Calcium Channels
Voltage-dependent cell membrane glycoproteins selectively permeable to calcium ions. They are categorized as L-, T-, N-, P-, Q-, and R-types based on the activation and inactivation kinetics, ion specificity, and sensitivity to drugs and toxins. The L- and T-types are present throughout the cardiovascular and central nervous systems and the N-, P-, Q-, & R-types are located in neuronal tissue.
Calcium Channel Blockers
Inositol 1,4,5-Trisphosphate Receptors
Calcium Channels, L-Type
Long-lasting voltage-gated CALCIUM CHANNELS found in both excitable and nonexcitable tissue. They are responsible for normal myocardial and vascular smooth muscle contractility. Five subunits (alpha-1, alpha-2, beta, gamma, and delta) make up the L-type channel. The alpha-1 subunit is the binding site for calcium-based antagonists. Dihydropyridine-based calcium antagonists are used as markers for these binding sites.
Ion Channels
Calcium Channels, N-Type
Calcium Channels, T-Type
Calcium Signaling
Signal transduction mechanisms whereby calcium mobilization (from outside the cell or from intracellular storage pools) to the cytoplasm is triggered by external stimuli. Calcium signals are often seen to propagate as waves, oscillations, spikes, sparks, or puffs. The calcium acts as an intracellular messenger by activating calcium-responsive proteins.
Calcium Channel Agonists
Agents that increase calcium influx into calcium channels of excitable tissues. This causes vasoconstriction in VASCULAR SMOOTH MUSCLE and/or CARDIAC MUSCLE cells as well as stimulation of insulin release from pancreatic islets. Therefore, tissue-selective calcium agonists have the potential to combat cardiac failure and endocrinological disorders. They have been used primarily in experimental studies in cell and tissue culture.
Ion Channel Gating
The opening and closing of ion channels due to a stimulus. The stimulus can be a change in membrane potential (voltage-gated), drugs or chemical transmitters (ligand-gated), or a mechanical deformation. Gating is thought to involve conformational changes of the ion channel which alters selective permeability.
Receptors, Cytoplasmic and Nuclear
Intracellular receptors that can be found in the cytoplasm or in the nucleus. They bind to extracellular signaling molecules that migrate through or are transported across the CELL MEMBRANE. Many members of this class of receptors occur in the cytoplasm and are transported to the CELL NUCLEUS upon ligand-binding where they signal via DNA-binding and transcription regulation. Also included in this category are receptors found on INTRACELLULAR MEMBRANES that act via mechanisms similar to CELL SURFACE RECEPTORS.
Calcium
A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.
Potassium Channels, Inwardly Rectifying
Calcium Channels, P-Type
Dihydropyridines
Inositol 1,4,5-Trisphosphate
Intracellular messenger formed by the action of phospholipase C on phosphatidylinositol 4,5-bisphosphate, which is one of the phospholipids that make up the cell membrane. Inositol 1,4,5-trisphosphate is released into the cytoplasm where it releases calcium ions from internal stores within the cell's endoplasmic reticulum. These calcium ions stimulate the activity of B kinase or calmodulin.
Receptors, Interleukin-1
Cell surface receptors that are specific for INTERLEUKIN-1. Included under this heading are signaling receptors, non-signaling receptors and accessory proteins required for receptor signaling. Signaling from interleukin-1 receptors occurs via interaction with SIGNAL TRANSDUCING ADAPTOR PROTEINS such as MYELOID DIFFERENTIATION FACTOR 88.
Calcium Channels, R-Type
Nifedipine
Potassium Channel Blockers
Chloride Channels
omega-Conotoxin GVIA
Electrophysiology
Calcium, Dietary
Membrane Potentials
The voltage differences across a membrane. For cellular membranes they are computed by subtracting the voltage measured outside the membrane from the voltage measured inside the membrane. They result from differences of inside versus outside concentration of potassium, sodium, chloride, and other ions across cells' or ORGANELLES membranes. For excitable cells, the resting membrane potentials range between -30 and -100 millivolts. Physical, chemical, or electrical stimuli can make a membrane potential more negative (hyperpolarization), or less negative (depolarization).
omega-Conotoxins
Potassium Channels, Voltage-Gated
Diltiazem
KATP Channels
Heteromultimers of Kir6 channels (the pore portion) and sulfonylurea receptor (the regulatory portion) which affect function of the HEART; PANCREATIC BETA CELLS; and KIDNEY COLLECTING DUCTS. KATP channel blockers include GLIBENCLAMIDE and mitiglinide whereas openers include CROMAKALIM and minoxidil sulfate.
Isradipine
Patch-Clamp Techniques
An electrophysiologic technique for studying cells, cell membranes, and occasionally isolated organelles. All patch-clamp methods rely on a very high-resistance seal between a micropipette and a membrane; the seal is usually attained by gentle suction. The four most common variants include on-cell patch, inside-out patch, outside-out patch, and whole-cell clamp. Patch-clamp methods are commonly used to voltage clamp, that is control the voltage across the membrane and measure current flow, but current-clamp methods, in which the current is controlled and the voltage is measured, are also used.
Potassium Channels, Calcium-Activated
Nitrendipine
Mibefradil
Sodium Channel Blockers
Barium
Nimodipine
omega-Agatoxin IVA
TRPC Cation Channels
Shaker Superfamily of Potassium Channels
Neurons
Cells, Cultured
Large-Conductance Calcium-Activated Potassium Channels
Potassium
An element in the alkali group of metals with an atomic symbol K, atomic number 19, and atomic weight 39.10. It is the chief cation in the intracellular fluid of muscle and other cells. Potassium ion is a strong electrolyte that plays a significant role in the regulation of fluid volume and maintenance of the WATER-ELECTROLYTE BALANCE.
Calcium Carbonate
Cyclic Nucleotide-Gated Cation Channels
Oocytes
Molecular Sequence Data
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
Calcium Chloride
Rats, Sprague-Dawley
TRPV Cation Channels
Dose-Response Relationship, Drug
Nicardipine
A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents.
Xenopus laevis
Amino Acid Sequence
Ryanodine Receptor Calcium Release Channel
A tetrameric calcium release channel in the SARCOPLASMIC RETICULUM membrane of SMOOTH MUSCLE CELLS, acting oppositely to SARCOPLASMIC RETICULUM CALCIUM-TRANSPORTING ATPASES. It is important in skeletal and cardiac excitation-contraction coupling and studied by using RYANODINE. Abnormalities are implicated in CARDIAC ARRHYTHMIAS and MUSCULAR DISEASES.
TRPM Cation Channels
Acid Sensing Ion Channels
Spider Venoms
Calcium Phosphates
Epithelial Sodium Channels
Kv1.3 Potassium Channel
Ether-A-Go-Go Potassium Channels
A family of voltage-gated potassium channels that are characterized by long N-terminal and C-terminal intracellular tails. They are named from the Drosophila protein whose mutation causes abnormal leg shaking under ether anesthesia. Their activation kinetics are dependent on extracellular MAGNESIUM and PROTON concentration.
Calcium Isotopes
Kv1.2 Potassium Channel
Kv1.1 Potassium Channel
Calcium Radioisotopes
Protein Subunits
Amlodipine
Kv1.5 Potassium Channel
Agatoxins
Xenopus
Myocardium
Small-Conductance Calcium-Activated Potassium Channels
Sodium
Action Potentials
Rabbits
Ion Transport
Adenosine Triphosphate
Mollusk Venoms
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.
Transient Receptor Potential Channels
A broad group of eukaryotic six-transmembrane cation channels that are classified by sequence homology because their functional involvement with SENSATION is varied. They have only weak voltage sensitivity and ion selectivity. They are named after a DROSOPHILA mutant that displayed transient receptor potentials in response to light. A 25-amino-acid motif containing a TRP box (EWKFAR) just C-terminal to S6 is found in TRPC, TRPV and TRPM subgroups. ANKYRIN repeats are found in TRPC, TRPV & TRPN subgroups. Some are functionally associated with TYROSINE KINASE or TYPE C PHOSPHOLIPASES.
KCNQ Potassium Channels
Shab Potassium Channels
Rats, Wistar
Cell Membrane
Shaw Potassium Channels
Kv1.4 Potassium Channel
Tetrodotoxin
Protein Structure, Tertiary
The level of protein structure in which combinations of secondary protein structures (alpha helices, beta sheets, loop regions, and motifs) pack together to form folded shapes called domains. Disulfide bridges between cysteines in two different parts of the polypeptide chain along with other interactions between the chains play a role in the formation and stabilization of tertiary structure. Small proteins usually consist of only one domain but larger proteins may contain a number of domains connected by segments of polypeptide chain which lack regular secondary structure.
Models, Biological
Calcium Oxalate
Mutation
Chelating Agents
Gallopamil
G Protein-Coupled Inwardly-Rectifying Potassium Channels
Calcium Gluconate
Shal Potassium Channels
Presynaptic Terminals
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.
Magnesium
Fura-2
Peptides
Members of the class of compounds composed of AMINO ACIDS joined together by peptide bonds between adjacent amino acids into linear, branched or cyclical structures. OLIGOPEPTIDES are composed of approximately 2-12 amino acids. Polypeptides are composed of approximately 13 or more amino acids. PROTEINS are linear polypeptides that are normally synthesized on RIBOSOMES.
Thapsigargin
KCNQ2 Potassium Channel
Binding Sites
Hyperpolarization-Activated Cyclic Nucleotide-Gated Channels
Transfection
Guinea Pigs
Nickel
Neurotransmitter Agents
Signal Transduction
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
Lanthanum
Cadmium
Scorpion Venoms
Nisoldipine
NAV1.5 Voltage-Gated Sodium Channel
Hippocampus
A curved elevation of GRAY MATTER extending the entire length of the floor of the TEMPORAL HORN of the LATERAL VENTRICLE (see also TEMPORAL LOBE). The hippocampus proper, subiculum, and DENTATE GYRUS constitute the hippocampal formation. Sometimes authors include the ENTORHINAL CORTEX in the hippocampal formation.
Models, Molecular
Intermediate-Conductance Calcium-Activated Potassium Channels
Membrane Proteins
Synaptic Transmission
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.
KCNQ3 Potassium Channel
Large-Conductance Calcium-Activated Potassium Channel alpha Subunits
Ions
Ganglia, Spinal
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.
Hydrogen-Ion Concentration
Cations
Protein Binding
Muscle Contraction
Ryanodine
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.
Delayed Rectifier Potassium Channels
Calmodulin
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, Messenger
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.
NAV1.2 Voltage-Gated Sodium Channel
A voltage-gated sodium channel subtype that mediates the sodium ion permeability of excitable membranes. Defects in the SCN2A gene which codes for the alpha subunit of this sodium channel are associated with benign familial infantile seizures type 3, and early infantile epileptic encephalopathy type 11.
Voltage-Gated Sodium Channels
Myocytes, Cardiac
Cell Membrane Permeability
Charybdotoxin
Lipid Bilayers
Cytosol
Strontium
Flunarizine
Calcimycin
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.
HEK293 Cells
Enzyme Inhibitors
GTP-Binding Proteins
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.-.
Protein Conformation
The characteristic 3-dimensional shape of a protein, including the secondary, supersecondary (motifs), tertiary (domains) and quaternary structure of the peptide chain. PROTEIN STRUCTURE, QUATERNARY describes the conformation assumed by multimeric proteins (aggregates of more than one polypeptide chain).
Fluorescent Dyes
Protein Isoforms
Glutamic Acid
4-Aminopyridine
Kidney
Cyclic AMP
Synapses
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.
Cations, Divalent
Apamin
Protein Kinase C
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.
Structure-Activity Relationship
Cyclic AMP-Dependent Protein Kinases
Calcium-Binding Proteins
Potassium Chloride
Caffeine
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.
Receptors, Drug
Sequence Homology, Amino Acid
Felodipine
Antihypertensive Agents
Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS.
Mutagenesis, Site-Directed
Sulfonylurea Receptors
Muscle, Smooth
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)
Cerebellum
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.
Cricetinae
Sarcolemma
Brain
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.
NAV1.4 Voltage-Gated Sodium Channel
Voltage-Dependent Anion Channels
Homeostasis
Extracellular Space
Dogs
Azetidinecarboxylic Acid
Multiple structural domains contribute to voltage-dependent inactivation of rat brain alpha(1E) calcium channels. (1/107)
We have investigated the molecular determinants that mediate the differences in voltage-dependent inactivation properties between rapidly inactivating (R-type) alpha(1E) and noninactivating (L-type) alpha(1C) calcium channels. When coexpressed in human embryonic kidney cells with ancillary beta(1b) and alpha(2)-delta subunits, the wild type channels exhibit dramatically different inactivation properties; the half-inactivation potential of alpha(1E) is 45 mV more negative than that observed with alpha(1C), and during a 150-ms test depolarization, alpha(1E) undergoes 65% inactivation compared with only about 15% for alpha(1C). To define the structural determinants that govern these intrinsic differences, we have created a series of chimeric calcium channel alpha(1) subunits that combine the major structural domains of the two wild type channels, and we investigated their voltage-dependent inactivation properties. Each of the four transmembrane domains significantly affected the half-inactivation potential, with domains II and III being most critical. In particular, substitution of alpha(1C) sequence in domains II or III with that of alpha(1E) resulted in 25-mV negative shifts in half-inactivation potential. Similarly, the differences in inactivation rate were predominantly governed by transmembrane domains II and III and to some extent by domain IV. Thus, voltage-dependent inactivation of alpha(1E) channels is a complex process that involves multiple structural domains and possibly a global conformational change in the channel protein. (+info)An R-type Ca(2+) current in neurohypophysial terminals preferentially regulates oxytocin secretion. (2/107)
Multiple types of voltage-dependent Ca(2+) channels are involved in the regulation of neurotransmitter release (Tsien et al., 1991; Dunlap et al., 1995). In the nerve terminals of the neurohypophysis, the roles of L-, N-, and P/Q-type Ca(2+) channels in neuropeptide release have been identified previously (Wang et al., 1997a). Although the L- and N-type Ca(2+) currents play equivalent roles in both vasopressin and oxytocin release, the P/Q-type Ca(2+) current only regulates vasopressin release. An oxytocin-release and Ca(2+) current component is resistant to the L-, N-, and P/Q-type Ca(2+) channel blockers but is inhibited by Ni(2+). A new polypeptide toxin, SNX-482, which is a specific alpha(1E)-type Ca(2+) channel blocker (Newcomb et al., 1998), was used to characterize the biophysical properties of this resistant Ca(2+) current component and its role in neuropeptide release. This resistant component was dose dependently inhibited by SNX-482, with an IC(50) of 4.1 nM. Furthermore, SNX-482 did not affect the other Ca(2+) current types in these CNS terminals. Like the N- and P/Q-type Ca(2+) currents, this SNX-482-sensitive transient Ca(2+) current is high-threshold activated and shows moderate steady-state inactivation. At the same concentrations, SNX-482 blocked the component of oxytocin, but not of vasopressin, release that was resistant to the other channel blockers, indicating a preferential role for this type of Ca(2+) current in oxytocin release from neurohypophysial terminals. Our results suggest that an alpha(1E) or "R"-type Ca(2+) channel exists in oxytocinergic nerve terminals and, thus, functions in controlling only oxytocin release from the rat neurohypophysis. (+info)Developmental changes in calcium channel types mediating central synaptic transmission. (3/107)
Multiple types of high-voltage-activated Ca(2+) channels trigger neurotransmitter release at the mammalian central synapse. Among them, the omega-conotoxin GVIA-sensitive N-type channels and the omega-Aga-IVA-sensitive P/Q-type channels mediate fast synaptic transmission. However, at most central synapses, it is not known whether the contributions of different Ca(2+) channel types to synaptic transmission remain stable throughout postnatal development. We have addressed this question by testing type-specific Ca(2+) channel blockers at developing central synapses. Our results indicate that N-type channels contribute to thalamic and cerebellar IPSCs only transiently during early postnatal period and P/Q-type channels predominantly mediate mature synaptic transmission, as we reported previously at the brainstem auditory synapse formed by the calyx of Held. In fact, Ca(2+) currents directly recorded from the auditory calyceal presynaptic terminal were identified as N-, P/Q-, and R-types at postnatal day 7 (P7) to P10 but became predominantly P/Q-type at P13. In contrast to thalamic and cerebellar IPSCs and brainstem auditory EPSCs, N-type Ca(2+) channels persistently contribute to cerebral cortical EPSCs and spinal IPSCs throughout postnatal months. Thus, in adult animals, synaptic transmission is predominantly mediated by P/Q-type channels at a subset of synapses and mediated synergistically by multiple types of Ca(2+) channels at other synapses. (+info)alpha(1E) subunits form the pore of three cerebellar R-type calcium channels with different pharmacological and permeation properties. (4/107)
R-type Ca(2+) channels cooperate with P/Q- and N-type channels to control neurotransmitter release at central synapses. The leading candidate as pore-forming subunit of R-type channels is the alpha(1E) subunit. However, R-type Ca(2+) currents with permeation and/or pharmacological properties different from those of recombinant Ca(2+) channels containing alpha(1E) subunits have been described, and therefore the molecular nature of R-type Ca(2+) channels remains not completely settled. Here, we show that the R-type Ca(2+) current of rat cerebellar granule cells consists of two components inhibited with different affinity by the alpha(1E) selective antagonist SNX482 (IC(50) values of 6 and 81 nM) and a third component resistant to SNX482. The SNX482-sensitive R-type current shows the unique permeation properties of recombinant alpha(1E) channels; it is larger with Ca(2+) than with Ba(2+) as charge carrier, and it is highly sensitive to Ni(2+) block and has a voltage-dependence of activation consistent with that of G2 channels with unitary conductance of 15 pS. On the other hand, the SNX482-resistant R-type current shows permeation properties similar to those of recombinant alpha(1A) and alpha(1B) channels; it is larger with Ba(2+) than with Ca(2+) as charge carrier(,) and it has a low sensitivity to Ni(2+) block and a voltage-dependence of activation consistent with that of G3 channels with unitary conductance of 20 pS. Gene-specific knock-down by antisense oligonucleotides demonstrates that the different cerebellar R-type channels are all encoded by the alpha(1E) gene, suggesting the existence of alpha(1E) isoforms with different pore properties. (+info)Calcium currents in hair cells isolated from semicircular canals of the frog. (5/107)
L-type and R-type Ca(2+) currents were detected in frog semicircular canal hair cells. The former was noninactivating and nifedipine-sensitive (5 microM); the latter, partially inactivated, was resistant to omega-conotoxin GVIA (5 microM), omega-conotoxin MVIIC (5 microM), and omega-agatoxin IVA (0.4 microM), but was sensitive to mibefradil (10 microM). Both currents were sensitive to Ni(2+) and Cd(2+) (>10 microM). In some cells the L-type current amplitude increased almost twofold upon repetitive stimulation, whereas the R-type current remained unaffected. Eventually, run-down occurred for both currents, but was prevented by the protease inhibitor calpastatin. The R-type current peak component ran down first, without changing its plateau, suggesting that two channel types generate the R-type current. This peak component appeared at -40 mV, reached a maximal value at -30 mV, and became undetectable for voltages > or =0 mV, suggestive of a novel transient current: its inactivation was indeed reversibly removed when Ba(2+) was the charge carrier. The L-type current and the R-type current plateau were appreciable at -60 mV and peaked at -20 mV: the former current did not reverse for voltages up to +60 mV, the latter reversed between +30 and +60 mV due to an outward Cs(+) current flowing through the same Ca(2+) channel. The physiological role of these currents on hair cell function is discussed. (+info)The spider toxin omega-Aga IIIA defines a high affinity site on neuronal high voltage-activated calcium channels. (6/107)
The spider toxin omega-agatoxin IIIA (omega-Aga-IIIA) is a potent inhibitor of high voltage-activated calcium currents in the mammalian brain. To establish the biochemical parameters governing its action, we radiolabeled the toxin and examined its binding to native and recombinant calcium channels. In experiments with purified rat synaptosomal membranes, both kinetic and equilibrium data demonstrate one-to-one binding of omega-Aga-IIIA to a single population of high affinity sites, with K(d) = approximately 9 pm and B(max) = approximately 1.4 pmol/mg protein. Partial inhibition of omega-Aga-IIIA binding by omega-conotoxins GVIA, MVIIA, and MVIIC identifies N and P/Q channels as components of this population. omega-Aga-IIIA binds to recombinant alpha(1B) and alpha(1E) calcium channels with a similar high affinity (K(d) = approximately 5-9 pm) in apparent one-to-one fashion. Results from recombinant alpha(1B) binding experiments demonstrate virtually identical B(max) values for omega-Aga-IIIA and omega-conotoxin MVIIA, providing further evidence for a one-to-one stoichiometry of agatoxin binding to calcium channels. The combined evidence suggests that omega-Aga-IIIA defines a unique, high affinity binding site on N-, P/Q-, and R-type calcium channels. (+info)CaV2.2 and CaV2.3 (N- and R-type) Ca2+ channels in depolarization-evoked entry of Ca2+ into mouse sperm. (7/107)
As sperm prepare for fertilization, surface Ca(2+) channels must open to initiate required, Ca(2+)-mediated events. However, the molecular identity and functional properties of sperm Ca(2+) channels remain uncertain. Here, we use rapid local perfusion and single-cell photometry to examine the kinetics of calcium responses of mouse sperm to depolarizing stimuli. The linear rise of intracellular [Ca(2+)] evoked by approximately 10-s applications of an alkaline high [K(+)] medium directly reports activity of voltage-gated Ca(2+) channels. Little response occurs if external Ca(2+) is removed or if external or internal pH is elevated without depolarization. Responses are inhibited 30-40% by 30-100 micrometer Ni(2+) and more completely by 100-300 micrometer Cd(2+). They resist the dihydropyridines nitrendipine and PN200-110, but 1-10 micrometer mibefradil inhibits reversibly. They also resist the venom toxins calciseptine, omega-conotoxin MVIIC, and kurtoxin, but omega-conotoxin GVIA (5 micrometer) inhibits approximately 50%. GVIA also partially blocks transient, low voltage activated Ca(2+) currents of patch-clamped spermatids. Differential sensitivity of sperm responses to Ni(2+) and Cd(2+) and partial blockade by GVIA indicate that depolarization opens at least two types of voltage-gated Ca(2+) channels in epididymal sperm examined prior to capacitation. Involvement of a previously undetected Ca(V)2.2 (N-type) channel, suggested by the action of GVIA, is substantiated by immunodetection of Ca(2+) channel alpha(1B) subunits in sperm and sperm extracts. Resistance to dihydropyridines, calciseptine, MVIIC, and kurtoxin indicates that Ca(V)1, Ca(V)2.1, and Ca(V)3 (L-, P/Q-, and T-type) channels contribute little to this evoked response. Partial sensitivity to 1 micrometer mibefradil and an enhanced sensitivity of the GVIA-resistant component of response to Ni(2+) suggest participation of a Ca(V)2.3 (R-type) channel specified by previously found alpha(1E) subunits. Our examination of depolarization-evoked Ca(2+) entry indicates that mature sperm possess a larger palette of voltage-gated Ca(2+) channels than previously thought. Such diversity may permit specific responses to multiple cues encountered on the path to fertilization. (+info)Altered pain responses in mice lacking alpha 1E subunit of the voltage-dependent Ca2+ channel. (8/107)
alpha(1) subunit of the voltage-dependent Ca(2+) channel is essential for channel function and determines the functional specificity of various channel types. alpha(1E) subunit was originally identified as a neuron-specific one, but the physiological function of the Ca(2+) channel containing this subunit (alpha(1E) Ca(2+) channel) was not clear compared with other types of Ca(2+) channels because of the limited availability of specific blockers. To clarify the physiological roles of the alpha(1E) Ca(2+) channel, we have generated alpha(1E) mutant (alpha(1E)-/-) mice by gene targeting. The lacZ gene was inserted in-frame and used as a marker for alpha(1E) subunit expression. alpha(1E)-/- mice showed reduced spontaneous locomotor activities and signs of timidness, but other general behaviors were apparently normal. As involvement of alpha(1E) in pain transmission was suggested by localization analyses with 5-bromo-4-chloro-3-indolyl beta-d-galactopyranoside staining, we conducted several pain-related behavioral tests using the mutant mice. Although alpha(1E)+/- and alpha(1E)-/- mice exhibited normal pain behaviors against acute mechanical, thermal, and chemical stimuli, they both showed reduced responses to somatic inflammatory pain. alpha(1E)+/- mice showed reduced response to visceral inflammatory pain, whereas alpha(1E)-/- mice showed apparently normal response compared with that of wild-type mice. Furthermore, alpha(1E)-/- mice that had been presensitized with a visceral noxious conditioning stimulus showed increased responses to a somatic inflammatory pain, in marked contrast with the wild-type mice in which long-lasting effects of descending antinociceptive pathway were predominant. These results suggest that the alpha(1E) Ca(2 +) channel controls pain behaviors by both spinal and supraspinal mechanisms. (+info)
R-type calcium channel - Wikipedia
CACNA1E - Voltage-dependent R-type calcium channel subunit alpha - Homo sapiens (Human) - CACNA1E gene & protein
R-type calcium channel
MicrocircuitDB: Spine head calcium in a CA1 pyramidal cell model (Graham et al. 2014)
Channelpedia
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R-type calcium channel
The R-type calcium channel is a type of voltage-dependent calcium channel. Like the others of this class, the α1 subunit forms ... "Entrez Gene: CACNA1E calcium channel, voltage-dependent, R type, alpha 1E subunit". Soong TW, Stea A, Hodson CD, Dubel SJ, ... This α1 subunit is also known as the calcium channel, voltage-dependent, R type, alpha 1E subunit (CACNA1E) or Cav2.3 which in ... They are poorly understood, but like Q-type calcium channels, they appear to be present in cerebellar granule cells. They have ...
T-type calcium channel
Long-Lasting calcium channels). The new T-type channels were much different from the L-type calcium channels due to their ... are both blockers of T-type calcium channels; the second-line treatment, lamotrigine, although not a T-type calcium channel ... Calcium channel blockers (CCB) such as mibefradil can also block L-type calcium channels, other enzymes, as well as other ... Novel T-type calcium channel inhibitors have recently been discovered which more selectively target the CaV3.3 channel sub-type ...
N-type calcium channel
N-type calcium channels also called Cav2.2 channels are voltage gated calcium channels that are localized primarily on the ... and this shows that only the N-type calcium channel, not the P/Q/L type calcium channels, are involved in the release of ... to block the N-type calcium channels, have produced alleviation of intractable pain. Blockade of the N-type calcium channel is ... blocking of N-type calcium channels reduce glomerular pressure through dilation of arterioles. N-type calcium channels have ...
L-type calcium channel
P-type, and N-type. L-type calcium channels were peptide sequenced and it was found that there were 4 kinds of L-type calcium ... The L-type calcium channel (also known as the dihydropyridine channel, or DHP channel) is part of the high-voltage activated ... Unlike other voltage gated calcium channels, L-type calcium channels are resistant to ⍵-CT X (GVIA) and ⍵-AG A (IVA) inhibitory ... This channel has four isoforms: Cav1.1, Cav1.2, Cav1.3, and Cav1.4. L-type calcium channels are responsible for the excitation- ...
Q-type calcium channel
The Q-type calcium channel is a type of voltage-dependent calcium channel. Like the others of this class, the α1 subunit is the ... Q-Type+Calcium+Channel at the US National Library of Medicine Medical Subject Headings (MeSH) (Articles with short description ... They are poorly understood, but like R-type calcium channels, they appear to be present in cerebellar granule cells. They have ... Short description matches Wikidata, Protein pages needing a picture, Genes on human chromosome 19, Ion channels, ...
P-type calcium channel
The P-type calcium channel is a type of voltage-dependent calcium channel. Similar to many other high-voltage-gated calcium ... P-type calcium channels play a similar role to the N-type calcium channel in neurotransmitter release at the presynaptic ... There are many different types of calcium channels, so to prove that the P/Q type calcium channels are directly involved, a P/Q ... corresponds to what is functionally defined as the P-type and Q-type isoforms. P-type and Q-type calcium channels are closely ...
Calcium channel, voltage-dependent, T type, alpha 1H subunit
... a protein in the voltage-dependent calcium channel complex. Calcium channels mediate the influx of calcium ions into the cell ... Calcium channel, voltage-dependent, T type, alpha 1H subunit, also known as CACNA1H, is a protein which in humans is encoded by ... "Entrez Gene: CACNA1H calcium channel, voltage-dependent, T type, alpha 1H subunit". Cribbs LL, Lee JH, Yang J, Satin J, Zhang Y ... 2003). "T-type calcium channel regulation by specific G-protein betagamma subunits". Nature. 424 (6945): 209-13. doi:10.1038/ ...
Calcium channel blocker
N-type, L-type, and T-type voltage-dependent calcium channels are present in the zona glomerulosa of the human adrenal gland, ... Calcium channel blockers (CCB), calcium channel antagonists or calcium antagonists are a group of medications that disrupt the ... may increase or enhance the effects of calcium channel blockade. N-type calcium channels are found in neurons and are involved ... The resulting increase in intracellular calcium has different effects in different types of cells. Calcium channel blockers ...
Calcium channel
the receptor-operated calcium channels (in vasoconstriction) P2X receptors L-type calcium channel blockers are used to treat ... T-type calcium channel blockers are used to treat epilepsy. Increased calcium conductance in the neurons leads to increased ... A calcium channel is an ion channel which shows selective permeability to calcium ions. It is sometimes synonymous with voltage ... Calcium in biology - Use of calcium by organisms. "calcium channel" at Dorland's Medical Dictionary Striggow F, Ehrlich BE ( ...
Voltage-gated calcium channel
High-voltage-gated calcium channels include the neural N-type channel blocked by ω-conotoxin GVIA, the R-type channel (R stands ... opening of the L-type calcium channel permits influx of calcium into the cell. The calcium binds to the calcium release ... See reference for an illustration of the signaling cascade involving L-type calcium channels in smooth muscle). L-type calcium ... Voltage-gated calcium channels (VGCCs), also known as voltage-dependent calcium channels (VDCCs), are a group of voltage-gated ...
Calcium-dependent chloride channel
... groups of ligand-gated ion channels for chloride that have been identified in many epithelial and endothelial cell types as ... The Calcium-Dependent Chloride Channel (Ca-ClC) proteins (or calcium-activated chloride channels (CaCCs), are heterogeneous ... "1.A.17 The Calcium-Dependent Chloride Channel (Ca-ClC) Family". TCDB. Retrieved 16 April 2016. "Calcium activated chloride ... and calcium-dependent chloride channel anoctamin (ANO or TMEM16) channels ANO1 is highly expressed in human gastrointestinal ...
Calcium-activated potassium channel
It was concluded that there was a different unknown type of potassium channel allowing these currents. It is clear that SK ... Calcium-activated potassium channels are potassium channels gated by calcium, or that are structurally or phylogenetically ... These channels can only be opened by increased levels of intracellular calcium. This trait of SK channels suggests that they ... BK channel SK channel Slow after-hyperpolarisation Vergara, C.; Latorre, R.; Marrion, N. V.; Adelman, J. P. (1998). "Calcium- ...
Calcium channel opener
A calcium channel opener is a type of drug which facilitates ion transmission through calcium channels. An example is Bay K8644 ... mucolipin TRP channels (TRPMLs) and purinergic receptors of the P2X channel type. Calcium channel blocker Schramm M, Thomas G, ... Calcium permeable ion channels in lysosomal membranes that may be activated by a luminal pH increase include two pore channels ... which is an analogue of nifedipine that specifically and directly activates L-type voltage-dependent calcium channels. In ...
Calcium-induced calcium release
When an action potential depolarizes the cell membrane, voltage-gated Ca2+ channels (e.g., L-type calcium channels) are ... Calcium-induced calcium release (CICR) describes a biological process whereby calcium is able to activate calcium release from ... Iosub R, Avitabile D, Grant L, Tsaneva-Atanasova K, Kennedy HJ (March 2015). "Calcium-Induced calcium release during action ... Fabiato A (July 1983). "Calcium-induced release of calcium from the cardiac sarcoplasmic reticulum". The American Journal of ...
Dihydropyridine calcium channel blockers
... are derivatives of 1,4-dihydropyridine that are used as L-type calcium channel ... Calcium channel blocker (including section on non-dihydropyridine calcium channel blockers) Calcium channel Dihydropyridine ... Dihydropyridine class L-type calcium channel blockers include, in alphabetical order (brand names vary in different countries ... Compared with certain other L-type calcium channel blockers (for example those of the phenylalkylamine class such as verapamil ...
Piracetam
... inhibits N-type calcium channels. The concentration of piracetam achieved in central nervous system after a typical ... is much higher than the concentration necessary to inhibit N-type calcium channels (IC50 of piracetam in rat neurons was 3 μM ... Piracetam may exert its global effect on brain neurotransmission via modulation of ion channels (i.e., Na+, K+). It has been ... It is hypothesized to act on ion channels or ion carriers, thus leading to increased neuron excitability. GABA brain metabolism ...
Cilnidipine
Unlike other calcium antagonists, cilnidipine can act on the N-type calcium channel in addition to acting on the L-type calcium ... It is a calcium antagonist accompanied with L-type and N-type calcium channel blocking functions. ... Due to its blocking action at the N-type and L-type calcium channel, cilnidipine dilates both arterioles and venules, reducing ... May 2002). "Cilnidipine is a novel slow-acting blocker of vascular L-type calcium channels that does not target protein kinase ...
Cav1.2
"Osteoprotegerin expression and secretion are regulated by calcium influx through the L-type voltage-sensitive calcium channel ... This gene encodes an alpha-1 subunit of a voltage-dependent calcium channel. Calcium channels mediate the influx of calcium ... Calcium channel, voltage-dependent, L type, alpha 1C subunit (also known as Cav1.2) is a protein that in humans is encoded by ... Calcium channel Calcium channel associated transcriptional regulator ENSG00000285479 GRCh38: Ensembl release 89: ...
Childhood absence epilepsy
"Molecular characterization of T-type calcium channels". Cell Calcium. 40 (2): 89-96. doi:10.1016/j.ceca.2006.04.012. PMID ... Seizures are believed to originate in the thalamus, where there is an abundance of T-type calcium channels such as those ... first-line treatment for seizures only by blocking the low-threshold calcium currents produced by T-type calcium channels in ... there is an association between mutations in the calcium channel, voltage-dependent, T type, alpha 1H subunit (CACNA1H), and ...
Acetylcholine
... inhibits P-type calcium channels Myasthenia gravis Botulinum toxin: inhibits SNARE proteins Calcium channel blockers ( ... and thereby affecting P-type calcium channels): Antibiotics (clindamycin, polymyxin) Magnesium: antagonizes P-type calcium ... Nicotinic receptors come in two main types, known as muscle-type and neuronal-type. The muscle-type can be selectively blocked ... nifedipine, diltiazem) do not affect P-channels. These drugs affect L-type calcium channels. The autonomic nervous system ...
Ptu1
... reversibly blocks N-type calcium channels. In addition, it has a low affinity for L or P/Q-type channels. The mechanism by ... Ptu1 is a toxin that can reversibly bind N-type calcium channels. Its isolated from the assassin bug Peirates turpis. The toxin ... Second, Ptu1 has a relatively low binding affinity for N-type calcium channels compared to MVIIA. A possible explanation for ... a toxin from the assassin bug Peirates turpis that blocks the voltage-sensitive calcium channel N-type". Biochemistry. 40 (43 ...
CACNA1B
... together with β and α2δ subunits forms N-type calcium channel (Cav2.2 channel) PMID 26386135. It is a R-type calcium channel. ... subunits for the calcium channel I-II linker in relation to calcium channel function". The Journal of Physiology. 574 (Pt 2): ... "Entrez Gene: CACNA1B calcium channel, voltage-dependent, N type, alpha 1B subunit". Diriong S, Lory P, Williams ME, Ellis SB, ... The voltage-dependent N-type calcium channel subunit alpha-1B is a protein that in humans is encoded by the CACNA1B gene. The ...
CACNA1G
Cav3.1 is a type of low-voltage-activated calcium channel, also known as "T-type" for its transient on and off. It is expressed ... Calcium channel, voltage-dependent, T type, alpha 1G subunit, also known as CACNA1G or Cav3.1 is a protein which in humans is ... "Entrez Gene: CACNA1H calcium channel, voltage-dependent, T type, alpha 1H subunit". Perez-Reyes E, Cribbs LL, Daud A, Lacerda ... Kopecky, Benjamin J.; Liang, Ruqiang; Bao, Jianxin (2014). "T-type Calcium Channel Blockers as Neuroprotective Agents". ...
Calcium channel blocker toxicity
The three most common types of heart medications that result in this outcome are calcium channel blockers along with beta ... Calcium channel blocker toxicity is the taking of too much of the medications known as calcium channel blockers (CCBs), either ... Calcium channel blockers, also known as calcium channel antagonists, are widely used for a number of health conditions. Thus ... The calcium channel blocker that caused the greatest number of deaths in 2010 in the United States was verapamil. This agent is ...
CACNG3
Voltage-dependent calcium channel gamma-3 subunit is a protein that in humans is encoded by the CACNG3 gene. L-type calcium ... This gene is a member of the neuronal calcium channel gamma subunit gene subfamily of the PMP-22/EMP/MP20 family. This gene is ... "Entrez Gene: CACNG3 calcium channel, voltage-dependent, gamma subunit 3". Powers PA, Liu S, Hogan K, Gregg RG (1993). " ... It is an integral membrane protein that is thought to stabilize the calcium channel in an inactive (closed) state. This protein ...
Cav1.4
"Entrez Gene: CACNA1F calcium channel, voltage-dependent, L type, alpha 1F subunit". Catterall WA, Perez-Reyes E, Snutch TP, ... a protein in the voltage-dependent calcium channel complex. Calcium channels mediate the influx of calcium ions into the cell ... 1998). "An L-type calcium-channel gene mutated in incomplete X-linked congenital stationary night blindness". Nat. Genet. 19 (3 ... Cav1.4 also known as the calcium channel, voltage-dependent, L type, alpha 1F subunit (CACNA1F), is a human gene. This gene ...
CACNG1
Voltage-dependent calcium channel gamma-1 subunit is a protein that in humans is encoded by the CACNG1 gene. L-type calcium ... 1993). "Localization of the gamma-subunit of the skeletal muscle L-type voltage-dependent calcium channel gene (CACNLG) to ... and gamma-subunits of the human skeletal muscle L-type voltage-dependent calcium channel on chromosome 17q and exclusion as ... This gene is a member of the neuronal calcium channel gamma subunit gene subfamily of the PMP-22/EMP/MP20 family and is located ...
Bay K8644
... is a chemical compound that functions as an L-type calcium channel agonist. Bay K8644 is used primarily as a ... Bay K8644 targets L-type voltage-gated calcium channels. It is the first positive inotropic agent shown to act specifically and ... that enhances calcium currents in guinea pig and calf myocardial cells. A new type of positive inotropic agent". Circ Res. 56 ( ... Calcium channel openers, Nitro compounds, All stub articles, Cardiovascular system drug stubs). ...
CACNG4
Voltage-dependent calcium channel gamma-4 subunit is a protein that in humans is encoded by the CACNG4 gene. L-type calcium ... This gene is a member of the neuronal calcium channel gamma subunit gene subfamily of the PMP-22/EMP/MP20 family and is located ... "Entrez Gene: CACNG4 calcium channel, voltage-dependent, gamma subunit 4". Gerhard DS, Wagner L, Feingold EA, et al. (2004). " ... Voltage-dependent calcium channel GRCh38: Ensembl release 89: ENSG00000075461 - Ensembl, May 2017 GRCm38: Ensembl release 89: ...
CACNG2
L-type calcium channels are composed of five subunits. The protein encoded by this gene represents one of these subunits, gamma ... Calcium channel, voltage-dependent, gamma subunit 2, also known as CACNG2 or stargazin is a protein that in humans is encoded ... "Entrez Gene: CACNG2 calcium channel, voltage-dependent, gamma subunit 2". Brandler WM, Antaki D, Gujral M, Noor A, Rosanio G, ... This gene is a member of the neuronal calcium channel gamma subunit gene subfamily of the PMP-22/EMP/MP20 family. Stargazin is ...
Metabolism
For example, muscle contraction depends upon the movement of calcium, sodium and potassium through ion channels in the cell ... Three types of photosynthesis occur in plants, C3 carbon fixation, C4 carbon fixation and CAM photosynthesis. These differ by ... Hundreds of separate types of dehydrogenases remove electrons from their substrates and reduce NAD+ into NADH. This reduced ... Chemolithotrophy is a type of metabolism found in prokaryotes where energy is obtained from the oxidation of inorganic ...
Childbirth
The most widely used tocolytics include beta agonists, calcium channel blockers, and magnesium sulfate. The goal of ... Otherwise depending on how far along the pregnancy is, medications may be used to start labour or a type of surgery known as ... Levine D (15 March 2012). "Types of Forceps Used in Delivery". Healthline. Healthline Networks. Retrieved 10 August 2013. ... three channels to pass through it: the urethra, the vagina and the rectum. The infant's head and shoulders must go through a ...
HSPA1B
It later becomes incorporated into the CatSper complex, a specialized calcium ion channel that enables spermatozoa motility. ... Han C, Chen T, Li N, Yang M, Wan T, Cao X (February 2007). "HDJC9, a novel human type C DnaJ/HSP40 member interacts with and ... Liu J, Xia J, Cho KH, Clapham DE, Ren D (June 2007). "CatSperbeta, a novel transmembrane protein in the CatSper channel complex ... Liu J, Xia J, Cho KH, Clapham DE, Ren D (June 2007). "CatSperbeta, a novel transmembrane protein in the CatSper channel complex ...
MiR-137
L type, alpha 1C subunit), DPYD (Dihydropyrimidine dehydrogenase [NADP+]), CACNB2 (Voltage-dependent L-type calcium channel ... miR-137 is located on human chromosome 1p22 and has been implicated to act as a tumor suppressor in several cancer types ... a well-known member of the Rho GTPase family found be upregulated in many human cancer types such as colorectal, testicular and ... and is reported to be frequently silenced by promoter hyper-methylation in many tumour types, including colorectal, gastric, ...
Anterograde tracing
Mn2+ enters through voltage dependent calcium channels, is taken into intracellular organelles and is transported by the ... "Transsynaptic transport of wheat germ agglutinin expressed in a subset of type II taste cells of transgenic mice". BMC ...
Voltage-gated ion channel
With sixteen different identified genes for human calcium channels, this type of channel differs in function between cell types ... glutamate-gated ion channels, calcium-dependent chloride channels, monovalent cation:proton antiporters, type 1, and potassium ... Voltage-gated sodium channels and calcium channels are made up of a single polypeptide with four homologous domains. Each ... Voltage-gated ion-channels are usually ion-specific, and channels specific to sodium (Na+), potassium (K+), calcium (Ca2+), and ...
Boris Khodorov
... studying the mechanisms of C-type inactivation in voltage-gated ion channels and the effects of neurotoxins and local ... Duchen at the University College London, Khodorov was studying calcium homeostasis, glutamate excitotoxicity and mitochondrial ... After Soviet science was liberalized in the 1960s, he moved to ion channels, developing as a leader in the actions of local ... At the Vishnevsky Institute of Surgery, the Khodorov laboratory carried out pioneering studies in the field of ion channel ...
Sodium-potassium pump
... there is a short-circuit channel (i.e. a highly K-permeable ion channel) for potassium in the membrane, thus the voltage across ... In many types of tissue, ATP consumption by the Na⁺/K⁺-ATPases have been related to glycolysis. This was first discovered in ... This increased presence of calcium is what allows for the force of contraction to be increased. In the case of patients where ... This enzyme belongs to the family of P-type ATPases. The Na⁺/K⁺-ATPase helps maintain resting potential, affects transport, and ...
Pre-Bötzinger complex
Other research has also suggested that calcium flow through N-type calcium channels is essential for normal breathing, and is ... L-type calcium channels are known to increase the frequency of action potentials in some neurons, which might be the reason ... P/Q-type calcium channels are mainly responsible for the release of neurotransmitters that excite, or activate, postsynaptic ... Fictive sigh depends critically on synaptic mechanisms that involve P/Q type calcium channels, suggestive of a subset of ...
Environmental effects of shipping
In addition, calcium hydroxide commonly being produced by calcination of calcium carbonate releases yet more carbon dioxide ... As of 2006, almost all of the petroleum-based diesel fuel available in Europe and North America is of a ULSD type. However, ... According to a Discovery Channel article on Sonic Sea Journeys Deep into the Ocean over the last century, extremely loud noise ... usually calcium sulfate if flue gases are scrubbed by being passed through calcium hydroxide solution) which would have to be ...
Hyperosmolar hyperglycemic state
... calcium channel blockers, and phenytoin) HHS is usually precipitated by an infection, myocardial infarction, stroke or another ... DKA usually occurs in type 1 diabetics whereas HHS is more common in type 2 diabetics. DKA is characterized by a rapid onset, ... The main risk factor is a history of diabetes mellitus type 2. Occasionally it may occur in those without a prior history of ... and abdominal pain Weakness Low blood pressure with standing The main risk factor is a history of diabetes mellitus type 2. ...
Olfactory receptor neuron
... the CNG ion channel is open allowing sodium and calcium to rush into the cell. The influx of calcium begins a cascade of events ... which are located on the membranes of the cilia have been classified as a complex type of ligand-gated metabotropic channels. ... Calcium first binds to calmodulin to form CaM. CaM will then bind to the CNG channel and close it, stopping the sodium and ... opens ion channels in the cell membrane, resulting in an influx of sodium and calcium ions into the cell, and an efflux of ...
Histamine H3 receptor
... the β and γ subunits interact with N-type voltage gated calcium channels, to reduce action potential mediated influx of calcium ... Silver RB, Poonwasi KS, Seyedi N, Wilson SJ, Lovenberg TW, Levi R (Jan 2002). "Decreased intracellular calcium mediates the ... "Histamine Receptors: H3". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology ...
Sigma-1 receptor
The σ1 receptor has been shown to appear in a complex with voltage gated K+ channels (Kv1.4 and Kv1.5), leading to the idea ... Kekuda R, Prasad PD, Fei YJ, Leibach FH, Ganapathy V (December 1996). "Cloning and functional expression of the human type 1 ... that modulates calcium signaling through the IP3 receptor. In humans, the σ1 receptor is encoded by the SIGMAR1 gene. The σ1 ... Mutations in sigma-1 receptor have been associated with distal spinal muscular atrophy type 2. The following ligands have high ...
Novel Therapeutic Targets for Antiarrhythmic Drugs
Subjects covered in the book include both traditional approaches to looking at arrhythmia, such as ion channel effects, and ... Overall, the book advocates for segregating drug targets by disease type and state, rather than the conventional approach of ... Novel ideas offered included studying sodium-calcium exchanger and ryanodine receptor effects. One chapter (5) is dedicated to ...
Oxycodone
... closing calcium channels, and opening potassium channels. Opioids like oxycodone are thought to produce their analgesic effects ... It may improve quality of life in certain types of pain. It is unclear if use in chronic pain results in improved quality of ...
Yale School of Medicine
... characterized calcium channel types Frans Wackers (1977-1981, 1984-): nuclear cardiologist Brian Kobilka (1977-1981): ...
Doxepin
Bertelsen, Anne K.; Backonja, Misha-Miroslav (2007). "Drugs Targeting Voltage-Gated Sodium and Calcium Channels". Encyclopedia ... These metabolizer types include poor, intermediate, extensive, and ultrarapid metabolizers. Most people are extensive ... Doxepin is also a potent blocker of voltage-gated sodium channels, and this action is thought to be involved in both its ... Individuals can be categorized into different types of cytochrome P450 metabolizers depending on which genetic variations they ...
Metabotropic glutamate receptor
... the opening of calcium channels increasing in this way the cytosolic calcium concentrations. The lipophilic diacylglycerol ... a type of ion channel-linked receptor that is central in a neurotoxic process called excitotoxicity. Proteins called PDZ ... They can also inhibit glutamate release and can modulate voltage-dependent calcium channels. Group I mGluRs, but not other ... Eight different types of mGluRs, labeled mGluR1 to mGluR8 (GRM1 to GRM8), are divided into groups I, II, and III. Receptor ...
Benign paroxysmal positional vertigo
BPPV is a type of balance disorder along with labyrinthitis and Ménière's disease. It can result from a head injury or simply ... Within the labyrinth of the inner ear lie collections of calcium crystals known as otoconia or otoliths. In people with BPPV, ... These drugs vary considerably in their mechanisms of action, with many of them being receptor- or ion channel-specific. Among ... The Epley maneuver employs gravity to move the calcium crystal build-up from the posterior semicercular canal ( resulting in ...
Defender (association football)
"La Storia del Calcio: Il calcio dalle origini a oggi" (in Italian). Treccani: Enciclopedia dello Sport (2002). Retrieved 18 May ... A quick passing movement like a pair of one-two passes will leave the channel behind the defending full-back open. This ... there were often at least two types of centre-backs who played alongside one another: at least one man-to-man marking centre- ... Damele, Fulvio (1998). Calcio da manuale. Demetra. p. 104. Fontana, Mattia (7 July 2015). "L'evoluzione del libero: da Picchi a ...
Effects of cannabis
... inhibit calcium N channels, and disinhibit K+A channels. There are at least two types of cannabinoid receptors (CB1 and CB2). ...
Earthworm
The three types of nephridia are: integumentary, septal, and pharyngeal. The integumentary nephridia lie attached to the inner ... Food moves into the esophagus, where calcium (from the blood and ingested from previous meals) is pumped in to maintain proper ... Physical: The earthworm's burrowing creates a multitude of channels through the soil and is of great value in maintaining the ... blood calcium levels in the blood and food pH. From there the food passes into the crop and gizzard. In the gizzard, strong ...
Publix
In May 2014, Publix began offering Amlodipine, a calcium channel blocker used to treat high blood pressure and chest pain ( ... The store marked the first under the Food World banner for Publix and would become the first of 22 more of the type. In ... Publix announced in August 2007, that it would offer several types of antibiotics free to its customers. Customers must have a ... In March 2010, Publix announced the launch of another free prescription, Metformin for Type II Diabetes, the generic of ...
WNK1
... and large conductance calcium-activated potassium channel (BKCa) are the two primary channels for potassium secretion. WNK1 ... WNK1 has mutations associated with Gordon hyperkalemia-hypertension syndrome (pseudohypoaldosteronism Type II, featuring ... WNK1 regulates potassium channels found in the cortical collecting duct (CCD) and connecting tubule (CNT). Renal outer medullar ... GABA activates the GABAA receptor which is a Cl− ion channel. Cl− ions will enter the neuron causing hyperpolarization and ...
Find-me signals
The enzyme calcium-independent phospholipase A2 (iPLA2) is most likely responsible for the apoptotic cell releasing LPC as it ... Four types of find-me signals released from apoptotic cells have been discovered: Lipid lysophosphatidylcholine (LPC) ... They are released through a pannexin family channel known as PANX1. PANX1 is a four pass transmembrane protein that forms large ... "Pannexin 1 channels mediate 'find-me' signal release and membrane permeability during apoptosis". Nature. 467 (7317): 863-867. ...
Luciferase
Different types of cells (e.g. bone marrow stem cells, T-cells) can be engineered to express a luciferase allowing their non- ... Therefore, in order to lower the pH, voltage-gated channels in the scintillon membrane are opened to allow the entry of protons ... Calcium triggers release of the luciferin (coelenterazine) from the luciferin binding protein. The substrate is then available ... "BL Web: Luciferin types". ISCID Encyclopedia of Science and Philosophy. ISCID. Archived from the original on 2012-09-21. ...
Loop diuretic
... s also inhibit magnesium and calcium reabsorption in the thick ascending limb. Absorption of magnesium and calcium ... The difference in voltage in both sides are set up by potassium recycling through renal outer medullary potassium channel. By ... Meanwhile, according to 2013 European Society of Cardiology (ESC) guidelines, a loop diuretic can only replace thiazide-type ... This causes the magnesium and calcium ions to be repelled from luminal side to interstitial side, promoting their absorption. ...
Index of biochemistry articles
... calcium channel - calcium signaling - calcium-binding protein - calmodulin - calmodulin-binding protein - Calvin cycle - CAM ... IGF type 1 receptor - IGF type 2 receptor - IgG - IgM - immediate-early protein - immune cell - immune system - immunoglobulin ... Ion channel - ion channel gating - Ionic bond - ionization potential - iron-sulfur protein - isoenzyme - isoleucine - Isomer - ... interferon type I - interferon type II - interferon-alpha - interferon-beta - interleukin receptor - interleukin-1 receptor - ...
Calcium channel blockers: Types, list, side effects, uses & more
Calcium channel blockers are a common type of medication for high blood pressure and heart conditions. Learn how these ... Calcium channel blockers are a type of medication that people take to increase the flow of blood and oxygen to the heart. ... What are calcium channel blockers? Types, examples, side effects, and all else you need to know. ... Dihydropyridines target a specific type of calcium channel in the body. They cause the blood vessels to widen, lowering blood ...
Primary structure and functional expression of the omega-conotoxin-sensitive N-type calcium channel from rabbit brain
The complete amino acid sequence of a rabbit brain calcium channel (BIII) has been deduced by cloning and sequencing the cDNA. ... Primary structure and functional expression of the omega-conotoxin-sensitive N-type calcium channel from rabbit brain Neuron. ... The complete amino acid sequence of a rabbit brain calcium channel (BIII) has been deduced by cloning and sequencing the cDNA. ... sensitive calcium current with kinetics and voltage dependence like those previously reported for whole-cell N-type current. ...
L-type calcium channel
... The L-type calcium channel is a type of voltage-dependent calcium channel. Like the others of this class ... Calcium channel. Voltage-dependent calcium channel (L-type/Cavα(1.1, 1.2, 1.3, 1.4), N-type, P-type/Cavα(2.1), Q-type, R-type, ... The L-type calcium channel is a type of voltage-dependent calcium channel. Like the others of this class, the α1 subunit is the ... L-type calcium channel blockers are used as antiarrhythmics or antihypertensives, depending on whether the drugs has higher ...
Analgesic conotoxins: block and G protein-coupled receptor modulation of N-type (Ca(V) 2.2) calcium channels
These peptides target a wide variety of membrane receptors, ion channels and transporters, and have enormous potential for a ... Analgesic conotoxins: block and G protein-coupled receptor modulation of N-type (Ca(V) 2.2) calcium channels Br J Pharmacol. ... Structurally related ω-conotoxins bind directly to and selectively inhibit neuronal (N)-type voltage-gated calcium channels ( ... A series of newly discovered ω-conotoxins from Conus catus, including CVID-F, are potent and selective antagonists of N-type ...
Cacna1c MGI Mouse Gene Detail - MGI:103013 - calcium channel, voltage-dependent, L type, alpha 1C subunit
IPR005451 Voltage-dependent calcium channel, L-type, alpha-1C subunit. IPR005446 Voltage-dependent calcium channel, L-type, ... IPR031649 Voltage-dependent L-type calcium channel, IQ-associated domain. IPR031688 Voltage-gated calcium channel subunit alpha ... IPR002077 Voltage-dependent calcium channel, alpha-1 subunit. IPR014873 Voltage-dependent calcium channel, alpha-1 subunit, IQ ... J:329880 Sanderson JL, et al., The CaV1.2 G406R mutation decreases synaptic inhibition and alters L-type Ca(2+) channel- ...
Ca(v)1.4 L-Type Calcium Channels Contribute to Calpain Activation in Degenerating Photoreceptors of rd1 Mice
Schön, Christian; Paquet-Durand, Francois; Michalakis, Stylianos (2016): Ca(v)1.4 L-Type Calcium Channels Contribute to Calpain ... 1.4 L-type voltage-gated calcium channels (VGCC). Previously, we have shown that genetic ablation of the Cngb1 gene encoding ... In this study, we crossbred rd1 mice with the Cacna1f-deficient mouse lacking the Ca(v)1.4 alpha 1 subunit of the L-type VGCC. ... Our results show that genetic deletion of the synaptic Ca-v 1.4 L-type VGCCs impairs calpain activation and leads to a short- ...
2022 - Novel Fluorescence-Based High-Throughput FLIPR Assay Utilizing Membrane-Tethered Genetic Calcium Sensors to Identify T...
Type Calcium Channel Modulators SyncroPatch 384PE (a predecessor model of the SyncroPatch 384 instrument) Publication in ACS ... To illustrate, T-type Ca2+ channels are largely inactivated and unable to open to allow Ca2+ influx at −25 mV, the typical ... T-type voltage-gated Ca2+ channels have been implicated in many human disorders, and there has been increasing interest in ... However, the unique biophysical properties of T-type Ca2+ channels are not conducive for developing high-throughput screening ( ...
CACNG6 calcium voltage-gated channel auxiliary subunit gamma 6 [Homo sapiens (human)] - Gene - NCBI
Cardiac L-type calcium channel (Cav1.2) associates with gamma subunits. Yang L, et al. FASEB J, 2011 Mar. PMID 21127204, Free ... voltage-dependent calcium channel gamma-6 subunit. Names. calcium channel, voltage-dependent, gamma subunit 6. neuronal voltage ... part_of L-type voltage-gated calcium channel complex IBA Inferred from Biological aspect of Ancestor. more info ... part_of L-type voltage-gated calcium channel complex IDA Inferred from Direct Assay. more info ...
The terpenes camphene and alpha-bisabolol inhibit inflammatory and neuropathic pain via Cav3.2 T-type calcium channels. | Pain...
Centrally expressed Cav3.2 T-type calcium channel is critical for the initiation and maintenance of neuropathic pain. ... The terpenes camphene and alpha-bisabolol inhibit inflammatory and neuropathic pain via Cav3.2 T-type calcium channels.. ... The terpenes camphene and alpha-bisabolol inhibit inflammatory and neuropathic pain via Cav3.2 T-type calcium channels. ... The terpenes camphene and alpha-bisabolol inhibit inflammatory and neuropathic pain via Cav3.2 T-type calcium channels. ...
Calcium Channel Blocker Toxicity: Practice Essentials, Background, Pathophysiology
Calcium channel blocker (CCB) toxicity is one of the most lethal prescription drug overdoses; therefore, understanding the ... 9] The L-type calcium channel blockers decrease the flow of calcium into the cells of the cardiac conduction pathway, which ... encoded search term (Calcium Channel Blocker Toxicity) and Calcium Channel Blocker Toxicity What to Read Next on Medscape ... L-type calcium channels mediate the influx of calcium during depolarization in arterial smooth muscle. Clevidipine reduces mean ...
Down-regulation of L-type calcium channel and sarcoplasmic reticular Ca2+-ATPase mRNA in human atrial fibrillation without...
We investigated the gene expression of calcium-handling genes including L-type calcium channel, sarcoplasmic reticular calcium ... We investigated the gene expression of calcium-handling genes including L-type calcium channel, sarcoplasmic reticular calcium ... We investigated the gene expression of calcium-handling genes including L-type calcium channel, sarcoplasmic reticular calcium ... We investigated the gene expression of calcium-handling genes including L-type calcium channel, sarcoplasmic reticular calcium ...
Effects of combination of perindopril, indapamide, and calcium channel blockers in patients with type 2 diabetes mellitus:...
Effects of combination of perindopril, indapamide, and calcium channel blockers in patients with type 2 diabetes mellitus: ... T1 - Effects of combination of perindopril, indapamide, and calcium channel blockers in patients with type 2 diabetes mellitus ... Effects of combination of perindopril, indapamide, and calcium channel blockers in patients with type 2 diabetes mellitus: ... Effects of combination of perindopril, indapamide, and calcium channel blockers in patients with type 2 diabetes mellitus : ...
Calcium channel blockers - Mayo Clinic
Types of blood pressure medications. American Heart Association. https://www.heart.org/en/health-topics/high-blood-pressure/ ... Examples of calcium channel blockers. Calcium channel blockers are available in short-acting and long-acting forms. Short- ... Calcium causes the heart and arteries to squeeze (contract) more strongly. By blocking calcium, calcium channel blockers allow ... Calcium channel blockers are medications used to lower blood pressure. They work by preventing calcium from entering the cells ...
Calcium-channel blocker overdose: MedlinePlus Medical Encyclopedia
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 ... Verapamil (a type of calcium channel blocker) overdose is associated with the highest mortality risk. ...
Calcium channel blockers as antihypertensive agents : a need for caution : reports on individual drugs
dc.type. Journal / periodical articles. dc.subject.meshqualifier. adverse effects. en. dc.subject.meshqualifier. adverse ... Calcium channel blockers as antihypertensive agents : a need for caution : reports on individual drugs. dc.date.accessioned. ... Calcium channel blockers as antihypertensive agents : a need for caution : reports on individual drugs. en. ...
α|inf|1G|/inf| T-type calcium channel selectively regulates P-selectin surface expression in pulmonary capillary endothelium
T-type calcium channel selectively regulates P-selectin surface expression in pulmonary capillary endothelium Academic Article ... expression considerably mitigated by pharmacologic blockade of the T-type channel or genetic knockout of the T-type channel α1G ... the regulated P-selectin surface expression is triggered by Ca2+ transients evoked through activation of the α1G T-type channel ... Ca2+ transients also provoked P-selectin surface expression in alveolar capillaries that was abolished by T-type channel ...
Details for: Low-voltage-activated t-type calcium channels : › WHO HQ Library catalog
Calcium channels -- physiology -- pharmacology -- congresses , Cell communication -- congresses , Calcium channel blockers -- ... Low-voltage-activated t-type calcium channels : proceedings from the International Electrophysiology meeting, Montpellier, 21- ... Item type. Current library. Call number. Copy number. Status. Date due. Barcode. ... JoëlMaterial type: TextPublication details: Chester : Adis International, 1998. Description: 394 pISBN: 1898970823Subject(s): ...
Exploring the potential utility of calcium channel inhibitors in SARS-CoV-2 infection
... researchers discuss the role of calcium signaling pathways as targets of inhibition in potential new antiviral therapeutic ... The entry of calcium into the cells occurs via several types of calcium channels. ... This leads to CRAC channel activation.. CRAC channels regulate calcium channels in multiple cells including T cells, where they ... exploiting the various types of calcium channels.. Inhibition of such channels must also take into account the many and diverse ...
Structural basis for anion conduction in the calcium-activated chloride channel TMEM16A - Zurich Open Repository and Archive
Item Type:. Journal Article, refereed, original work. Communities & Collections:. 04 Faculty of Medicine , Department of ... The calcium-activated chloride channel TMEM16A is a member of a conserved protein family that comprises ion channels and lipid ... The calcium-activated chloride channel TMEM16A is a member of a conserved protein family that comprises ion channels and lipid ... Structural basis for anion conduction in the calcium-activated chloride channel TMEM16A ...
Calcium Channel Blocker Toxicity Clinical Presentation: History, Physical Examination
Calcium channel blocker (CCB) toxicity is one of the most lethal prescription drug overdoses; therefore, understanding the ... If the patient ingested medications, ascertain type, dose, and number or amount. With young children, ask for a complete list ... encoded search term (Calcium Channel Blocker Toxicity) and Calcium Channel Blocker Toxicity What to Read Next on Medscape ... because calcium channel blockers may cause enteric dysmotility. Bowel perforation secondary to calcium channel blocker ...
Association of A Novel Splice Site Mutation in P/Q-Type Calcium Channels with Childhood Epilepsy and Late-Onset Slowly...
Association of A Novel Splice Site Mutation in P/Q-Type Calcium Channels with Childhood Epilepsy and Late-Onset Slowly ... Association of A Novel Splice Site Mutation in P/Q-Type Calcium Channels with Childhood Epilepsy and Late-Onset Slowly ... The disease is associated with mutations in the voltage-gated calcium channel alpha 1A subunit (Cav2.1) that is encoded by the ... laevis oocytes expressing a wild-type versus mutant channel showed that the genetic defect caused a complete loss of channel ...
Novel neuroactive steroid with hypnotic and T-type calcium channel blocking properties exerts effective analgesia in a rodent...
Dive into the research topics of Novel neuroactive steroid with hypnotic and T-type calcium channel blocking properties exerts ... Novel neuroactive steroid with hypnotic and T-type calcium channel blocking properties exerts effective analgesia in a rodent ... Novel neuroactive steroid with hypnotic and T-type calcium channel blocking properties exerts effective analgesia in a rodent ... Novel neuroactive steroid with hypnotic and T-type calcium channel blocking properties exerts effective analgesia in a rodent ...
T-Type Calcium Channels - Structure-based characterization of novel Aurora Kinase inhibitors
Posted in T-Type Calcium Channels Search. Search. Recent Posts. *Intra\time and inter\time precision as symbolized with the ... Category: T-Type Calcium Channels. As shown in Figure 3C, JMJD6 was indeed able to decrease H4R3 ADMA test in which, ... Posted in T-Type Calcium Channels His-AfGST bound to LL-beads clearly, as shown from the same assay depicted in Shape 2a, as ... Similarly, inhibition of BK (1 M paxilline) or SK (300 nM apamin) channels had no effect on baseline afferent activity compared ...
P-Type Calcium Channels - Recent Advances in the Discovery of tyrosinase inhibitors
B.O.O.K Low-voltage-activated T-type calcium channels Ebook
Download Low-voltage-activated T-type calcium channels. Read Low-voltage-activated T-type calcium channels. A Guide for Parents ... Low-voltage-activated T-type calcium channels buy ebook Low-voltage-activated T-type calcium channels ibook download Cognitive ... artificielle ebook Low-voltage-activated T-type calcium channels pdf download Low-voltage-activated T-type calcium channels . ... B.O.O.K Low-voltage-activated T-type calcium channels Ebook. ... download Low-voltage-activated T-type calcium channels pdf ...
KEGG DGROUP: Dihydropyridine calcium channel blocker
Targeting intrinsically disordered regions facilitates disco... : PAIN
Ample data support a prominent role of peripheral T-type calcium channels 3.2 (CaV3.2) in generating ... 2.5.1. T-type/calcium channels 3.2 calcium channel current on cultured cell lines. Modified Tyrode solution consists of the ... potassium channels, enabling KCa1.1 activation,70 and may also affect sodium channels.30 T-type calcium channel specificity of ... Trigeminal neuropathic pain is alleviated by inhibition of Cav3.3 T-type calcium channels in mice. Channels (Austin) 2021;15:31 ...
T-Type Calcium Channels
Preparation, Antiepileptic Activity, and Cardiovascular Safety of Dihydropyrazoles as Brain-Penetrant T-Type Calcium Channel...
Types of Osteoarthritis Medications and Treatments
Learn about drug types, how they work, side effects, and other treatments. ... NSAID/calcium channel blocker. A combination formulation of NSAID and calcium channel blocker reduces pain and inflammation, ... The FDA-approved combination NSAID/calcium channel blocker drug for osteoarthritis patients with hypertension is:. *Celecoxib/ ... Osteoarthritis is a type of arthritis that involves the entire joint. Osteoporosis is not a type of arthritis. It is a disease ...
BlockersSubunitInhibitorsIntracellular calciumVerapamilDiltiazemInhibitionInfluxReceptorsCardiacDihydropyridineChlorideBlood vessels to relax and openAbstractExtracellularSodiumPharmacologySynapticDiabetesGeneCurrentsProteinVGCCsSelectivelyMedicationsMembraneNeuronsPulmonaryNifedipineAntagonistAntihypertensive agentsNeuronalNeuropathic painSelectiveATPasesMedicationLTCCHomeostasisAnalgesicsCACNA1GPatientsIngestionSkeletalModulateIrregular heartbeatIonsConcentrationHuman atrialOrganismDistinctInhibitVoltage
Blockers44
- What are calcium channel blockers? (medicalnewstoday.com)
- Calcium channel blockers are a type of medication that people take to increase the flow of blood and oxygen to the heart. (medicalnewstoday.com)
- Calcium channel blockers reduce the amount of calcium that can enter muscle cells in the heart and blood vessel walls through these channels. (medicalnewstoday.com)
- Calcium channel blockers are common medications that have a low risk of complications. (medicalnewstoday.com)
- There are two different types of calcium channel blockers, which are called dihydropyridines and nondihydropyridines. (medicalnewstoday.com)
- Doctors may also minimize this risk by prescribing extended-release calcium channel blockers. (medicalnewstoday.com)
- Doctors commonly use calcium channel blockers to treat high blood pressure . (medicalnewstoday.com)
- Scientists are currently exploring other potential uses for calcium channel blockers. (medicalnewstoday.com)
- For example, by reducing high blood pressure, they believe that calcium channel blockers may be able to lower the risk of Alzheimer's disease . (medicalnewstoday.com)
- Several other types of medication have an effect similar to that of calcium channel blockers. (medicalnewstoday.com)
- 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)
- The American Heart Association recommends 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)
- L-type calcium channel blockers are used as antiarrhythmics or antihypertensives, depending on whether the drugs has higher affinity to the heart (like verapamil ) or to the vessels ( nifedipine ). (bionity.com)
- The objective of the present analysis was to determine the effects of a fixed combination of perindopril and indapamide in combination with calcium channel blockers (CCBs) in patients with type 2 diabetes mellitus. (elsevier.com)
- Calcium channel blockers are medications used to lower blood pressure. (mayoclinic.org)
- By blocking calcium, calcium channel blockers allow blood vessels to relax and open. (mayoclinic.org)
- Some calcium channel blockers can also slow the heart rate, which can further lower blood pressure. (mayoclinic.org)
- Calcium channel blockers are also called calcium antagonists. (mayoclinic.org)
- Calcium channel blockers are available in short-acting and long-acting forms. (mayoclinic.org)
- For blacks and older people, calcium channel blockers might work better than other blood pressure medications, such as beta blockers, angiotensin-converting enzyme (ACE) inhibitors or angiotensin II receptor blockers. (mayoclinic.org)
- Avoid grapefruit products while taking certain calcium channel blockers. (mayoclinic.org)
- Calcium-channel blockers are a type of medicine used to treat high blood pressure and heart rhythm disturbances. (medlineplus.gov)
- Other medicines may also contain calcium-channel blockers. (medlineplus.gov)
- Earlier, calcium channel blockers were successfully tested against flu viruses, the Japanese encephalitis virus, and the Ebola virus, among others. (news-medical.net)
- Treatment with calcium channel blockers was associated with an anti-inflammatory effect and thus a reduced likelihood of cytokine storm . (news-medical.net)
- [ 14 ] These onset times should be considered when discharging patients home who may or may not have ingested calcium channel blockers. (medscape.com)
- A series of dihydropyrazole derivatives was developed as potent, selective, and brain-penetrating T-type calcium channel blockers. (sophion.com)
- This indicates that ZNS is distinct from other T-type calcium channel blockers in terms of modulation of the voltage dependence of the mutant Ca V 3.1. (biomedcentral.com)
- These results suggest that ZNS is distinct from other T-type calcium channel blockers in terms of its modulation of the voltage dependence of the mutant Ca V 3.1. (biomedcentral.com)
- Blain A, Greally E, Laval S, Blamire A, Straub V, MacGowan GA. Beta-Blockers, Left and Right Ventricular Function, and In-Vivo Calcium Influx in Muscular Dystrophy Cardiomyopathy . (ncl.ac.uk)
- The pharmacology of these calcium channel blockers is very well-understood, so an understanding of how they influence myelination could potentially bring us closer to new therapies more rapidly than some other therapeutic possibilities," said Lawrence Wrabetz, MD, professor of neurology and biochemistry and director of the HJKRI. (buffalo.edu)
- IMSEAR at SEARO: Calcium channel blockers in acute inflammation. (who.int)
- Srivastava VK, Saxena KK, Gupta B. Calcium channel blockers in acute inflammation. (who.int)
- Alternatives to metoprolol for the treatment of AFib include other beta-blockers, calcium channel blockers, and digoxin. (druggenius.com)
- Alternatives for metoprolol for the treatment of high blood pressure include other beta-blockers and calcium channel blockers. (druggenius.com)
- Calcium channel blockers, such as verapamil hydrochloride and diltiazem hydrochloride, lower blood pressure by preventing calcium from entering the cells of the heart and arteries. (druggenius.com)
- Calcium channel blockers , which work similarly to beta-blockers to stop arrhythmias. (druggenius.com)
- Alternatives to metoprolol for the treatment of PVCs include other beta-blockers, calcium channel blockers, or anti-arrhythmic drugs, such as amiodarone (Pacerone) or flecainide (Tambocor). (druggenius.com)
- Alternative drugs for the treatment of SVT include adenosine (Adenocard), which also decreases heart rate, calcium channel blockers (like diltiazem), digoxin (Lanoxin), other beta-blocker or amiodarone (Cordarone, Pacerone). (druggenius.com)
- Alternative medications for palpitations may include other beta-blockers, ACE inhibitors, calcium channel blockers, and digoxin to lower blood pressure and slow the heart rate. (druggenius.com)
- calcium channel blockers lower blood high cholesterol arteries pressure within 50 years. (atime.org)
- high blood pressure medication labetalol side effects These medications are available to calcium channel blockers, and then calcium channel blocker. (atime.org)
- Here, L-type calcium channel blockers obtained from a U.S. Food and Drug Administration (FDA)-approved compound library were identified as effective anti-SFTSV compounds. (bvsalud.org)
- In this article, L-type calcium channel blockers were identified as anti-SFTSV compounds through an FDA-approved compound library screen. (bvsalud.org)
Subunit9
- Previously, we have shown that genetic ablation of the Cngb1 gene encoding the B subunit of the rod CNG channel delays the fast progressing degeneration in the rd1 mutant mouse model of retinitis pigmentosa. (uni-muenchen.de)
- In this study, we crossbred rd1 mice with the Cacna1f-deficient mouse lacking the Ca(v)1.4 alpha 1 subunit of the L-type VGCC. (uni-muenchen.de)
- This particular gamma subunit is an integral membrane protein that is thought to stabilize the calcium channel in an inactive (closed) state. (nih.gov)
- Only in capillaries was the thrombin-stimulated P-selectin surface expression considerably mitigated by pharmacologic blockade of the T-type channel or genetic knockout of the T-type channel α1G-subunit. (uab.edu)
- The disease is associated with mutations in the voltage-gated calcium channel alpha 1A subunit (Cav2.1) that is encoded by the CACNA1A gene. (synergy-munich.de)
- and T‑type, which are encoded by α1 subunit genes. (spandidos-publications.com)
- These alterations of L-type HVCC subunit expressions followed the increased their mRNA expressions, suggesting that the L-type HVCC functions associated with increase in their protein molecules are involved in development of physical dependence. (nii.ac.jp)
- In addition, the differences in L-type HVCC subunit expression patterns and in response of L-type HVCC subunit expression to dantrolene are considered to suggest different pathogenesis between physical and psychological dependence. (nii.ac.jp)
- The total and membrane protein expression levels of Cav1.2 [pore-forming subunit of L-type calcium channels (LTCC)], but not the insulin receptors, were decreased in OZR. (cdc.gov)
Inhibitors10
- Angiotensin converting enzyme (ACE) inhibitors are another type of medication for high blood pressure and a variety of heart conditions. (medicalnewstoday.com)
- Here, we describe a novel GCaMP6s-CAAX-based calcium assay utilizing a high-throughput fluorometric imaging plate reader (Molecular Devices, Sunnyvale, CA) format that can identify both activators and inhibitors of T-type Ca 2+ channels. (nanion.de)
- The current paper discusses the potential for the use of calcium inhibitors in SARS-CoV-2 infections. (news-medical.net)
- Several inhibitors of these channels, such as amlodipine, nifedipine, felodipine, verapamil and diltiazem are being tested for the current infection as well. (news-medical.net)
- Development of primary sensory neuron-specific inhibitors of Ca V 3.2 channels is an opportunity for achieving effective analgesic therapeutics, but success has been elusive. (lww.com)
- Thus, an MLPCN high-throughput screen (HTS) was conducted to identify novel T-type Ca(2+) channel inhibitors free from IP constraints, and freely available through the MLPCN, for use by the biomedical community to study T-type Ca(2+) channels. (vanderbilt.edu)
- Based on the basal ganglia circuitry in Parkinson's disease (PD), the effects of ML218 in STN neurons suggest a therapeutic role for T-type Ca(2+) channel inhibitors, and ML218 was found to be orally efficacious in haloperidol-induced catalepsy, a preclinical PD model, with comparable efficacy to an A(2A) antagonist, a clinically validated PD target. (vanderbilt.edu)
- Sodium glucose cotransporter 2 inhibitors (SGLT2i) are the first antidiabetic compounds that effectively reduce heart failure hospitalization and cardiovascular death in type 2 diabetics. (frontiersin.org)
- Sodium glucose cotransporter 2 (SGLT2) inhibitors (SGLT2i) are kidney-targeted anti-diabetic agents that have exhibited marked reductions in cardiovascular events and mortality of type 2 diabetes (T2D) patients. (frontiersin.org)
- Phosphodiesterase type 4 inhibitors and on-demand paroxetine in arousal cues adds to the processing of the skin into a for a particular collier draws upon a number of gay ance occurring in mid- to late adult life. (gatech.edu)
Intracellular calcium4
- BACKGROUND: Recent studies have demonstrated that atrial electrical remodeling in atrial fibrillation is associated with intracellular calcium overload. (elsevier.com)
- These changes in intracellular calcium dynamics are considered to participate in psychological dependence by MET and cocains. (nii.ac.jp)
- Includes calculation of intracellular Calcium. (yale.edu)
- 17] Moreover, it has been suggested that an extracellular calcium-sensing receptor (CaSR) also contributes to the rise in intracellular calcium concentration. (hardmix.net)
Verapamil5
- Verapamil (a type of calcium channel blocker) overdose is associated with the highest mortality risk. (medlineplus.gov)
- The principal mechanism of action for Verapamil is to prevent calcium entering cells. (trymable.com)
- Research suggests that Verapamil has an effect on many different types of calcium channels, some of which are found in high numbers in the trigeminal system, and other parts of the brain and brainstem. (trymable.com)
- Acting at these calcium channels to prevent nerve activation, Verapamil reduces the likelihood of migraines occurring. (trymable.com)
- També vam demostrar que la combinació amb verapamil, un inhibidor dels canals de calci, augmentava l'alliberament viral, la citotoxicitat i l'eficàcia antitumoral en varis models tumorals. (ub.edu)
Diltiazem3
- The image below illustrates the chemical structure of the calcium channel blocker diltiazem. (medscape.com)
- Chronic administrations of ethanol, morphine, and nicotine produced increase of Bmax values of [^3H] diltiazem binding to the particulate fractions from animal cerebral cortex and increased expressions of α1C and α1D subunits of L-type high voltage-gated calcium channels (HVCCs) in animal cerebral cortex. (nii.ac.jp)
- Similarly, long-term exposure of cerebrocortical neurons in primary culture to these drugs of abuse also increased Bmax values of [^3H]diltiazem binding and expressions of α1C and α1D subunits of L-type HVCCs. (nii.ac.jp)
Inhibition9
- A new paper, published in Cells , discusses the role of calcium signaling pathways as targets of inhibition in potential new antiviral therapeutic pathways. (news-medical.net)
- A new plant-derived natural small molecule, called neferine, was also identified as a potential entry inhibitor of the virus, and showed 75% inhibition of infection in cell cultures in a pseudovirus assay, by inhibiting calcium channels in the cell membrane. (news-medical.net)
- The role of calcium has been well documented in numerous cellular processes, including cell proliferation and inhibition and activation of various intracellular enzymes ( 23 - 25 ). (spandidos-publications.com)
- Electrophysiology studies in subthalamic nucleus (STN) neurons demonstrated robust effects of ML218 on the inhibition of T-Type calcium current, inhibition of low threshold spike and rebound burst activity. (vanderbilt.edu)
- However, inhibition of Ca2+ influx through voltage-operated calcium channels and L-type Ca(2+)channel blocking effect appears to be involved in the mechanism of vasorelaxant effect of TMB at high concentrations. (ktu.edu.tr)
- Inhibition of L-type calcium channels for preventing noise induced hearing loss and tinnitus. (cdc.gov)
- Inhibition of calcineurin, the activation of which is triggered by calcium influx, using FK506 or cyclosporine was shown to reduce SFTSV production, suggesting the important role of calcium signaling on SFTSV genome replication. (bvsalud.org)
- Inhibition of cancer cell growth and c-Myc transcriptional activity by a c-Myc helix 1-type peptide fused to an internalization sequence. (semanticscholar.org)
- Inhibition of cancer cell growth by calcium channel antagonists in the athymic mouse. (semanticscholar.org)
Influx5
- To illustrate, T-type Ca 2+ channels are largely inactivated and unable to open to allow Ca 2+ influx at −25 mV, the typical resting membrane potential of the cell lines commonly used in cellular screening assays. (nanion.de)
- Membrane depolarization causes the rapid influx of calcium, shifting the membrane potential towards the positive side. (news-medical.net)
- In vivo myocardial calcium influx is increased in the delta sarcoglycan deficient mouse model of muscular dystrophy cardiomyopathy. (ncl.ac.uk)
- Journal Article] First phase of glucose-stimulated insulin secretion from MIN 6 cells does not always require extracelluar calcium influx. (nii.ac.jp)
- Furthermore, the L-type calcium current (ICaL) in OZR exhibited defective inactivation and lost the complete inactivation back to the closed state, leading to increased Ca2+ influx. (cdc.gov)
Receptors7
- In skeletal muscle, there is a very high concentration of DHP receptors, representing L-type calcium channels, situated in the T-tubules. (bionity.com)
- These peptides target a wide variety of membrane receptors, ion channels and transporters, and have enormous potential for a range of pharmaceutical applications. (nih.gov)
- However, unlike many forms of synaptic plasticity, thalamoamygdala LTP was independent of NMDA receptors, despite their presence at these synapses, and instead was dependent on L-type voltage-gated calcium channels. (nyu.edu)
- Endocannabinoids (eCBs) are endogenous lipids that bind principally type‐1 and type‐2 cannabinoid (CB1 and CB2) receptors. (semanticscholar.org)
- In addition, sustained exposure to MET and cocaine significantly enhanced ryanodine-induced increase of calcium oscillation in cerebrocortical neurons when examining with fura-2, suggesting the lonf-term exposure to MET and cocaine enhanced ryanodine receptors through which calcium-induced calcium release. (nii.ac.jp)
- These receptors could also impact the function and manifestation of CCR5 and CXCR4 on human being monocytes, two main GPCR chemokine coreceptors of human being immunodeficiency pathogen type 1 (HIV-1) [14], [15]. (mdm2-inhibitors.com)
- Furthermore, human being FPR expression continues to be observed in several distinct cells and cell types ([6]C[7] and sources therein), indicating a much broad distribution of the receptors and their significant role in vivo physiologically. (mdm2-inhibitors.com)
Cardiac7
- Cardiac L-type calcium channel (Cav1.2) associates with gamma subunits. (nih.gov)
- These are the channels allowing for the fastest movement of calcium ions in the cytosol and are thus found in excitable tissues, including pacemaker, neuronal or certain types of cardiac cells, as well as skeletal muscle cells. (news-medical.net)
- When calcium channel blocker 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)
- Blain A, Greally E, Laval S, Straub V, MacGowan G. An MRI study of the effects of metoprolol on in vivo cardiac calcium homeostasis . (ncl.ac.uk)
- Here, we review the direct effects of SGLT2i Empagliflozin (Empa), Dapagliflozin (Dapa), and Canagliflozin (Cana) on various cardiac cell types and cardiac function, and how these may contribute to the cardiovascular benefits observed in large clinical trials. (frontiersin.org)
- These results also provided mechanistic insights into a remodeled cardiac electrophysiology under the condition of insulin resistance, enhancing our understanding of long QT associated with obese type 2 diabetic patients. (cdc.gov)
Dihydropyridine3
- A phylogenetic tree representing evolutionary relationships indicates that BIII is grouped together with the other rabbit brain calcium channels, BI and BII, into a subfamily that is distinct from the dihydropyridine-sensitive L-type subfamily. (nih.gov)
- Nitrendipine, a dihydropyridine calcium channel antagonist is a typical poorly water-soluble drug. (sphinxsai.com)
- Dihydropyridine calcium channel-blocking drugs are not recommended for the treatment of HFrEF. (medscape.com)
Chloride1
- The calcium-activated chloride channel TMEM16A is a member of a conserved protein family that comprises ion channels and lipid scramblases. (uzh.ch)
Blood vessels to relax and open1
- So, blocking calcium allows blood vessels to relax and open. (druggenius.com)
Abstract1
- Motivated by the negative feedback calcium exerts on the gating dynamics of a calcium-conducting ion channel in olfactory receptor neurons, we develop an abstract two-state (open/closed) signalling module with negative feedback. (math.ca)
Extracellular2
- To address this issue, we developed cell lines that express K ir 2.3 channels to hyperpolarize the membrane potential to −70 mV, thus allowing T-type channels to return to their resting state where they can be subsequently activated by membrane depolarization in the presence of extracellular KCl. (nanion.de)
- 3], Elevation of extracellular calcium concentrations induces an increase in intracellular free calcium concentrations. (hardmix.net)
Sodium1
- Predicting functional effects of missense variants in voltage-gated sodium and calcium channels. (uni-koeln.de)
Pharmacology2
- Murali Prakriya, PhD, associate professor of Pharmacology, and his team have shown how two channel proteins interact with each other to control the flow of calcium ions into cells and modulate downstream immune responses. (northwestern.edu)
- Our findings show that these calcium channels modulate the maturation of oligodendrocytes in the brain after birth , " said Pablo M. Paez, PhD, an assistant professor in the Department of Pharmacology and Toxicology in the Jacobs School of Medicine and Biomedical Sciences at UB and a research scientist with the Hunter James Kelly Research Institute (HJKRI) at UB, where most of the work was done. (buffalo.edu)
Synaptic4
- Ca2+ can enter the photoreceptor cell via outer segment cyclic nucleotide-gated (CNG) channels or synaptic Ca(v)1.4 L-type voltage-gated calcium channels (VGCC). (uni-muenchen.de)
- Our results show that genetic deletion of the synaptic Ca-v 1.4 L-type VGCCs impairs calpain activation and leads to a short-term preservation of photoreceptors in the rd1 mouse. (uni-muenchen.de)
- The immediately releasable pool of mouse chromaffin cell vesicles is coupled to P/Q-type calcium channels via the synaptic protein interaction site. (uba.ar)
- LTP at these synapses was dependent on postsynaptic calcium entry, similar to synaptic plasticity in other regions of the brain. (nyu.edu)
Diabetes7
- A total of 11 140 patients with type 2 diabetes mellitus were randomly assigned to fixed combination of perindopril-indapamide (4/1.25 mg) or placebo. (elsevier.com)
- The combination of perindopril and indapamide with CCBs seems to provide further protection against mortality in patients with type 2 diabetes mellitus. (elsevier.com)
- Misalignment of circadian rhythms has been evidenced in patients with type 1 diabetes and there is a close relationship between alterations in neuroendocrine sleep architecture, circadian clock oscillations, glucose metabolism, autonomic function, and diurnal profiles of blood pressure and heart rate [ 1 - 5 ]. (intechopen.com)
- They are not that the benefits of cost-lowering the blood circulation of these medications and allow a calcium intake to the body herbs to lower blood pressure Dr. Axe to reduce the risk of diabetes, or kidney disease. (jewishledger.com)
- Regular exercise is linked to lower weight, improved blood pressure and cholesterol levels, enhanced mood, and reduced risk of type 2 diabetes. (sharecare.com)
- For example, in random controlled studies, drinking hibiscus tea or extract lowered systolic and diastolic blood pressure in adults with moderate hypertension and type 2 diabetes. (webmd.com)
- In randomized controlled trials of patients with type 2 diabetes who were largely free of symptomatic HF at baseline, thiazolidinediones were associated with fluid retention and increased rates of HF . (medscape.com)
Gene6
- Evaluation of voltage-dependent calcium channel γ gene families identified several novel potential susceptible genes to schizophrenia. (nih.gov)
- OBJECTIVES: We investigated the gene expression of calcium-handling genes including L-type calcium channel, sarcoplasmic reticular calcium adenosine triphosphatase (Ca 2+ -ATPase), ryanodine receptor, calsequestrin and phospholamban in human atrial fibrillation. (elsevier.com)
- CONCLUSIONS: L-type calcium channel and the sarcoplasmic reticular Ca 2+ -ATPase gene were down-regulated in atrial fibrillation. (elsevier.com)
- In addition, the molecular mechanism of action of a tumor suppressor gene may change depending on the tumor type. (spandidos-publications.com)
- The voltage gated N-type calcium channel (Ca V 2.2) is encoded by the gene CACNA1B. (nanion.de)
- Localization of the gene encoding the α 2 / δ -subunits of the L-type voltage-dependent calcium channel to chromosome 7q and analysis of the segregation of flanking markers in malignant hyperthermia susceptible families. (bvsalud.org)
Currents4
- Muscle depolarization results in large gating currents, but anomolously low calcium flux, which is now explained by the very slow activation of the ionic currents. (bionity.com)
- Surprisingly, however, α-conotoxins Vc1.1, RgIA and PeIA more potently inhibit N-type VGCC currents via a GABA(B) GPCR mechanism in rat sensory neurones. (nih.gov)
- The Dynamite 8 simulates ion channel currents in cells in real-time during patch clamp experiments. (nanion.de)
- Decay of internal calcium concentration due to calcium currents and atpase pump. (ox.ac.uk)
Protein6
- Calcium channel gamma subunits: a functionally diverse protein family. (nih.gov)
- Within coronaviruses too, the viral envelope proteins have been found to act as calcium ion channels within key protein processing organelles like the endoplasmic reticulum Golgi apparatus intermediate compartment (ERGIC). (news-medical.net)
- Using established prediction algorithms, we localized the IDRs in Ca V 3.2 protein and identified several Ca V 3.2iPA candidates that significantly reduced Ca V 3.2 current in HEK293 cells stably expressing human wide-type Ca V 3.2. (lww.com)
- By deleting the ORAI2 protein from the CRAC channel, the scientists showed that the flow of calcium ions into cells was markedly increased. (northwestern.edu)
- The bone marrow (BM) stromal cell antigen-2 (BST-2), also known as tetherin, CD317, PDCA-1, or HM1.24, is a membrane protein overexpressed in several types of tumors and may act as a promising target for cancer treatment via antibody-dependent cellular cytotoxicity. (bvsalud.org)
- Two extra human being FPRs, AZD-3965 IC50 specified FPR2 (www.uniprot.org/uniprot/"type":"entrez-protein","attrs":"text":"P25090″,"term_id":"399504″,"term_text":"P25090″P25090) and FPR3 (www.uniprot.org/uniprot/"type":"entrez-protein","attrs":"text":"P25089″,"term_id":"38258904″,"term_text":"P25089″P25089), had been subsequently cloned by low-stringency hybridization using the FPR1 AZD-3965 IC50 cDNA like a probe. (mdm2-inhibitors.com)
VGCCs3
- Structurally related ω-conotoxins bind directly to and selectively inhibit neuronal (N)-type voltage-gated calcium channels (VGCCs) of nociceptive primary afferent neurones. (nih.gov)
- A series of newly discovered ω-conotoxins from Conus catus, including CVID-F, are potent and selective antagonists of N-type VGCCs. (nih.gov)
- Calcium channels may be generally categorized into two major classes: Voltage-gated calcium channels (VGCCs) and ligand-gated calcium channels (LGCCs). (spandidos-publications.com)
Selectively1
- L-type channels are selectively blocked by dihydropyridines. (bionity.com)
Medications7
- Sometimes, a doctor might prescribe a calcium channel blocker with other high blood pressure medications or with cholesterol-lowering drugs such as statins. (mayoclinic.org)
- Types of blood pressure medications. (mayoclinic.org)
- https://www.heart.org/en/health-topics/high-blood-pressure/changes-you-can-make-to-manage-high-blood-pressure/types-of-blood-pressure-medications. (mayoclinic.org)
- What are the types of osteoarthritis medications? (medicinenet.com)
- The different types of medications prescribed for osteoarthritis help alleviate symptoms and slow the progression of the disease. (medicinenet.com)
- how do i naturally reduce my blood pressure and can make the most benefits to avoid high blood pressure medications but supplements to take for high blood pressure are always types of medicine. (gordanaj.com)
- The SPCs are the first types of the use of these medications that may be found in pregnancy, especially those who isn't likely to be done. (sc-celje.si)
Membrane4
- Furthermore, to simplify the HTS assay and to reduce reagent cost, we stably expressed a membrane-tethered genetic calcium sensor, GCaMP6s-CAAX, that displays superior signal to the background compared to the untethered GCaMP6s or the synthetic Ca 2+ sensor Fluo-4AM. (nanion.de)
- Depolarization of endothelial plasma membrane via high K+ perfusion capable of eliciting cytosolic Ca2+ transients also provoked P-selectin surface expression in alveolar capillaries that was abolished by T-type channel blockade or α1G knockout. (uab.edu)
- Voltage-gated calcium ion channels are found mostly in the cell membrane of excitable cells. (news-medical.net)
- Calcium can then enter the cell and initiates the fusion of the neurotransmitter vesicles with the membrane. (nanion.de)
Neurons7
- 3β-OH exerted prominent enantioselective thermal and mechanical antinociception in healthy rats and reduced T-channel-dependent excitability of primary sensory neurons. (wustl.edu)
- 3β-OH can be used to reduce T-channel-dependent excitability of peripheral sensory neurons as an adjuvant for induction and maintenance of general anaesthesia while improving analgesia and lowering the amount of volatile anaesthetic needed for surgery. (wustl.edu)
- Conventional studies on ion channels have primarily focused on the crucial roles these channels perform in excitatory cell types, including neurons, cardiomyocytes and secretory cells ( 1 ). (spandidos-publications.com)
- The Discovery and Characterization of ML218: A Novel, Centrally Active T-Type Calcium Channel Inhibitor with Robust Effects in STN Neurons and in a Rodent Model of Parkinson's Disease. (vanderbilt.edu)
- On the other hand, methamphetamine(MET) and cocaine produced decreased Kd value of binding with no changes of L-type HVCC subu … More nit expressions in animal cerebral cortex and cerebral cortical neurons. (nii.ac.jp)
- In cerebrocortical neurons, exposure to nifedipine and dantrolene also abolished the alteration of L-type HVCC functions induced by MET and cocaine, while the changes of L-type HVCCs associated with increased expressions of their subunits were not affected by similar treatments. (nii.ac.jp)
- Journal Article] Increase in expression of α1 and α2/δ subunits of L-type high voltage-gated calcium channels after sustained ethanol exposure in cerebral cortical neurons. (nii.ac.jp)
Pulmonary1
- Our findings reveal an intracellular WPb-independent P-selectin pool in pulmonary capillary endothelium, where the regulated P-selectin surface expression is triggered by Ca2+ transients evoked through activation of the α1G T-type channel. (uab.edu)
Nifedipine1
- In conditioned place preference(CPP) test, intraventricular administration of nifedipine and dantrolene abolished increased CPP by MET and enhanced L-type HVCC functions described above. (nii.ac.jp)
Antagonist1
- However, the main ingredient is called a calcium-channel antagonist. (medlineplus.gov)
Antihypertensive agents1
- It can be used alone or in combination with other antihypertensive agents, especially thiazide-type diuretics [see DRUG INTERACTIONS ]. (rxlist.com)
Neuronal2
- Because LTCCs have a broad role in neuronal function and are altered with aging, we examined the effects of E2 on these channels. (jneurosci.org)
- The strong depolarization of neuronal action potentials causes the opening of the channel. (nanion.de)
Neuropathic pain2
- The terpenes camphene and alpha-bisabolol inhibit inflammatory and neuropathic pain via Cav3.2 T-type calcium channels. (painresearchforum.org)
- [5] So it is difficult to select a right drug in different types of neuropathic pain. (ijp-online.com)
Selective1
- T-type voltage-gated Ca 2+ channels have been implicated in many human disorders, and there has been increasing interest in developing highly selective and potent T-type Ca 2+ channel modulators for potential clinical use. (nanion.de)
ATPases1
- In keeping with the central place of calcium in bodily processes, the concentrations of calcium within the cell and within cell organelle compartments are maintained within very tight limits, using various energy-intensive methods including molecular pumps, ion channels and ATPases. (news-medical.net)
Medication1
- Currently it is recommended to continue with the optimal dose for three months, before considering another type of preventive medication. (trymable.com)
LTCC1
- An increase in L-type voltage-gated calcium channel (LTCC) current is a prominent biomarker of brain aging and is believed to contribute to cognitive decline and vulnerability to neuropathologies. (jneurosci.org)
Homeostasis1
- The effect of calcium on these processes varies by location, extent and calcium homeostasis stage ( 26 , 27 ). (spandidos-publications.com)
Analgesics1
- Analgesics include two types, opioid and non-opioid. (medicinenet.com)
CACNA1G2
- Spinocerebellar ataxia (SCA) 42 is caused by a mutation in CACNA1G , which encodes the low voltage-gated calcium channel Ca V 3.1 (T-type). (biomedcentral.com)
- To investigate this possibility, we transfected wild-type and mutant CACNA1G into HEK293T cells and recorded the current using the whole-cell patch-clamp technique. (biomedcentral.com)
Patients2
- Among this bones, it is important to be effective in treating blood pressure, but also really as well as a majority of both calcium intake and in many of these patients. (jewishledger.com)
- L-type calcium channel mutations in Japanese patients with inherited arrhythmias. (cdc.gov)
Ingestion1
- Ingestion of excessive calcium channel blocker (CCB) agents is one of the most potentially lethal prescription drug overdoses. (medscape.com)
Skeletal2
- Transient expression in cultured skeletal muscle myotubes derived from muscular dysgenic mice demonstrates that the BIII channel mediates an omega-conotoxin-sensitive calcium current with kinetics and voltage dependence like those previously reported for whole-cell N-type current. (nih.gov)
- Greally E, Blain A, Blamire AM, MacGowan G, Laval SH, Straub V. Manganese enhanced MRI as a useful in vivo outcome measure in assessing skeletal muscle calcium uptake in mouse models of muscular dystrophy . (ncl.ac.uk)
Modulate1
- A new study published in Nature Communications and co-authored by Northwestern Medicine scientists shows how two proteins of the Ca2+ release-activated Ca2+ (CRAC) channel family interact with each other to control the flow of calcium ions into cells and modulate downstream immune responses. (northwestern.edu)
Irregular heartbeat1
- Metoprolol treats arrhythmia, a type of irregular heartbeat. (druggenius.com)
Ions2
- The scientists showed that ORAI2 slows down or puts a "brake" on ORAI1's ability to conduct calcium ions. (northwestern.edu)
- The authors suggest that their results show how ORAI2 adjusts the amount of calcium ions flowing through ORAI1 channels with both proteins synergizing to control immune responses. (northwestern.edu)
Concentration1
- Analytic results are obtained for the open probability of the channel as well as the auto-correlation and response functions (both for the discrete channel variable and the continuous calcium concentration). (math.ca)
Human atrial1
- CO, Pb++ and SO2 effects on L-type calcium channel and action potential in human atrial myocytes. (udem.edu.co)
Organism1
- The nosocomial epidemiology of this organism is com- methods, performed organism typing by pulsed-field gel plex. (cdc.gov)
Distinct3
- Cell-attached patch recordings, with isotonic barium as the charge carrier, revealed distinct single channels with an average slope conductance of 14.3 pS. (nih.gov)
- Although the structure of the scramblase nhTMEM16 has defined the architecture of the family, it was unknown how a channel has adapted to cope with its distinct functional properties. (uzh.ch)
- Although different cell types establish distinct structures delineating the inside and outside of an embryo, they progressively become specified by the blastocyst stage, when two types of cell lineages are formed: the inner cell mass (ICM) and the trophectoderm (TE). (jbc.org)
Inhibit1
- Omega toxins inhibit the actions of these channels by altering their voltage dependence. (bvsalud.org)
Voltage14
- The L-type calcium channel is a type of voltage-dependent calcium channel . (bionity.com)
- Voltage-dependent calcium channels are composed of five subunits. (nih.gov)
- Low-voltage-activated t-type calcium channels : proceedings from the International Electrophysiology meeting, Montpellier, 21-22 October 1996 / guest editors: Richard W. Tsien, Jean-Paul Clozel, Joël Nargeot. (who.int)
- This genetic defect was predicted to result in an in-frame deletion removing 44 amino acids from the voltage-gated calcium channel Cav2.1. (synergy-munich.de)
- Furthermore, two-electrode voltage-clamp recordings performed from Xenopus laevis oocytes expressing a wild-type versus mutant channel showed that the genetic defect caused a complete loss of channel function. (synergy-munich.de)
- Weisskopf, MG, Bauer, EP & LeDoux, JE 1999, ' L-type voltage-gated calcium channels mediate NMDA-independent associative long-term potentiation at thalamic input synapses to the amygdala ', Journal of Neuroscience , vol. 19, no. 23, pp. 10512-10519. (nyu.edu)
- In this study, we performed whole-cell recordings of GFP-expressing HEK293T cells that expressed wild-type or mutant Ca V 3.1 and investigated the changes in the abnormal shift of voltage dependence of the mutant Ca V 3.1. (biomedcentral.com)
- On the other hand, ZNS did not affect the voltage dependence of wild-type Ca V 3.1. (biomedcentral.com)
- Moreover, efonidipine, another T-type calcium channel blocker, had no effect on tremors in our patient with SCA42 and did not improve the abnormal shift in the voltage dependence of the mutant Ca V 3.1. (biomedcentral.com)
- ZNS is known to have various effects, including impacts on T-type voltage-dependent calcium channel (VDCC) activity [ 8 ]. (biomedcentral.com)
- We also treated the cells with efonidipine, another T-type VDCC blocker that does not affect tremor suppression, and found that efonidipine did not affect the voltage dependence of Ca V 3.1. (biomedcentral.com)
- The work involved the study of voltage-operated calcium channels, which are responsible for initiating many physiological functions. (buffalo.edu)
- Based on these findings, Paez said it appears that in these animals, the inability to develop myelin normally persists into adulthood, suggesting that the expression of voltage-operated calcium channels during the first steps of myelination is essential for the brain's normal development. (buffalo.edu)
- Ca V 2.2 is a high voltage activated calcium channel. (nanion.de)