological functions of calcium-activated chloride channels that contain TMEM16A subunits. (pnas.org)
  • The molecular identification of TMEM16A and TMEM16B as CaCC subunits has made it possible to examine the physiological functions of calcium-activated chloride channels in molecular and genetic studies. (pnas.org)
  • α 2 δ 4 antibodies labeled photoreceptor terminals and colocalized with antibodies to synaptic vesicle glycoprotein 2 and voltage-gated Ca 2+ channel 1.4 (Ca V 1.4) α 1 subunits. (jneurosci.org)
  • The α2/β subunits form part of voltage-dependent calcium channels and as such are considered accessory proteins. (novapublishers.com)
  • Initial inquiries into the function of α2/β subunits revealed that they modify the voltage dependence, amplitude and kinetics of calcium currents. (novapublishers.com)
  • Calcium channel blockers, also called calcium antagonists, are a newer category of medications which are used to treat heart disease and hypertension . (healthcentral.com)
  • They're also called calcium antagonists. (healthline.com)
  • Calcium channel blockers ( CCB ), calcium channel antagonists or calcium antagonists [2] are a group of medications that disrupt the movement of calcium ( Ca 2+ ) through calcium channels . (wikipedia.org)
  • 1,4-dihydropyridines act as antagonists of these channels [ PMID: 12825828 , PMID: 15336981 ]. (ebi.ac.uk)
  • Calcium channel blockers (sometimes called calcium antagonists) are drugs that affect the way calcium passes into certain muscle cells and they are the most commonly prescribed medication for primary Raynaud's phenomenon. (cochrane.org)
  • Long-acting dihydropyridine calcium antagonists. (biomedsearch.com)
  • 10 nM), which blocks large conductance Ca(2+)-activated K(+)-channel function, completely blocked and reversed the inhibitory effects of a mu-opioid agonist, neuropeptide Y, and an alpha 2-adrenoceptor agonist on excitatory NANC responses. (pnas.org)
  • Vacuolar currents showed inward rectification at negative potentials, with a single-channel conductance of 40 picosiemens and an open probability dependent on potential. (sciencemag.org)
  • Increased calcium conductance in the neurons leads to increased depolarization and excitability. (wikipedia.org)
  • Calcium channel blockers reduce the neuronal calcium conductance and reduce the likelihood of experiencing epileptic attacks. (wikipedia.org)
  • The distribution, function, and pharmacology of these channels are consistent with the SK class of small-conductance,calcium-activated potassium channels, which contribute to the afterhyperpolarization in central neurons and other cell types. (sciencemag.org)
  • In this chapter we discuss the data obtained for a calcium-activated potassium channel of large unitary conductance. (springer.com)
  • In cell- attached patches, transient increases in [Ca2+]i following cell depolarization also resulted in inactivation of NMDA channels without altering the single-channel conductance. (jneurosci.org)
  • Voltage-gated calcium channels are classified as T, L, N, P, Q and R, and are distinguished by their sensitivity to pharmacological blocks, single-channel conductance kinetics, and voltage-dependence. (ebi.ac.uk)
  • Small conductance Ca 2+ -activated K + (SK) channels play significant roles in regulating the excitability of cardiomyocytes (CMs). (ahajournals.org)
  • Single channel studies have identified two types of calcium-activated potassium channel which can also be separated on biophysical and pharmacological grounds and have been named BK and SK channels. (nih.gov)
  • Initial hypoperfusion after exposure of cerebral vessels to oxyhemoglobin correlates with a suppression of voltage-gated potassium channel activity, whereas delayed cerebral vasospasm involves changes in other potassium channel and voltage-gated calcium channels expression and function. (hindawi.com)
  • Here, changes in calcium and potassium channel expression and function in animal models of subarachnoid hemorrhage and transient global ischemia are systematically reviewed and their clinical significance discussed. (hindawi.com)
  • Using the patch clamp technique, we were able to identify and characterize a calcium-activated potassium channel in the plasma membrane of lymphocytes from both strains of rat. (ahajournals.org)
  • Many patients with hypertension have benefited from calcium channel blockers. (healthcentral.com)
  • L-type calcium channel blockers are used to treat hypertension . (wikipedia.org)
  • [3] Calcium channel blockers are used as antihypertensive drugs , i.e., as medications to decrease blood pressure in patients with hypertension . (wikipedia.org)
  • N-type , L-type , and T-type voltage-dependent calcium channels are present in the zona glomerulosa of the human adrenal gland , and CCBs can directly influence the biosynthesis of aldosterone in adrenocortical cells , with consequent impact on the clinical treatment of hypertension with these agents . (wikipedia.org)
  • Calcium channel blockers are typically used to treat hypertension and have been viewed with caution in the United States since 1995, when the initial findings of several scattered studies found a possible link to heart attacks, strokes, cancer, gastrointestinal bleeding, and perhaps even Parkinson's disease, according to Brant S. (thefreedictionary.com)
  • the receptor-operated calcium channels (in vasoconstriction) P2X receptors L-type calcium channel blockers are used to treat hypertension. (wikipedia.org)
  • Fan Z, Chen Y, Liu H. Calcium channel blockers for pulmonary arterial hypertension. (cochrane.org)
  • Calcium channel-blockers are used to treat hypertension , angina , heart arrhythmias , and other heart-related conditions. (medicalcityhospital.com)
  • Short-acting calcium channel blockers are still prescribed to manage hypertension, which is one of the components of metabolic syndrome, and metabolic syndrome is a possible risk factor for pancreatic cancer. (healio.com)
  • Inhibits transmembrane calcium influx (prevents calcium from entering cells) in cardiac (heart) and vascular smooth muscle (blood vessel walls). (exrx.net)
  • In cardiac muscle, if these channels don't coordinate their firing, it will have detrimental repercussions on the reliability of the cardiac muscle contractions," said Luis Fernando Santana, professor and chair of the Department of Physiology and Membrane Biology at UC Davis. (biologynews.net)
  • In skeletal muscle, the L-type calcium channels act as a voltage sensor for excitation-contraction coupling, and in cardiac muscle, they provide a pathway for calcium influx. (ebi.ac.uk)
  • Calcium channel blockers are medicates that relax the arteries, says Mary Ann McLaughlin, MD, medical director of the Cardiac Health Program at The Mount Sinai Medical Center. (sharecare.com)
  • Bose, Diptiman D. "Store-Operated Calcium Entry Channels: Potential Role in Cardiac Function. (igi-global.com)
  • Our previous studies revealed that cardiac SK2 channels coupled with L-type Ca 2+ channels (LTCCs) through a physical bridge, α-actinin2, suggesting that LTCCs may be functionally coupled with SK2 channels by providing local Ca 2+ domain to activate the SK channels. (ahajournals.org)
  • However, a recent study suggested that sarcoplasmic reticulum (SR) Ca 2+ release is necessary and sufficient for the activation of cardiac SK channels. (ahajournals.org)
  • Furthermore, changes in SK channel activation kinetics following SR Ca 2+ depletion suggest both LTCC-mediated Ca 2+ influx and SR Ca 2+ release are necessary for the activation of cardiac SK channels. (ahajournals.org)
  • Calcium channel blockers are a class of medications that are approved to treat high blood pressure, heart failure, cardiac arrhythmias, and similar conditions. (mentalhelp.net)
  • Some calcium-channel blockers, such as Procardia (nifedipine), slow the electrical impulses that run through heart muscle, thus regulating arrhythmias. (factmonster.com)
  • Two different calcium channel blockers were included: nifedipine and nicardipine. (cochrane.org)
  • dihydropyridine calcium-channel blockers (for example amlodipine, felodipine and nifedipine) which make your arteries become wider. (bupa.co.uk)
  • The CGI component is attributed to the binding of the Ca2+-binding signaling protein calmodulin (CaM) to at least 1 site on the channel, as Ca2+-null CaM mutants abolish CGI in L-type channels. (wikipedia.org)
  • See protein channel . (thefreedictionary.com)
  • The channels coordinate through a protein called calmodulin, which binds to calcium and helps carry it through the channel. (biologynews.net)
  • We suggest that [Ca2+]i transients induce NMDA channel inactivation by binding to either the channel or a nearby regulatory protein to alter channel gating. (jneurosci.org)
  • An IP 3 receptor-binding protein enhances sensitivity of the Ca 2+ release channel to feedback inhibition by Ca 2+ . (sciencemag.org)
  • The localized endoplasmic reticulum protein, stromal interaction molecule (STIM) and plasma membrane Ca2+ channels, ORAI form the minimal functional unit of SOCE. (igi-global.com)
  • Synthetic peptide from the N-terminus of Human Two pore calcium channel protein 2 (NM_139075.3). (abcam.com)
  • To mediate these heterogeneity of biological actions, these channels are targeted to specific sites at the plasma membrane where they form supramolecular assemblies containing diverse regulatory and protein effectors that couple the influx of calcium to a particular downstream signal cascade. (fz-juelich.de)
  • The life of the channel protein starts in the endoplasmic reticulum. (fz-juelich.de)
  • We combine molecular biology, protein biochemistry, electrophysiology and laser scanning and spinning disk microscopy to study and track fluorescently labeled calcium channels in living cells. (fz-juelich.de)
  • PURPOSE: We investigated whether dipyridamole and various calcium channel blockers are inhibitors and/or substrates of breast cancer resistance protein (BCRP). (biomedsearch.com)
  • A set of fluorophenoxyanilides, designed to be simplified analogues of previously reported ω-conotoxin GVIA mimetics, were prepared and tested for N-type calcium channel inhibition in a SH-SY5Y neuroblastoma FLIPR assay. (mdpi.com)
  • 2,4 Whether an increase in vascular calcium-activated potassium (K Ca ) channel activity after NO synthesis inhibition could contribute to the maintenance of basal conduit artery diameter and mechanics has never been investigated in vivo in humans. (ahajournals.org)
  • 16-19 Thus, the present study was designed to assess in vivo, at the level of the radial artery, the effect of the acute vascular K Ca channel blockade in the regulation of basal conduit artery diameter and mechanical properties before and after inhibition of NO synthesis. (ahajournals.org)
  • Since lymphatic drainage relies on contraction of the smooth muscle inside the lymphatic vessel supported by voltage-gated calcium channels, inhibition of voltage-gated calcium channel poses a threat towards lymphatic removal of interstitial fluid essential for normal lymphatic system functioning. (wikipedia.org)
  • A class of drugs that act by selective inhibition of calcium influx through cell membranes or on the release and binding of calcium in intracellular pools. (jove.com)
  • Inhibition of the channel by FAD-PS mutants did not require γ-secretase activity or the production of Aβ40 or 42, since treatment of the cells with the γ-secretase inhibitors compound E or L-685,458 did not affect the currents. (alzforum.org)
  • Channels underlying neuronal calcium-activated potassium currents. (nih.gov)
  • In many cell types rises in cytosolic calcium, either due to influx from the extracellular space, or by release from an intracellular store activates calcium dependent potassium currents on the plasmalemma. (nih.gov)
  • In neurons, these currents are largely activated following calcium influx via voltage gated calcium channels active during the action potentials. (nih.gov)
  • In this review, we discuss the properties of the different types of calcium-activated potassium channels and the relationship between these channels and the macroscopic currents present in neurons. (nih.gov)
  • The Cav1 family forms channels mediating L-type calcium currents, the Cav2 family mediates P/Q-, N-, and R-type calcium currents, while the Cav3 family mediates T-type calcium currents. (ebi.ac.uk)
  • SK currents coupled with Ca 2+ influx via LTCCs continued to be elicited after application of caffeine, ryanodine or thapsigargin to deplete SR Ca 2+ store, suggesting that LTCCs provide the immediate Ca 2+ microdomain for the activation of SK channels in CMs. (ahajournals.org)
  • They block the small pores in cells that let calcium pass through, and widen blood vessels as well as affect the activity of nerve cells. (webmd.com)
  • They can slow the heart rate and relax blood vessels and they work by diminishing the flow of calcium between cells. (healthcentral.com)
  • When calcium flow is limited, your heart's contractions aren't as strong with each beat, and your blood vessels are able to relax. (healthline.com)
  • The goal of the present analysis is to review ion channel expression and function in healthy cerebral blood vessels as well as after SAH. (hindawi.com)
  • Calcium channel blockers block calcium from entering cells of the heart and smooth muscle in the walls of blood vessels. (drugs.com)
  • Calcium channel blockers reduce the speed at which calcium moves into heart muscle, blood vessels, and cells in the heart that control your heart rate. (everydayhealth.com)
  • Calcium channel blockers relax and widen blood vessels. (cigna.com)
  • Calcium-channel blockers restrict how much calcium can enter the muscle cells in your blood vessels. (bupa.co.uk)
  • Dihydropyridine calcium channel blockers can worsen proteinuria in patients with nephropathy . (wikipedia.org)
  • For those who suffer from angina , calcium channel blockers have proved to be among the most effective medications ever discovered. (healthcentral.com)
  • Calcium channel blockers are common medications that have a low risk of complications. (medicalnewstoday.com)
  • Calcium channel blockers (CCBs) are a class of medications used to treat high blood pressure. (healthline.com)
  • One such class of medications is calcium channel blockers, or CCBs. (livestrong.com)
  • Sandee Lamotte, CNN , 26 May 2020 That might include medication (such as blood thinners, anti-seizure medications, or calcium channel blockers that can reduce some of the symptoms of Moyamoya). (merriam-webster.com)
  • Commonly recommended medications include beta blockers, calcium channel blockers and tricyclic antidepressants. (thefreedictionary.com)
  • Calcium channel blockers are medications that relax the arteries. (sharecare.com)
  • Calcium channel blockers may interact with other medications, so always tell your doctor about every medication, recreational drug, vitamin, and supplement - whether over-the-counter (OTC) or prescription - that you are taking. (everydayhealth.com)
  • The other studied antihypertensive medications, including long-acting calcium channel blockers, did not appear associated with increased risk for pancreatic cancer. (healio.com)
  • Women who had ever used short-acting calcium channel blockers demonstrated significantly lower sRAGE levels compared with those who used any other antihypertensive medications (1,158 pg/mL vs. 1,446 pg/mL, P = 0.032). (healio.com)
  • The mechanism of action underlying ziconotide's therapeutic profile derives from its potent and selective blockade of neuronal N-type voltage-sensitive calcium channels (NVSCCs). (ingentaconnect.com)
  • This suggests that ChTX-sensitive K(+)-channel activation may be a common mechanism for the prejunctional modulation of sensory nerves in airways. (pnas.org)
  • [ 71 ] The presumed mechanism of action is through calcium antagonism. (medscape.com)
  • We report for the first time the results of an electrophysiologic study of a similar case and the successful use of calcium channel blockers, shedding light on the possible mechanism and management of these patients. (springer.com)
  • This mechanism may play a role in downregulation of postsynaptic calcium entry during sustained synaptic activity. (jneurosci.org)
  • Elevations in cytosolic calcium levels are used by all cells as a signaling mechanism for a variety of physiological processes but also represent a key even in most, if not all, degenerative processes. (utah.edu)
  • Dihydropyridine (DHP) calcium channel blockers are derived from the molecule dihydropyridine and often used to reduce systemic vascular resistance and arterial pressure. (wikipedia.org)
  • Benzothiazepine calcium channel blockers belong to the benzothiazepine class of compounds and are an intermediate class between phenylalkylamine and dihydropyridines in their selectivity for vascular calcium channels. (wikipedia.org)
  • Healthy cerebrovascular myocytes express members of several different ion channel families which regulate resting membrane potential, vascular diameter, and vascular tone and are involved in cerebral autoregulation. (hindawi.com)
  • Indeed, endothelium-derived hyperpolarizing factor (EDHF) is described as the non-NO and non-PGI 2 factor leading to smooth muscle cell hyperpolarization and relaxation by the opening of vascular K Ca channels. (ahajournals.org)
  • CCBs reduce blood pressure by limiting the amount of calcium or the rate at which calcium flows into the heart muscle and arterial cell walls. (healthline.com)
  • Several studies showed that calcium channel blockers (CCBs) reduce right ventricular hypertrophy and improve long-term haemodynamics in PAH. (cochrane.org)
  • Calcium channel blockers reduce the amount of calcium that can enter muscle cells in the heart and blood vessel walls via these channels. (medicalnewstoday.com)
  • Calcium-channel blockers slow down the amount of calcium that can get into heart muscle cells and so reduce how fast and strongly it can contract. (bupa.co.uk)
  • To examine this hypothesis, we have studied whether K(+)-channel blockers inhibit the effects of neuromodulators of sensory nerves in guinea pig bronchi by using selective K(+)-channel blockers. (pnas.org)
  • Phenylalkylamine calcium channel blockers are relatively selective for myocardium, reduce myocardial oxygen demand and reverse coronary vasospasm, and are often used to treat angina. (wikipedia.org)
  • Zalicus applies its expertise in the discovery and development of selective ion channel modulators and its combination high throughput screening capabilities to discover innovative therapeutics for itself and its collaborators in the areas of pain, inflammation, oncology and infectious disease. (aol.com)
  • This press release contains forward-looking statements within the meaning of the Private Securities Litigation Reform Act of 1995 concerning Zalicus, its product candidate Z944, its potential and the plans for its further clinical preclinical development, the Zalicus selective Ion channel modulation technology and its other business plans. (aol.com)
  • The 4-domain architecture (and several key regulatory sites, such as the EF hand and IQ domain at the C-terminus) is also shared by the voltage gated sodium channels, which are thought to be evolutionary related to VGCCs. (wikipedia.org)
  • Cannon SC, Brown RH, Corey DP (1991) A sodium channel defect in hyperkalemic periodic paralysis: potassium-induced failure of inactivation. (springer.com)
  • It shares sequence characteristics with all voltage-dependent cation channels, and exploits the same 6-helix bundle structural motif - in both sodium and calcium channels, this motif is repeated 4 times within the sequence to give a 24-helix bundle. (ebi.ac.uk)
  • changing the calcium permeability has little effect on action potentials. (wikipedia.org)
  • Researchers have found that both beta-blockers and calcium channel blockers are effective in lowering blood pressure, making them useful treatments for a variety of conditions that affect the heart, including angina and arrhythmia. (medicalnewstoday.com)
  • Recent Examples on the Web Those preventative medicine treatments include anticonvulsants, antidepressants, beta blockers and calcium channel blockers that might help control withdrawal pain without risking medication overuse headaches. (merriam-webster.com)
  • What is the role of calcium channel blockers in urinary incontinence treatment? (medscape.com)
  • In the global picture, this is yet another problem to be added to the list caused by calcium channel blockers," Furberg said. (eurekalert.org)
  • However, the main ingredient is called a calcium-channel antagonist. (medlineplus.gov)
  • This report reviews the experimental evidence from animal and human studies, both in vitro and in vivo, that the calcium channel blockers inhibit bronchoconstriction. (ingentaconnect.com)
  • Zipes DP, Fischer JC (1974) Effects of agents which inhibit the slow channel on sinus node automaticity and atrioventricular conduction in the dog. (springer.com)
  • or = 0.2 mM, suggesting that inactivation resulted from transmembrane calcium influx. (jneurosci.org)
  • The drugs attach to the surface membrane of the muscles in the artery wall and prevent calcium from entering. (healthcentral.com)
  • Depiction of binding sites of various antagonistic drugs in the L-type calcium channel. (wikipedia.org)
  • Belongs to a family of drugs called calcium channel blockers. (fpnotebook.com)
  • The calcium channel blockers are a group of drugs which impede calcium ion entry into cells, thereby inhibiting myocardial and smooth muscle contraction, as well as various secretory processes. (ingentaconnect.com)
  • One drug, an angiotensin-converting enzyme (ACE) inhibitor, has proven effective in preventing progression to stages IV and V Calcium channel blockers , another class of antihypertensive drugs, also show promise. (thefreedictionary.com)
  • Contingent on regulatory approval, ziconotide will be the first in a new class of neurological drugs: the N-type calcium channel blockers, or NCCBs. (ingentaconnect.com)
  • The findings offer a first glimpse at the intricate relationship between the insulin secretion machinery and calcium channels, and suggests that drugs aimed at their interaction could be developed to treat diabetes. (uu.se)
  • Calcium channel blockers are prescribed for high blood pressure and heart problems, but be careful when using one with diuretics, ACE inhibitors, or other drugs. (everydayhealth.com)
  • Calcium channel blockers are a class of drugs prescribed for high blood pressure and other heart diseases. (everydayhealth.com)
  • Grapefruit (and its juice) can alter the effects of many drugs, including calcium channel blockers. (everydayhealth.com)
  • Older adults who take blood pressure drugs called calcium channel blockers could experience severe drops in blood pressure if also given antibiotics such as erythromycin (brands like E-Mycin) or clarithromycin (Biaxin), according to a new study. (mcknights.com)
  • Calcium channel blockers are the most commonly prescribed drugs for people with primary Raynaud's phenomenon. (cochrane.org)
  • The investigators assessed four types of antihypertensive drugs: beta blockers, diuretics, angiotensin converting enzyme inhibitors and calcium channel blockers. (healio.com)
  • Those who used calcium channel blockers for more than 3 years demonstrated a 107% higher risk than those who had ever used other antihypertensive drugs. (healio.com)
  • The adverse effects of electromagnetic fields may be mediated by activation of voltage-gated calcium channels. (greenmedinfo.com)
  • WINSTON-SALEM, NC -- Calcium channel blockers and certain kinds of diuretics are associated with brain damage and memory loss, according to a report in today's Journal of the American Geriatrics Society -- another in a string of adverse findings about calcium channel blockers. (eurekalert.org)
  • Treatment with calcium channel blockers was associated with a number of adverse events including headaches, flushing and ankle swelling. (cochrane.org)
  • [4] Calcium channel blockers are also frequently used to alter heart rate (especially from atrial fibrillation), to prevent peripheral and cerebral vasospasm , and to reduce chest pain caused by angina pectoris . (wikipedia.org)
  • Voltage-gated calcium channels (VGCCs), also known as voltage-dependent calcium channels (VDCCs), are a group of voltage-gated ion channels found in the membrane of excitable cells (e.g., muscle, glial cells, neurons, etc.) with a permeability to the calcium ion Ca2+. (wikipedia.org)
  • Research suggests that the way the brain uses calcium to regulate nerve cells may not work right in some people with bipolar disorder. (webmd.com)
  • It flows between the heart cells and surrounding fluid through a sort of chemical revolving door - the calcium channel. (healthcentral.com)
  • it acts by selectively blocking the uptake of calcium by the cells. (webmd.com)
  • This mineral enters muscle cells through ion channels, which are tiny pores on the surface of the cell. (medicalnewstoday.com)
  • Free calcium (Ca 2+ ) in the cytoplasm of plant cells is important for the regulation of many cellular processes and the transduction of stimuli. (sciencemag.org)
  • The patch-clamp technique was used to study Ca 2+ channels in the vacuole of sugar beet cells. (sciencemag.org)
  • L-type channels have been thought to have a role in AD for some time and this study shows a direct link between memory loss and L-type channel overproduction in brain cells. (bris.ac.uk)
  • Electrophysiology experiments with vacuolar membrane patches showed that membranes from wild-type Arabidopsis or cells engineered to overexpress TPC1 , but not those from a mutant plant that does not express TPC1 , had a cationic current with a steep calcium dependence. (sciencemag.org)
  • In guard cells, TPC1 was not directly responsible for ABA regulation of stomatal aperture, but TPC1-deficient cells did not exhibit a decrease in stomatal aperture in response to elevated calcium concentration. (sciencemag.org)
  • Because vasospastic smooth muscle cells are known to be depolarized compared to controls [ 3 , 4 ], the expression and function of ion channels in these cells after SAH are of great interest. (hindawi.com)
  • The finding is important, the researchers said, because understanding how these channels collaborate could lead to improved therapies that target aberrant calcium channels in malfunctioning cells. (biologynews.net)
  • They found that when cells begin responding to calcium, channels start grouping in clusters of two or more and open cooperatively, allowing cells to fire more rapidly. (biologynews.net)
  • This suggests that Ca(2+)- dependent inactivation occurs in intact cells and can be triggered by calcium entry through nearby voltage-gated calcium channels, although calcium entry through NMDA channels was more effective. (jneurosci.org)
  • Voltage-dependent Ca2+ channels (VDCC) are a family of molecules that allow cells to couple electrical activity to intracellular Ca2+ signalling. (ebi.ac.uk)
  • They are poorly understood, but like Q-type calcium channels , they appear to be present in cerebellar granule cells. (bionity.com)
  • This *very cool* paper in The Journal of Physiology ( also featured in the F1000 ) by authors Tünde Molnar, Peter Barabas, Lutz Birnbaumer, Claudio Punzo, Vladimir Kefalov and David Krizaj examines mechanisms of cytosolic calcium levels in rod photoreceptor cells. (utah.edu)
  • For example, calcium changes in photoreceptor cells regulate both our sensitivity to light and transmission of light-evoked signals from photoreceptors towards the brain, yet rod photoreceptors also die when calcium levels get too high or too low. (utah.edu)
  • Researchers from Uppsala University have studied beta cells of type-2 diabetic donors, and find that a mislocalized calcium channel contributes to the failed insulin secretion associated with the disease. (uu.se)
  • We hypothesized that the store-operated calcium entry (SOCE) channel, Orai1, participates in the activation of Th17 cells and influences renal injury. (jci.org)
  • Calcium-channel blockers are medicines that work on the muscle cells of your heart and your arteries. (bupa.co.uk)
  • To do this, calcium flows into these cells through special holes, or channels. (bupa.co.uk)
  • Mutations in presenilin associated with familial Alzheimer disease perturb calcium signaling in cells. (alzforum.org)
  • In contrast, the current through the same channel was suppressed in HEK293 cells stably transfected with either FAD-PS mutant L286V or ΔE9, consistent with the proteins' known effects on CCE. (alzforum.org)
  • The TRPM7-associated MIC channel is known to be activated by PIP2, and the researchers showed that even in cells expressing mutant PS1, applying PIP2 directly to the cytoplasm of cells in the patch clamp solution could activate the channels to wild-type levels. (alzforum.org)
  • These findings suggested that a PIP2 deficit might be the cause of diminished MIC channel activity in PS mutant-expressing cells. (alzforum.org)
  • METHODS: The effect of dipyridamole and the calcium channel blockers on mitoxantrone efflux by BCRP-overexpressing human embryonic kidney (HEK) cells was determined by flow cytometry. (biomedsearch.com)
  • Who should take calcium channel blockers? (healthline.com)
  • You should not, however, take calcium channel blockers with grapefruit juice or grapefruit. (everydayhealth.com)
  • Remember to take calcium channel blockers exactly as your doctor or pharmacist recommends. (everydayhealth.com)
  • Voltage-gated calcium (Ca2+) channels are key transducers of membrane potential changes into intracellular Ca2+ transients that initiate many physiological events. (stopumts.nl)
  • Together the papers highlight novel roles and versatility of these membrane channels. (alzforum.org)
  • The authors reasoned that membrane depolarization triggers calcium influx, and there are several calcium channels that might be responsible for the effect. (alzforum.org)
  • We examined the lateral membrane mobility of presynaptic L-type Ca 2+ channels at photoreceptor ribbon synapses of the tiger salamander ( Ambystoma tigrinum ) retina. (jneurosci.org)
  • Our results show that Ca V channels at rod and cone synapses are not fixed, but move within a membrane domain equal to or slightly larger than the area beneath the synaptic ridge at the base of the ribbon. (jneurosci.org)
  • Pharmacological disruption of the cytoskeleton or membrane cholesterol significantly increased the dimensions of the confinement domain of Ca V channels, suggesting that macromolecular scaffolds are important for organizing the synapse. (jneurosci.org)
  • Nicotinic acid adenine dinucleotide phosphate (NAADP) receptor that may function as one of the major voltage-gated Ca(2+) channels (VDCC) across the lysosomal membrane. (abcam.com)
  • SK channels are unique in that they are gated solely by intracellular Ca 2+ and hence, function to integrate intracellular Ca 2+ and membrane potentials on a beat-to-beat basis in the heart. (ahajournals.org)
  • Mature channels assembled at the plasma membrane are finely regulated for their permeation properties until they are removed from the cell surface by endocytosis. (fz-juelich.de)
  • A second quality control may decide their sorting fate after internalization: either the channel is recycled back to the plasma membrane or derived to the degradation pathway. (fz-juelich.de)
  • Concerted activation of different voltage-gated Ca( (2+) ) channel isoforms may determine the kinetics of insulin release from pancreatic islets. (nih.gov)
  • So calcium channel blockers have been studied as a treatment for bipolar disorder, but there isn't enough evidence yet that they work. (webmd.com)
  • Which calcium channel blockers have been studied to treat bipolar disorder? (webmd.com)
  • Activation of particular VGCCs allows Ca2+ to rush into the cell, which, depending on the cell type, results in activation of calcium-sensitive potassium channels, muscular contraction, excitation of neurons, up-regulation of gene expression, or release of hormones or neurotransmitters. (wikipedia.org)
  • To study these tiny channels, the researchers used high-resolution microscopy, electrophysiological measurements and optogenetic technologies -- light-sensitive probes that can stimulate neurons to fire electrical signals -- to study rat hippocampal neurons. (biologynews.net)
  • Calcium-dependent inactivation of NMDA channels was examined on cultured rat hippocampal neurons using whole-cell voltage-clamp and cell-attached single-channel recording. (jneurosci.org)
  • However, the American Heart Association recommend calcium channel blockers as a first-line pharmacological treatment for high blood pressure in most people and advise that beta-blockers should be a second-choice option. (medicalnewstoday.com)
  • This article presents the molecular relationships and physiological functions of these Ca2+ channel proteins and provides information on their molecular, genetic, physiological, and pharmacological properties. (stopumts.nl)
  • These channels could participate in the regulation of cytoplasmic Ca 2+ by sequestering Ca 2+ inside the vacuole. (sciencemag.org)
  • Structure and regulation of voltage-gated Ca2+ channels. (ebi.ac.uk)
  • The role of calcium and calcium-permeable channels in cancer is well-established, whereas the information about molecular nature of channels regulating autophagy and the mechanisms of this regulation is still limited. (frontiersin.org)
  • Here we review existing mechanisms of autophagy regulation by calcium and calcium-permeable ion channels. (frontiersin.org)
  • Furthermore, we will also discuss some calcium-permeable channels as the potential new candidates for autophagy regulation. (frontiersin.org)
  • The role of NO in the regulation of the mechanical properties of conduit arteries is controversial in humans, and the involvement of an endothelium-derived hyperpolarizing factor (EDHF), acting through calcium-activated potassium (K Ca ) channels, has never been investigated at this level in vivo. (ahajournals.org)
  • They demonstrate the involvement of K Ca channels in the regulation of the mechanical properties of peripheral conduit arteries, supporting a role for EDHF at this level in vivo. (ahajournals.org)
  • 12,13 In humans, the recent demonstration of the contribution of K Ca channels in the regulation of forearm arteriolar resistance strongly suggests a role for EDHF in vivo. (ahajournals.org)
  • Functional analysis of cloned channels allowed to identify structural elements in the pore forming regions determining Ca2+ permeability for many types of ligand-gated channels. (nih.gov)
  • TPC stands for two-pore channel, and TPC1 has two fused Shaker-like segments, each with six transmembrane domains and two EF hands, which are domains associated with calcium binding. (sciencemag.org)
  • Two pore calcium channel subfamily. (abcam.com)
  • Deregulation of the TRPM7, which forms the pore of the MIC channel, has been implicated in neurodegeneration due to ischemia and in the mysterious Guamanian neurodegenerative disorder, so it is a good candidate to play a role in Alzheimer disease. (alzforum.org)
  • The researchers, led by first author Natalie Landman, found that the transient potential melastatin 7 (TRPM7)-associated Mg2+-inhibited cation channel (MIC) is activated in PS1/2 knockout mouse embryonic fibroblasts. (alzforum.org)
  • Long-acting calcium channel blockers are significantly less effective than other antihypertensive agents in reducing the disease's major cardiovascular complications, according to a new metaanalysis. (thefreedictionary.com)
  • The following tables explain gating, gene, location and function of different types of calcium channels, both voltage and ligand-gated. (wikipedia.org)
  • Compendium of voltage-gated ion channels: calcium channels. (ebi.ac.uk)
  • The functional role of the Ca2+ entry mediated by various ligand-gated channels in mammalian central nervous system is less understood. (nih.gov)
  • In this study, Tünde Molnar and her coworkers in David Krizaj's group at the Moran Eye Institute identified two new calcium pathways in mammalian rods that are likely to contribute a protective role against pathologically low calcium levels experienced during sustained illuminations. (utah.edu)
  • Homologues of TRPC channels play a key role in fly vision but have never been studied in mammalian photoreceptors, suggesting potentially intriguing new parallels between calcium and photoreceptor signaling pathways of the two phyla. (utah.edu)
  • While it is true that mammalian milk products are the best source of dietary calcium, there still are other places to get calcium in your diet. (thedietchannel.com)
  • In 2019, the country was number 3 comparing other countries in Calcium Channel Blocking Medicine Use with 89.5 Units (Defined Daily Dosage) Per Thousand Persons Per Day. (nationmaster.com)
  • With 54.6 Units (Defined Daily Dosage) Per Thousand Persons Per Day in 2019, the country was ranked number 12 comparing other countries in Calcium Channel Blocking Medicine Use. (nationmaster.com)
  • Ligand-gated channels activated by excitatory neurotransmitters: glutamate, acetylcholine, ATP or serotonin are cation channels permeable to Ca2+. (nih.gov)
  • Finally we will propose the possible link between calcium permeable channels, autophagy and cancer progression and therapeutic response. (frontiersin.org)