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.
A class of drugs that act by selective inhibition of calcium influx through cellular membranes.
Voltage-dependent cell membrane glycoproteins selectively permeable to calcium ions. They are categorized as L-, T-, N-, P-, Q-, and R-types based on the activation and inactivation kinetics, ion specificity, and sensitivity to drugs and toxins. The L- and T-types are present throughout the cardiovascular and central nervous systems and the N-, P-, Q-, & R-types are located in neuronal tissue.
A calcium channel blocker with marked vasodilator action. It is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive.
A potent antagonist of CALCIUM CHANNELS that is highly selective for VASCULAR SMOOTH MUSCLE. It is effective in the treatment of chronic stable angina pectoris, hypertension, and congestive cardiac failure.
Pyridine moieties which are partially saturated by the addition of two hydrogen atoms in any position.
Long-lasting voltage-gated CALCIUM CHANNELS found in both excitable and nonexcitable tissue. They are responsible for normal myocardial and vascular smooth muscle contractility. Five subunits (alpha-1, alpha-2, beta, gamma, and delta) make up the L-type channel. The alpha-1 subunit is the binding site for calcium-based antagonists. Dihydropyridine-based calcium antagonists are used as markers for these binding sites.
A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure.
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.
Gated, ion-selective glycoproteins that traverse membranes. The stimulus for ION CHANNEL GATING can be due to a variety of stimuli such as LIGANDS, a TRANSMEMBRANE POTENTIAL DIFFERENCE, mechanical deformation or through INTRACELLULAR SIGNALING PEPTIDES AND PROTEINS.
A class of drugs that stimulate sodium influx through cell membrane channels.
CALCIUM CHANNELS that are concentrated in neural tissue. Omega toxins inhibit the actions of these channels by altering their voltage dependence.
A heterogenous group of transient or low voltage activated type CALCIUM CHANNELS. They are found in cardiac myocyte membranes, the sinoatrial node, Purkinje cells of the heart and the central nervous system.
Signal transduction mechanisms whereby calcium mobilization (from outside the cell or from intracellular storage pools) to the cytoplasm is triggered by external stimuli. Calcium signals are often seen to propagate as waves, oscillations, spikes, sparks, or puffs. The calcium acts as an intracellular messenger by activating calcium-responsive proteins.
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.
Compounds that either stimulate the opening or prevent closure of VOLTAGE-GATED SODIUM CHANNELS.
A class of drugs that act by inhibition of potassium efflux through cell membranes. Blockade of potassium channels prolongs the duration of ACTION POTENTIALS. They are used as ANTI-ARRHYTHMIA AGENTS and VASODILATOR AGENTS.
Heteromultimers of Kir6 channels (the pore portion) and sulfonylurea receptor (the regulatory portion) which affect function of the HEART; PANCREATIC BETA CELLS; and KIDNEY COLLECTING DUCTS. KATP channel blockers include GLIBENCLAMIDE and mitiglinide whereas openers include CROMAKALIM and minoxidil sulfate.
A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.
Potassium channels where the flow of K+ ions into the cell is greater than the outward flow.
CALCIUM CHANNELS located within the PURKINJE CELLS of the cerebellum. They are involved in stimulation-secretion coupling of neurons.
CALCIUM CHANNELS located in the neurons of the brain.
The study of the generation and behavior of electrical charges in living organisms particularly the nervous system and the effects of electricity on living organisms.
A calcium channel blockader with preferential cerebrovascular activity. It has marked cerebrovascular dilating effects and lowers blood pressure.
A calcium channel blocker that is a class IV anti-arrhythmia agent.
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).
CALCIUM CHANNELS located in the neurons of the brain. They are inhibited by the marine snail toxin, omega conotoxin MVIIC.
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.
Cell membrane glycoproteins that form channels to selectively pass chloride ions. Nonselective blockers include FENAMATES; ETHACRYNIC ACID; and TAMOXIFEN.
A guanidine that opens POTASSIUM CHANNELS producing direct peripheral vasodilatation of the ARTERIOLES. It reduces BLOOD PRESSURE and peripheral resistance and produces fluid retention. (Martindale The Extra Pharmacopoeia, 31st ed)
A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.
Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.
An element of the alkaline earth group of metals. It has an atomic symbol Ba, atomic number 56, and atomic weight 138. All of its acid-soluble salts are poisonous.
A neurotoxic peptide, which is a cleavage product (VIa) of the omega-Conotoxin precursor protein contained in venom from the marine snail, CONUS geographus. It is an antagonist of CALCIUM CHANNELS, N-TYPE.
The relationship between the dose of an administered drug and the response of the organism to the drug.
The ability of a substrate to allow the passage of ELECTRONS.
Calcium compounds used as food supplements or in food to supply the body with calcium. Dietary calcium is needed during growth for bone development and for maintenance of skeletal integrity later in life to prevent osteoporosis.
The rate dynamics in chemical or physical systems.
Compounds that either stimulate the opening or prevent closure of EPITHELIAL SODIUM ION CHANNELS.
A family of structurally related neurotoxic peptides from mollusk venom that inhibit voltage-activated entry of calcium into the presynaptic membrane. They selectively inhibit N-, P-, and Q-type calcium channels.
The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM.
Potassium channel whose permeability to ions is extremely sensitive to the transmembrane potential difference. The opening of these channels is induced by the membrane depolarization of the ACTION POTENTIAL.
An element in the alkali group of metals with an atomic symbol K, atomic number 19, and atomic weight 39.10. It is the chief cation in the intracellular fluid of muscle and other cells. Potassium ion is a strong electrolyte that plays a significant role in the regulation of fluid volume and maintenance of the WATER-ELECTROLYTE BALANCE.
Potassium channels whose activation is dependent on intracellular calcium concentrations.
An antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide.
Abrupt changes in the membrane potential that sweep along the CELL MEMBRANE of excitable cells in response to excitation stimuli.
A derivative of the NIACINAMIDE that is structurally combined with an organic nitrate. It is a potassium-channel opener that causes vasodilatation of arterioles and large coronary arteries. Its nitrate-like properties produce venous vasodilation through stimulation of guanylate cyclase.
A potassium-channel opening vasodilator that has been investigated in the management of hypertension. It has also been tried in patients with asthma. (Martindale, The Extra Pharmacopoeia, 30th ed, p352)
A benzimidazoyl-substituted tetraline that selectively binds and inhibits CALCIUM CHANNELS, T-TYPE.
A class of drugs that act by inhibition of sodium influx through cell membranes. Blockade of sodium channels slows the rate and amplitude of initial rapid depolarization, reduces cell excitability, and reduces conduction velocity.
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
The muscle tissue of the HEART. It is composed of striated, involuntary muscle cells (MYOCYTES, CARDIAC) connected to form the contractile pump to generate blood flow.
An autoimmune disease characterized by weakness and fatigability of proximal muscles, particularly of the pelvic girdle, lower extremities, trunk, and shoulder girdle. There is relative sparing of extraocular and bulbar muscles. CARCINOMA, SMALL CELL of the lung is a frequently associated condition, although other malignancies and autoimmune diseases may be associated. Muscular weakness results from impaired impulse transmission at the NEUROMUSCULAR JUNCTION. Presynaptic calcium channel dysfunction leads to a reduced amount of acetylcholine being released in response to stimulation of the nerve. (From Adams et al., Principles of Neurology, 6th ed, pp 1471)
Azoles of one NITROGEN and two double bonds that have aromatic chemical properties.
A subgroup of TRP cation channels that contain 3-4 ANKYRIN REPEAT DOMAINS and a conserved C-terminal domain. Members are highly expressed in the CENTRAL NERVOUS SYSTEM. Selectivity for calcium over sodium ranges from 0.5 to 10.
A neuropeptide toxin from the venom of the funnel web spider, Agelenopsis aperta. It inhibits CALCIUM CHANNELS, P-TYPE by altering the voltage-dependent gating so that very large depolarizations are needed for channel opening. It also inhibits CALCIUM CHANNELS, Q-TYPE.
A benzoate-cevane found in VERATRUM and Schoenocaulon. It activates SODIUM CHANNELS to stay open longer than normal.
Voltage-gated potassium channels whose primary subunits contain six transmembrane segments and form tetramers to create a pore with a voltage sensor. They are related to their founding member, shaker protein, Drosophila.
The species Oryctolagus cuniculus, in the family Leporidae, order LAGOMORPHA. Rabbits are born in burrows, furless, and with eyes and ears closed. In contrast with HARES, rabbits have 22 chromosome pairs.
Elements of limited time intervals, contributing to particular results or situations.
Drugs that bind to and activate dopamine receptors.
A white crystal or crystalline powder used in BUFFERS; FERTILIZERS; and EXPLOSIVES. It can be used to replenish ELECTROLYTES and restore WATER-ELECTROLYTE BALANCE in treating HYPOKALEMIA.
The hollow, muscular organ that maintains the circulation of the blood.
An adenine nucleotide containing three phosphate groups esterified to the sugar moiety. In addition to its crucial roles in metabolism adenosine triphosphate is a neurotransmitter.
A major class of calcium activated potassium channels whose members are voltage-dependent. MaxiK channels are activated by either membrane depolarization or an increase in intracellular Ca(2+). They are key regulators of calcium and electrical signaling in a variety of tissues.
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.
Compounds with a core of fused benzo-pyran rings.
Use of electric potential or currents to elicit biological responses.
The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.
Female germ cells derived from OOGONIA and termed OOCYTES when they enter MEIOSIS. The primary oocytes begin meiosis but are arrested at the diplotene state until OVULATION at PUBERTY to give rise to haploid secondary oocytes or ova (OVUM).
A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.
A subgroup of TRP cation channels named after vanilloid receptor. They are very sensitive to TEMPERATURE and hot spicy food and CAPSAICIN. They have the TRP domain and ANKYRIN repeats. Selectivity for CALCIUM over SODIUM ranges from 3 to 100 fold.
Established cell cultures that have the potential to propagate indefinitely.
Carbonic acid calcium salt (CaCO3). An odorless, tasteless powder or crystal that occurs in nature. It is used therapeutically as a phosphate buffer in hemodialysis patients and as a calcium supplement.
The commonest and widest ranging species of the clawed "frog" (Xenopus) in Africa. This species is used extensively in research. There is now a significant population in California derived from escaped laboratory animals.
A subgroup of cyclic nucleotide-regulated ION CHANNELS within the superfamily of pore-loop cation channels. They are expressed in OLFACTORY NERVE cilia and in PHOTORECEPTOR CELLS and some PLANTS.
A salt used to replenish calcium levels, as an acid-producing diuretic, and as an antidote for magnesium poisoning.
Cell membrane glycoproteins that are selectively permeable to potassium ions. At least eight major groups of K channels exist and they are made up of dozens of different subunits.
Contractile activity of the MYOCARDIUM.
A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents.
The nonstriated involuntary muscle tissue of blood vessels.
A tetrameric calcium release channel in the SARCOPLASMIC RETICULUM membrane of SMOOTH MUSCLE CELLS, acting oppositely to SARCOPLASMIC RETICULUM CALCIUM-TRANSPORTING ATPASES. It is important in skeletal and cardiac excitation-contraction coupling and studied by using RYANODINE. Abnormalities are implicated in CARDIAC ARRHYTHMIAS and MUSCULAR DISEASES.
A methylpyrrole-carboxylate from RYANIA that disrupts the RYANODINE RECEPTOR CALCIUM RELEASE CHANNEL to modify CALCIUM release from SARCOPLASMIC RETICULUM resulting in alteration of MUSCLE CONTRACTION. It was previously used in INSECTICIDES. It is used experimentally in conjunction with THAPSIGARGIN and other inhibitors of CALCIUM ATPASE uptake of calcium into SARCOPLASMIC RETICULUM.
A subgroup of TRP cation channels named after melastatin protein. They have the TRP domain but lack ANKYRIN repeats. Enzyme domains in the C-terminus leads to them being called chanzymes.
Venoms of arthropods of the order Araneida of the ARACHNIDA. The venoms usually contain several protein fractions, including ENZYMES, hemolytic, neurolytic, and other TOXINS, BIOLOGICAL.
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.
A family of proton-gated sodium channels that are primarily expressed in neuronal tissue. They are AMILORIDE-sensitive and are implicated in the signaling of a variety of neurological stimuli, most notably that of pain in response to acidic conditions.

Melatonin inhibits release of luteinizing hormone (LH) via decrease of [Ca2+]i and cyclic AMP. (1/640)

The role of [Ca2+]i and cAMP in transduction of the melatonin inhibitory effect on GnRH-induced LH release from neonatal rat gonadotrophs has been studied, because melatonin inhibits the increase of both intracellular messengers. Treatments increasing Ca2+ influx (S(-) Bay K8644 or KCI) or cAMP concentration (8-bromo-cAMP or 3-isobutyl-1-methylxanthine) potentiated the GnRH-induced LH release and partially diminished the inhibitory effect of melatonin. Combination of the treatments increasing cAMP and calcium concentrations blocked completely the melatonin inhibition of LH release. The combined treatment with 8-bromo-cAMP and S(-) Bay K8644 also blocked the melatonin inhibition of GnRH-induced [Ca2+]i increase in 89 % of the gonadotrophs, while any of the treatments alone blocked the melatonin effect in about 25 % of these cells. These observations suggest that a cAMP-dependent pathway is involved in regulation of Ca2+ influx by melatonin and melatonin inhibition of LH release may be mediated by the decrease of both messengers.  (+info)

Intracellular Ca2+ concentrations in cultured chicken photoreceptor cells: sustained elevation in depolarized cells and the role of dihydropyridine-sensitive Ca2+ channels. (2/640)

PURPOSE: Retinal photoreceptor cells are tonically depolarized in darkness. Ca2+ influx in darkness plays a critical role in the regulation of neurotransmitter release and melatonin synthesis in these sensory cells. The purpose of the present study was to examine the dynamic changes of intracellular Ca2+ concentrations ([Ca2+]in ) in response to a tonic depolarizing stimulus and to determine the role of dihydropyridine-sensitive calcium channels in the response. METHODS: Photoreceptor cells were prepared from embryonic chick retina and cultured for 6-12 days. Cells were depolarized by exposure to 35 mM extracellular K+. [Ca2+]in of individual photoreceptor cell bodies/synaptic terminals was determined by ratiometric fura-2 image analysis. RESULTS: Chemical depolarization with 35 mM [K+]out greatly increased [Ca2+]in of inner segment/synaptic terminal regions of photoreceptors. The increase usually reached a plateau after the first few minutes of stimulation and was sustained for prolonged periods (>2 h) in the presence of high K+. When the extracellular K+ concentration was reduced, the [Ca2+]in rapidly returned to the basal level. Substitution of 1 mM CoCl2 for CaCl2 in the superfusion medium rapidly and reversibly reduced the [Ca2+]in of depolarized photoreceptor cells. Antagonists of L-type Ca2+ channels, nitrendipine and nifedipine, inhibited the K+-evoked increase of [Ca2+]in. Bay K 8644, a dihydropyridine Ca2+ channel agonist, potentiated the increase of [Ca2+]in elicited by high K+. In some cells, Bay K 8644 alone increased [Ca2+]in under basal conditions. CONCLUSIONS: The increase of [Ca2+]in elicited by depolarization with 35 mM extracellular K+ is due to influx of calcium through the dihydropyridine-sensitive voltage-gated channels. Intracellular [Ca2+] remains elevated for extended periods of time during tonic depolarization. This sustained response requires continuous Ca2+ channel activity.  (+info)

Voltage inactivation of Ca2+ entry and secretion associated with N- and P/Q-type but not L-type Ca2+ channels of bovine chromaffin cells. (3/640)

1. In this study we pose the question of why the bovine adrenal medullary chromaffin cell needs various subtypes (L, N, P, Q) of the neuronal high-voltage activated Ca2+ channels to control a given physiological function, i.e. the exocytotic release of catecholamines. One plausible hypothesis is that Ca2+ channel subtypes undergo different patterns of inactivation during cell depolarization. 2. The net Ca2+ uptake (measured using 45Ca2+) into hyperpolarized cells (bathed in a nominally Ca2+-free solution containing 1.2 mM K+) after application of a Ca2+ pulse (5 s exposure to 100 mM K+ and 2 mM Ca2+), amounted to 0.65 +/- 0.02 fmol cell-1; in depolarized cells (bathed in nominally Ca2+-free solution containing 100 mM K+) the net Ca2+ uptake was 0.16 +/- 0.01 fmol cell-1. 3. This was paralleled by a dramatic reduction of the increase in the cytosolic Ca2+ concentration, [Ca2+]i, caused by Ca2+ pulses applied to fura-2-loaded single cells, from 1181 +/- 104 nM in hyperpolarized cells to 115 +/- 9 nM in depolarized cells. 4. A similar decrease was observed when studying catecholamine release. Secretion was decreased when K+ concentration was increased from 1.2 to 100 mM; the Ca2+ pulse caused, when comparing the extreme conditions, the secretion of 807 +/- 35 nA of catecholamines in hyperpolarized cells and 220 +/- 19 nA in depolarized cells. 5. The inactivation by depolarization of Ca2+ entry and secretion occluded the blocking effects of combined omega-conotoxin GVIA (1 microM) and omega-agatoxin IVA (2 microM), thus suggesting that depolarization caused a selective inactivation of the N- and P/Q-type Ca2+ channels. 6. This was strengthened by two additional findings: (i) nifedipine (3 microM), an L-type Ca2+ channel blocker, suppressed the fraction of Ca2+ entry (24 %) and secretion (27 %) left unblocked by depolarization; (ii) FPL64176 (3 microM), an L-type Ca2+ channel 'activator', dramatically enhanced the entry of Ca2+ and the secretory response in depolarized cells. 7. In voltage-clamped cells, switching the holding potential from -80 to -40 mV promoted the loss of 80 % of the whole-cell inward Ca2+ channel current carried by 10 mM Ba2+ (IBa). The residual current was blocked by 80 % upon addition of 3 microM nifedipine and dramatically enhanced by 3 microM FPL64176. 8. Thus, it seems that the N- and P/Q-subtypes of calcium channels are more prone to inactivation at depolarizing voltages than the L-subtype. We propose that this different inactivation might occur physiologically during different patterns of action potential firing, triggered by endogenously released acetylcholine under various stressful conditions.  (+info)

A new scorpion toxin (BmK-PL) stimulates Ca2+-release channel activity of the skeletal-muscle ryanodine receptor by an indirect mechanism. (4/640)

A peptide toxin isolated from the Chinese scorpion Buthus martensi Karsch (BmK-PL) stimulated Ca2+-release channel activity in both triad membranes and reconstituted ryanodine receptors partially purified from rabbit skeletal muscle. In [3H]ryanodine binding experiments, the toxin increased the affinity of ryanodine for the receptor, from a Kd of 24.3 nM to 2.9 nM, which is an enhancement similar to that seen with known receptor activators, such as ATP and high concentrations of KCl. In contrast, toxin enhancement was not observed with purified receptors, although intrinsic binding activity and stimulation by the conventional receptor activators were retained. In single channel recordings of Ca2+-release activity, the toxin increased the open channel probability (Po) from 0.019 to 0.043 (226% of control) in triad preparations. Further toxin enhancement of Po from 0.07 to 0.37 (529% of control) was observed using partially-purified receptors in the presence of ATP. When purified receptors were assayed in the presence of ATP, however, they showed a high value of Po (0.33) and no further increase was observed following application of the toxin. Results derived from two different experimental methods consistently suggest that a molecule(s) required for toxin-induced enhancement is absent from the purified receptor preparation. Western blot analysis of receptors prepared using three different protocols showed that triadin was missing from the purified receptor preparation. The scorpion toxin minimally enhanced Ca2+-release channel activity of cardiac preparations. From these results, we conclude that the toxin preferentially increases the activity of skeletal-muscle ryanodine receptors by an indirect mechanism, possibly binding to associated protein molecule(s). Triadin is a strong candidate for such a molecule.  (+info)

BAY K 8644 modifies Ca2+ cross signaling between DHP and ryanodine receptors in rat ventricular myocytes. (5/640)

The amplification factor of dihydropyridine (DHP)/ryanodine receptors was defined as the amount of Ca2+ released from the sarcoplasmic reticulum (SR) relative to the influx of Ca2+ through L-type Ca2+ channels in rat ventricular myocytes. The amplification factor showed steep voltage dependence at potentials negative to -10 mV but was less dependent on voltage at potentials positive to this value. In cells dialyzed with 0.2 mM cAMP in addition to 2 mM fura 2, the Ca2+-channel agonist (-)-BAY K 8644 enhanced Ca2+-channel current (ICa), shifted the activation curve by -10 mV, and significantly delayed its inactivation. Surprisingly, BAY K 8644 reduced the amplification factor by 50% at all potentials, even though the caffeine-releasable Ca2+ stores were mostly intact at holding potentials of -90 mV. In contrast, brief elevation of extracellular Ca2+ activity from 2 to 10 mM enhanced both ICa and intracellular Ca2+ transients in the absence or presence of BAY K 8644 but had no significant effect on the amplification factor. BAY K 8644 abolished the direct dependence of the rate of inactivation of ICa on the release of Ca2+ from the SR. These findings suggest that the gain of the Ca2+-induced Ca2+ release in cardiac myocytes is regulated by the gating kinetics of cardiac L-type Ca2+ channels via local exchange of Ca2+ signals between DHP and ryanodine receptors and that BAY K 8644 suppresses the amplification factor through attenuation of the Ca2+-dependent inactivation of Ca2+ channels.  (+info)

Inositol 1,3,4,5-tetrakisphosphate enhances long-term potentiation by regulating Ca2+ entry in rat hippocampus. (6/640)

1. The effect of inositol 1,3,4,5-tetrakisphosphate (InsP4) on long-term potentiation (LTP) was investigated in the CA1 region of rat hippocampal slices. Intracellular application of InsP4 and EPSP recordings were carried out using the whole-cell configuration. 2. Induction of LTP in the presence of InsP4 (100 microM) resulted in a substantial enhancement of the LTP magnitude compared with control potentiation. Using an intrapipette perfusion system, it was established that application of InsP4 was required during induction of potentiation for this enhancement to occur. An enhancement of LTP was not observed if a non-metabolizable inositol 1,4,5-trisphosphate (InsP3) analogue (2,3-dideoxy-1,4,5-trisphosphate, 100 microM) was applied intracellularly. 3. Current-voltage relations of NMDA receptor-mediated EPSCs were not altered by InsP4 application. The presence of InsP4 was slightly effective in relieving a D-(-)-2-amino-5-phosphonopentanoic acid (D-APV)-induced block of LTP. 4. The peak current amplitude of voltage-gated calcium channels (VGCCs) was increased by InsP4. omega-Conotoxin GVIA inhibited the InsP4-induced LTP facilitation. 5. These data indicate that InsP4 can modify the extracellular Ca2+ entry through upregulation of VGCCs, which may in turn contribute to the observed enhancement of LTP induced by InsP4. 6. To investigate the possible involvement of intracellular Ca2+ release in the facilitatory effect of InsP4 on LTP, different inhibitors of the endoplasmic reticulum-dependent Ca2+ release were applied (heparin, ryanodine, cyclopiazonic acid). The results suggest that InsP4 activates postsynaptic InsP3-dependent Ca2+ release which normally does not contribute to the calcium-induced calcium release-dependent LTP.  (+info)

Differentially expressed genes in C6.9 glioma cells during vitamin D-induced cell death program. (7/640)

C6.9 rat glioma cells undergo a cell death program when exposed to 1, 25-dihydroxyvitamin D3 (1,25-D3). As a global analytical approach, we have investigated gene expression in C6.9 engaged in this cell death program using differential screening of a rat brain cDNA library with probes derived from control and 1,25-D3-treated cells. Using this methodology we report the isolation of 61 differentially expressed cDNAs. Forty-seven cDNAs correspond to genes already characterized in rat cells or tissues. Seven cDNAs are homologous to yeast, mouse or human genes and seven are not related to known genes. Some of the characterized genes have been reported to be differentially expressed following induction of programmed cell death. These include PMP22/gas3, MGP and beta-tubulin. For the first time, we also show a cell death program induced up-regulation of the c-myc associated primary response gene CRP, and of the proteasome RN3 subunit and TCTP/mortalin genes. Another interesting feature of this 1,25-D3 induced-cell death program is the down-regulated expression of transcripts for the microtubule motor dynein heavy chain/MAP 1C and of the calcium-binding S100beta protein. Finally 15 upregulated cDNAs encode ribosomal proteins suggesting a possible involvement of the translational apparatus in this cell program. Alternatively, these ribosomal protein genes could be up-regulated in response to altered rates of cellular metabolism, as has been demonstrated for most of the other isolated genes which encode proteins involved in metabolic pathways. Thus, this study presents to our knowledge the first characterization of genes which are differentially expressed during a cell death program induced by 1, 25-D3. Therefore, this data provides new information on the fundamental mechanisms which participate in the antineoplastic effects of 1,25-D3 and on the machinery of a cell death program in a glioma cell line.  (+info)

Bicarbonate and chloride secretion in Calu-3 human airway epithelial cells. (8/640)

Serous cells are the predominant site of cystic fibrosis transmembrane conductance regulator expression in the airways, and they make a significant contribution to the volume, composition, and consistency of the submucosal gland secretions. We have employed the human airway serous cell line Calu-3 as a model system to investigate the mechanisms of serous cell anion secretion. Forskolin-stimulated Calu-3 cells secrete HCO-3 by a Cl-offdependent, serosal Na+-dependent, serosal bumetanide-insensitive, and serosal 4,4'-dinitrostilben-2,2'-disulfonic acid (DNDS)-sensitive, electrogenic mechanism as judged by transepithelial currents, isotopic fluxes, and the results of ion substitution, pharmacology, and pH studies. Similar studies revealed that stimulation of Calu-3 cells with 1-ethyl-2-benzimidazolinone (1-EBIO), an activator of basolateral membrane Ca2+-activated K+ channels, reduced HCO-3 secretion and caused the secretion of Cl- by a bumetanide-sensitive, electrogenic mechanism. Nystatin permeabilization of Calu-3 monolayers demonstrated 1-EBIO activated a charybdotoxin- and clotrimazole- inhibited basolateral membrane K+ current. Patch-clamp studies confirmed the presence of an intermediate conductance inwardly rectified K+ channel with this pharmacological profile. We propose that hyperpolarization of the basolateral membrane voltage elicits a switch from HCO-3 secretion to Cl- secretion because the uptake of HCO-3 across the basolateral membrane is mediated by a 4,4 '-dinitrostilben-2,2'-disulfonic acid (DNDS)-sensitive Na+:HCO-3 cotransporter. Since the stoichiometry reported for Na+:HCO-3 cotransport is 1:2 or 1:3, hyperpolarization of the basolateral membrane potential by 1-EBIO would inhibit HCO-3 entry and favor the secretion of Cl-. Therefore, differential regulation of the basolateral membrane K+ conductance by secretory agonists could provide a means of stimulating HCO-3 and Cl- secretion. In this context, cystic fibrosis transmembrane conductance regulator could serve as both a HCO-3 and a Cl- channel, mediating the apical membrane exit of either anion depending on basolateral membrane anion entry mechanisms and the driving forces that prevail. If these results with Calu-3 cells accurately reflect the transport properties of native submucosal gland serous cells, then HCO-3 secretion in the human airways warrants greater attention.  (+info)

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In addition to the shift in the I-V relationship for L-type currents of R163C Het and Hom myotubes, we found that this MH mutation caused an increased responsiveness to the dihydropyridine agonist ±Bay K 8644. In particular, L-type currents of MHS R163C myotubes were potentiated to a greater degree (Hom , Het) than WT myotubes (Fig. 4). This observation suggests that one of the retrograde effects of R163C mutation on the L-type channel activity of the DHPR is to facilitate entry of the channel into the long-open gating state (i.e., mode 2; Nowycky et al., 1985), which might explain the enhanced potentiation by ±Bay K 8644. Interestingly, Bay K 8644 enhances pharmacologically (halothane or isofluorane) induced contractures in both swine and human MHS muscle (Williams et al., 1991; Adnet et al., 1992), consistent with the idea that altered L-type current may contribute to the pathogenesis of this disease.. Compared with previous reports on the inactivation of L-type current in normal human ...
The synthesis of a series of adenophostin A analogues modified at C-6 and C-2 of adenine is described. The target compounds were synthesized by a convergent route involving a modified Vorbrüggen condensation of either 6-chloropurine or 2,6-dichloropurine with a protected disaccharide, yielding two versatile intermediates capable of undergoing substitution with a range of nucleophiles. The new analogues showed a range of abilities to mobilize Ca(2+) from the intracellular stores of permeabilized hepatocytes and are among the first totally synthetic compounds to approach the activity of adenophostin A. In agreement with the biological results, docking studies of adenophostin A using the recently reported X-ray crystal structure of the type 1 Ins(1,4,5)P(3) receptor binding core suggested that, in likely binding modes of adenophostin A, the area around N(6) may be relatively open, identifying this region of the adenophostin A molecule as a promising target for further elaboration. The docking results also
The IUPHAR/BPS Guide to Pharmacology. adenophostin A ligand page. Quantitative data and detailed annnotation of the targets of licensed and experimental drugs.
Page 1 of 7 - Comparing FPL-53 and CaF2 - posted in Refractors : Many discussions on Cloudy Nights focus on Which is better?. An occasional topic is how fluor-crown glass, FPL53, compares to synthetic crystal fluorite, CaF2. Fortunately, Vladimir Sacek offers examples at http://www.telescope...po_examples.htm - nicely answering the question. Design #15 is for a FPL53 doublet (ZKN7 and FPL53) and design #16 is for a CaF2 doublet (K5 and CaF2), allowing for an easy comparison. Both a...
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With PDEs inactivated by IBMX, we assume that there are two pathways for inhibition of ICa(L) by cGMP/PKG, namely, phosphorylation of the α1c subunit that antagonizes the stimulant effect of cAMP/PKA and/or activation of PP that dephosphorylates the α1c subunit. Can 8-Br-cGMP or CCh suppress Ca2+ current through L-type channels in the presence of ATPγS, which allows kinases to thiophosphorylate substrates that resist phosphatase action? Irreversible suppression by 8-Br-cGMP would indicate that thiophosphorylation of the channel had occurred at a site different from that acted upon by cAMP/PKA (Méry et al., 1991; Sumii and Sperelakis, 1995). Alternatively, failure of 8-Br-cGMP to suppress ICa(L) in ATPγS would indicate that the thiophosphorylated channel was resistant to phosphatase. Our results are consistent with the PP hypothesis for inhibition by cGMP of current through L-type channels in guinea pig ventricular myocytes.. Neurotransmitter regulation of ICa(L) by reversible ...
Calcitriol ,Calcitriol manufacturer,Calcitriol CAS No 32222-06-3,Calcitriol Molecular Formula C27H44O3,Calcitriol Synonyms (1R,3S)-5-[2-[(1R,3aR,7aS)-1-[(2R)-6-hydroxy-6-methyl-heptan-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H- inden-4-ylidene]ethylidene]-4-methylidene-cyclohexane-1,3-diol,Calcitriol Molecular weight 416.64 g/mol,Calcitriol manufacturing by A.S.Joshi & Company
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The glyconucleotides adenophostin A and B are the most potent known agonists at type 1 inositol trisphosphate [Ins(1,4,5)P3] receptors, although their stuctures differ markedly from that of Ins(1,4,5)P3. Equilibrium competition binding with [3H]Ins(1,4,5)P3 and unidirectional 45Ca2+ flux measurements were used to examine the effects of adenophostin A in hepatocytes, which express predominantly type 2 Ins(1,4,5)P3 receptors. Both Ins(1,4,5)P3 (Kd = 8.65 +/- 0.98 nM) and adenophostin A (Kd = 0.87 +/- 0.20 nM) bound to a single class of [3H]Ins(1,4,5)P3-binding site and each fully mobilized the same intracellular Ca2+ pool; although, adenophostin A (EC50 = 10.9 +/- 0.7 nM) was more potent than Ins(1,4,5)P3 (EC50 = 153 +/- 11 nM). Working on the assumption that it is the phosphorylated glucose component of the adenophostins that mimics the critical features of Ins(1,4,5)P3, we synthesized various phosphorylated disaccharide analogs containing this structure. The novel disaccharide-based analogs, sucrose 3,4
1,4-Dihydropyridines (DHP), the most commonly used antihypertensives, function by inhibiting the L-type voltage-gated Ca 2+ (Ca v ) channels. DHP compounds exhibit chirality-specific antagonistic or agonistic effects. The structure of rabbit Ca v 1.1 bound to an achiral drug nifedipine reveals the general binding mode for DHP drugs, but the molecular basis for chiral specificity remains elusive. Here, we report five cryo-EM structures of nanodisc-embedded Ca v 1.1 in the presence of the bestselling drug amlodipine, a DHP antagonist ( R )-(+)-Bay K8644, and a titration of its agonistic enantiomer ( S )-(-)-Bay K8644 at resolutions of 2.9-3.4 Å. The amlodipine-bound structure reveals the molecular basis for the high efficacy of the drug. All structures with the addition of the Bay K8644 enantiomers exhibit similar inactivated conformations, suggesting that ( S )-(-)-Bay K8644, when acting as an agonist, is insufficient to lock the activated state of the channel for a prolonged duration ...
Adenophostin A is a glyconucleotide natural product with the highest known potency for the D-myo-inositol 1,4,5-trisphosphate receptor. Using synthetic adenophostin A we have investigated the macroscopic and microscopic protonation process of this compound by performing (31)P NMR, (1)H NMR, and potentiometric titration experiments. The logarithms of the first to the fourth stepwise protonation constants are, respectively, log K(1) = 8.48, log K(2) = 6.20, log K(3) = 4.96, and log K(4) = 3.80. The latter constant refers to the protonation equilibrium involving the N1 adenine nitrogen. From the microconstants the protonation fractions of each individual phosphate group can be calculated. Remarkably, the ionization state of the phosphates of adenophostin A at near physiological pH is very similar to those of inositol 1,4,5-trisphosphate, indicating that differences in phosphate charge cannot account for the high potency of this molecule. The analysis of the (1)H chemical shifts vs pH provided complementary
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The use of TIR-FM enabled us to visualize the steady state and calcium-induced submembrane movement, docking, and fusion of intracellular compartments to the plasma membrane. We found that calcium ionophore A23187 induced increase in calcium did not cause exocytosis of Golgi, ER, early, or late endosomes, and did not lead to an increase in exocytosis of post-Golgi vesicles. The absence of an effect of calcium on exocytosis of early endosomes is in agreement with the previously reported absence of an affect of calcium increase on transferrin recycling (Rodriguez et al., 1997). On the other hand, absence of an effect of calcium on exocytosis of Golgi and Golgi-derived vesicles is contrary to the proposed role of Golgi derived compartments in Ca2+-induced exocytosis in fibroblasts (Togo et al., 1999).. An increase in calcium caused either by the calcium ionophore A23187 or by the IP3-dependent calcium channel agonists thrombin and bombesin, led to exocytosis of lysosomes. Using dual-color live-cell ...
TY - JOUR. T1 - Hydrochlorothiazide: An hyperglycaemia-inducing agent and K-ATP channel agonist in human beta-cells and clonal insulin-secreting cells.. AU - Barnes, PD. AU - OBrien, RE. AU - Abdel-Wahab, Yasser. AU - Cosgrove, KE. AU - Flatt, Peter. AU - Dunne, MJ. PY - 1999/8. Y1 - 1999/8. M3 - Article. VL - 42. SP - 482. JO - Diabetologia. JF - Diabetologia. SN - 0012-186X. IS - Suppl.. ER - ...
4SC was developing small molecule openers of the human Ca2+-activated and voltage-dependent potassium channel BKCa as potential therapeutics for the treatment
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This is because adrenergic stimulation by agonists results in normal calcium channel regulation. If these adrenergic receptors ... Kerns, William (2007). "Management of β-Adrenergic Blocker and Calcium Channel Antagonist Toxicity". Emergency Medicine Clinics ... there will be an excess in calcium channel inhibition, which causes most of these problems. Adrenergic receptor Alpha blocker ... A receptor's agonist does not bind to its allosteric binding site. The binding of a non-competitive antagonist is irreversible ...
... is a chemical compound that functions as a calcium channel agonist. Bay K8644 is used primarily as a biochemical ... calcium channels (L-Type). It is the first positive inotropic agent shown to act specifically and directly on calcium channels ... that enhances calcium currents in guinea pig and calf myocardial cells. A new type of positive inotropic agent". Circ Res. 56 ( ...
Bhugra P, Gulati OD (1996). "Interaction of calcium channel blockers with different agonists in aorta from normal and diseased ... Bhugra P, Gulati OD (2001). "Influence of chronic treatment of rats with isoprenaline and calcium channel blockers on response ...
Monoterpenoids also induce agonist-specific desensitization of TRPV3 channels in a calcium-independent manner. Resolvin E1 ( ... 2009). "Monoterpenoids Induce Agonist-Specific Desensitization of Transient Receptor Potential Vanilloid-3 (TRPV3) ion Channels ... Farnesyl pyrophosphate is an endogenous agonist of TRPV3, while incensole acetate from frankincense also acts as an agonist at ... and the two encoded proteins are thought to associate with each other to form heteromeric channels. The TRPV3 channel has wide ...
In the visual system, cannabinoids agonist induce a dose dependent modulation of calcium, chloride and potassium channels. This ... Negatively to D-type outward potassium channels Negatively to N-type and P/Q-type calcium channels. The CB1 receptor is encoded ... including the positively influenced inwardly rectifying potassium channels (=Kir or IRK), and calcium channels, which are ... The inverse agonist MK-9470 makes it possible to produce in vivo images of the distribution of CB1 receptors in the human brain ...
... calcium-channel blockers and beta-adrenergic agonists, may increase the risk. Anesthesia: General anesthetics during surgery ... Urologic Emergencies Archived 2010-03-10 at the Wayback Machine Urology Channel portal. 2010-02-10 Özveren, B; Keskin, S (2016 ... Medications: Anticholinergics and medications with anticholinergic properties, alpha-adrenergic agonists, opiates, nonsteroidal ...
... calcium channel blockers, PPAR-γ agonists, curcuminoids, ethanol, NMDA antagonists, caffeine. In addition to traditional ... Langham, J; C Goldfrad; G Teasdale; D Shaw; K Rowan (2003). "Calcium channel blockers for acute traumatic brain injury" (PDF). ... Forsyth, R. J.; Jayamoni, B.; Paine, T. C. (October 18, 2006). "Monoaminergic agonists for acute traumatic brain injury". The ... Yi, Jae-Hyuk; Seung-Won Park; Nathaniel Brooks; Bradley T. Lang; Raghu Vemuganti (2008). "PPARγ agonist rosiglitazone is ...
... a putative calcium channel agonist isolated from a marine dinoflagellate". Journal of Biochemistry. 104 (2): 184-7. doi:10.1093 ... Inns RH, Tuckwell NJ, Bright JE, Marrs TC (July 1990). "Histochemical demonstration of calcium accumulation in muscle fibres ...
Alpha/Beta Adrenergic Agonists, Calcium Channel Blockers, Anticoagulants, Cardiovascular, Opioid Analgesics". emedicine. ... Cite journal requires ,journal= (help) Schade R, Andersohn F, Suissa S, Haverkamp W, Garbe E (2007). "Dopamine agonists and the ... calcium blockers and avoiding very strenuous activity. As of 2007, the American Heart Association no longer recommends ... "Valvular heart disease and the use of dopamine agonists for Parkinson's disease". N. Engl. J. Med. 356 (1): 39-46. doi:10.1056/ ...
... calcium channel agonists MeSH D27.505.519.562.249 - calcium channel blockers MeSH D27.505.519.562.374 - ionophores MeSH D27.505 ... calcium channel agonists MeSH D27.505.954.411.793.610 - nasal decongestants MeSH D27.505.954.411.918 - vasodilator agents MeSH ... calcium channel blockers MeSH D27.505.954.411.207 - cardioplegic solutions MeSH D27.505.954.411.222 - cardiotonic agents MeSH ... 500 - potassium channel blockers MeSH D27.505.519.562.750 - sodium channel blockers MeSH D27.505.519.562.812 - sodium chloride ...
... dopamine agonists, TNF inhibitors, calcium channel blockers (especially verapamil and diltiazem), salbutamol, and tamsulosin. ... Certain calcium channel blockers, such as diltiazem and verapamil, are known to decrease the force with which the heart ejects ... Tetrandrine can lead to low blood pressure through inhibition of L-type calcium channels. Yohimbine can exacerbate heart ... alpha-2 adrenergic receptor agonists, minoxidil, itraconazole, cilostazol, anagrelide, stimulants (e.g., methylphenidate), ...
... calcium channels. Depolarization may be brought about by stretching of the cell, agonist-binding its G protein-coupled receptor ... opening of the L-type calcium channel permits influx of calcium into the cell. The calcium binds to the calcium release ... High-voltage-gated calcium channels include the neural N-type channel blocked by ω-conotoxinGVIA, the R-type channel (R stands ... Voltage-gated calcium channels (VGCCs), also known as voltage-dependent calcium channels (VDCCs), are a group of voltage-gated ...
... calcium channels.[13][14] Depolarization may be brought about by stretching of the cell, agonist-binding its G protein-coupled ... P-type calcium channel ("Purkinje") /Q-type calcium channel. HVA (high voltage activated). Cav2.1 (CACNA1A). α2δ, β, possibly γ ... Voltage-gated calcium channels (VGCCs), also known as voltage-dependent calcium channels (VDCCs), are a group of voltage-gated ... opening of the L-type calcium channel permits influx of calcium into the cell. The calcium binds to the calcium release ...
Acetylcholine Digoxin The non-dihydropyridine calcium channel blockers diltiazem and verapamil Most Adrenergic agonists ...
Calcium channel blockersEdit. Calcium channel blockers block the entry of calcium into muscle cells in artery walls. ... Alpha-2 adrenergic receptor agonistsEdit. Central alpha agonists lower blood pressure by stimulating alpha-receptors in the ... JNC8[who?] recommends calcium channel blockers to be a first-line treatment either as monotherapy or in combination with ... Calcium kidney stones" N Engl J Med 2010;363(10) 954-963. Worcester, Elaine M.; Coe, Fredric L. (2010). "Calcium Kidney Stones" ...
In addition, β2 agonists open large conductance calcium-activated potassium channels and thereby tend to hyperpolarize airway ... β2 (beta2) adrenergic receptor agonists, also known as adrenergic β2 receptor agonists, are a class of drugs that act on the β2 ... Like other β adrenergic agonists, they cause smooth muscle relaxation. β2 adrenergic agonists' effects on smooth muscle cause ... Discovery and development of β2 agonists Proskocil, Becky J.; Fryer, Allison D. (1 November 2005). "β2-Agonist and ...
β1 agonists stimulate adenylyl cyclase activity and opening of calcium channel (cardiac stimulants; used to treat cardiogenic ... Prenalterol Xamoterol β2 agonists stimulate adenylyl cyclase activity and closing of calcium channel (smooth muscle relaxants; ... Beta adrenergic agonists or beta agonists are medications that relax muscles of the airways, causing widening of the airways ... In general, pure beta-adrenergic agonists have the opposite function of beta blockers: beta-adrenoreceptor agonist ligands ...
... calcium channel blockers, diuretics, sedatives, alpha-adrenergic agonist, alpha 1 antagonists). Urinary symptoms may include ... For urinary retention, cholinergics (muscarinic agonists) like bethanechol can improve the squeezing ability of the bladder. ...
... is a chemical compound which acts as an "agonist" (i.e. channel opener) of the TRPML family of calcium channels. It has ... February 2018). "Robust lysosomal calcium signaling through channel TRPML1 is impaired by lysosomal lipid accumulation". FASEB ... Feng X, Xiong J, Lu Y, Xia X, Zhu MX (December 2014). "Differential mechanisms of action of the mucolipin synthetic agonist, ML ... on insect TRPML and mammalian TRPML1". Cell Calcium. 56 (6): 446-56. doi:10.1016/j.ceca.2014.09.004. PMC 4252876. PMID 25266962 ...
... and other β2 receptor agonists also increase the conductance of channels sensitive to calcium and potassium ions, ... While preferred over agents such as atosiban and ritodrine, its role has largely been replaced by the calcium channel blocker ... It is a short-acting β2 adrenergic receptor agonist which works by causing relaxation of airway smooth muscle. It is used to ... The 1972 Munich Olympics were the first Olympics where anti-doping measures were deployed, and at that time beta-2 agonists ...
Also, roscovitine can either act as an agonist or antagonist for the P-type calcium channels in the presynaptic membrane. ... The P-type calcium channel is a type of voltage-dependent calcium channel. Similar to many other high-voltage-gated calcium ... type calcium channels are voltage-dependent calcium channels that are classified under the high voltage activated class channel ... P-type calcium channel blockers act to impede the flow of calcium. The blocking of calcium currents may cause the organism to ...
... which is responsible for turning on calcium inflow channels. A decrease in activation of calcium channels will therefore result ... beta2-adrenergic agonists, and clonidine. Some evidence suggests that sotalol should be avoided in the setting of heart failure ... As with other beta blockers, it may interact with calcium channel blockers, catecholamine-depleting drugs, insulin or ... In consideration of these important properties of calcium, two conclusions can be drawn. First, with less calcium in the cell, ...
A more recent example is the N-type calcium channel blocker ziconotide analgesic which is based on a cyclic peptide cone snail ... The most potent narcotic component of opium is the alkaloid morphine which acts as an opioid receptor agonist. ... an N-type neuronal calcium channel blocker found in the venom of Conus magus". Toxicon. 36 (11): 1651-8. doi:10.1016/S0041-0101 ... ion channels, and enzymes. In some cases, they have also served as leads in the development of novel drugs. For example, ...
... and a neuronal calcium channel blocker. Capsaicin is able to excite and desensitize C-fibers. As such, it is not only able to ... It is suggested that this compound, similarly to its trans isomer, is an agonist of the vanilloid receptor VR1 (TRPV1) ... activation of calcium-dependent protein kinase C isoforms and subsequent channel phosphorylation. Desensitization involves both ... St Pierre M, Reeh PW, Zimmermann K (June 2009). "Differential effects of TRPV channel block on polymodal activation of rat ...
They found that charged sodium-channel blockers can be targeted into nociceptors by the application of TRPV1 agonists to ... Voltage sensing in thermo-TRP channels has been reviewed by Brauchi et al. TRP channels have six TMS helices. These channels ... 2F37​ Transient receptor potential cation channel subfamily A member 1: PDB: 3J9P​ Voltage-gated ion channel Ion channel ... The transient receptor potential Ca2+ channel (TRP-CC) family (TC# 1.A.4) is a member of the voltage-gated ion channel (VIC) ...
The drug also dose-dependently blocks voltage-gated calcium channels. It is not a benzodiazepine; instead, it is an imidazolone ... a full agonist of this site). It is the first partial agonist to be approved for the treatment of epilepsy. ... partial agonist of the benzodiazepine site of the GABAA receptor (up to 12-21% of the maximal potentiation of diazepam, ... the first partial benzodiazepine receptor agonist developed for the treatment of epilepsy". CNS Drugs. 28 (1): 29-43. doi: ...
They are ligand-gated ion channels with binding sites for acetylcholine as well as other agonists. When agonists bind to a ... calcium and sodium ions. The nAChRs are made up by different subunits which determine the quaternary structure of the receptor ... Drugs that influence nAChRs can be agonists, partial agonists or antagonists. Agonists, e.g. nicotine, can however act as ... When ACh or other agonists bind to the receptors it stabilizes the open state of the ion channel allowing influx of cations ...
... which are agonists of the transient receptor potential (TRP) family of calcium channels. FAAH knockout mice display highly ... Deutsch DG, Chin SA (September 1993). "Enzymatic synthesis and degradation of anandamide, a cannabinoid receptor agonist". ... agonist. Due to the ability of FAAH to regulate nociception, it is currently viewed as an attractive drug target for the ... "A FAAH-regulated class of N-acyl taurines that activates TRP ion channels". Biochemistry. 45 (30): 9007-15. doi:10.1021/ ...
... (EVP-22) is a chemical compound which acts as an "agonist" (i.e. channel opener) for the TRPML2 calcium channel, with ... November 2018). "Selective agonist of TRPML2 reveals direct role in chemokine release from innate immune cells". eLife. 7. doi: ... November 2020). "TRPML2 is an osmo/mechanosensitive cation channel in endolysosomal organelles". Science Advances. 6 (46): ... high selectivity for TRPML2 and no significant activity at the related TRPML1 and TRPML3 channels. It has been used to ...
... is a chemical compound which acts as an "agonist" (i.e. channel opener) for the TRPML3 calcium channel, with high ... October 2020). "ML-SA1, a selective TRPML agonist, inhibits DENV2 and ZIKV by promoting lysosomal acidification and protease ... selectivity for TRPML3 and no significant activity at the related TRPML1 and TRPML2 channels. It has demonstrated antiviral ...
Other research has also suggested that calcium flow through N-type calcium channels is essential for normal breathing, and is ... Several synthetic compounds have been shown to act on neurons specific to the preBötC, most being selective agonists or ... Other potassium channels like large conductance calcium-dependent potassium channels and sodium chloride dependent potassium ... voltage gated calcium channels become activated and calcium is able to flow into the cell which usually leads to the release of ...
性鈣通道(英語:Voltage-dependent calcium channel). 突觸後致. 密物質(英語:Postsynaptic density) ... Glutamate receptor agonist(英語:Excitatory amino acid agonist) (AMPA(英語:Ampakine)) ... Acetylcholine receptor agonist(英語:Parasympathomimetic_drug) (Muscarinic(英語:Muscarinic agonist) ... 腎上腺素受體激動藥 (α
Tropomyosin receptor kinase B § Agonists. References[edit]. *^ a b c GRCh38: Ensembl release 89: ENSG00000176697 - Ensembl, May ... NMDA receptor activation by rapid successive firing allows calcium influx in addition to sodium. The calcium influx triggered ... will communicate regularly and maintain the synapse structure and function long after the initial activation of NMDA channels. ... Promoter IV activity, leading to the translation of exon IV-containing mRNA, is strongly stimulated by calcium and is primarily ...
... is a drug developed by Abbott, which acts as an agonist at neural nicotinic acetylcholine receptors selective for the ... Ion channel. modulators. Calcium blockers. *Gabapentin. *Gabapentin enacarbil. *Mirogabalin. *Pregabalin. *Ziconotide. Sodium ... heptanes as Novel α4β2 Nicotinic Acetylcholine Receptor Selective Agonists". Journal of Medicinal Chemistry. 50 (22): 5493-5508 ... heptane α4β2 nicotinic acetylcholine receptor selective agonist: Synthesis, analgesic efficacy and tolerability profile in ...
L-Type calcium channel blockers (e.g., dihydropyridines: nifedipine). *Nebivolol (beta blocker) ... Sarcosine; Polyamine site agonists: Neomycin. *Spermidine. *Spermine; Other positive allosteric modulators: 24S- ... "Structural insights into calcium-bound S100P and the V domain of the RAGE complex". PLOS ONE. 9 (8): e103947. Bibcode ...
Agonists. *Cations (incl. aluminum, calcium, gadolinium, magnesium, strontium, zinc). *Dehydroandrosterone. * ... DDE concentration and percent eggshell thinning in Double-crested Conmorant eggs(North Channel, Lake Huron, Ont.) ... p'-DDE impairs the shell gland's ability to excrete calcium carbonate onto the developing egg.[7][9][10][11][12] Multiple ...
Prolactin modulators: Prolactin inhibitors: D2 receptor agonists (e.g., bromocriptine, cabergoline); Prolactin releasers: D2 ... Bradykinin raises internal calcium levels in neocortical astrocytes causing them to release glutamate, though this finding has ... See also: Receptor/signaling modulators • Ion channel modulators. Retrieved from " ...
... but could relate to actions of the drug on voltage-activated calcium channels. Lamotrigine blocks T-type calcium channels ... It also blocks L-, N-, and P-type calcium channels and has weak 5-hydroxytryptamine-3 (5-HT3) receptor inhibition. These ... However, it does inhibit native and recombinant high-voltage-activated calcium channels (N- and P/Q/R-types) at therapeutic ... Whether this activity on calcium channels accounts for lamotrigine's broader clinical spectrum of activity in comparison with ...
General: β-receptor blockers ("beta blockers"), calcium channel blockers, diuretics, cardiac glycosides, antiarrhythmics, ... gamolenic acid, gonadotropin release inhibitor, progestogen, dopamine agonists, oestrogen, prostaglandins, gonadorelin, ... calcium channel blockers, thiazide diuretics, loop diuretics, aldosterone inhibitors. *Coagulation: anticoagulants, heparin, ... Anti-glaucoma: adrenergic agonists, beta-blockers, carbonic anhydrase inhibitors/hyperosmotics, cholinergics, miotics, ...
Calcium channel blockers. *renin-angiotensin system *ACE inhibitors. *Angiotensin II receptor antagonists ... Benzodiazepines (GABA receptor agonists) *Midazolam (Versed) is given at the onset of anesthesia and has been shown in recent ... cation uptake by the receptor channel and contraction of isolated guinea-pig ileum", Eur J Pharmacol, 530 (1-2): 136-43, doi: ...
The cause is thought to be blockade of hERG voltage-gated potassium channels.[41][42] The risks are dose-dependent, and appear ... upper gastrointestinal motility disorders and to prevent gastrointestinal symptoms associated with the use of dopamine agonist ... the voltage-gated potassium channel KCNH2 gene (hERG/Kv11.1), and the α1D-adrenoceptor ADRA1D gene.[58] ... Ion channel modulators. Calcium. VDCCs. Blockers. *L-type-selective: Dihydropyridines: Amlodipine. *Aranidipine ...
GABAR agonists: Progabide; GAT-1 inhibitors: Tiagabine. Channel. modulators. Sodium blockers. *Hydantoins: Ethotoin ... Calcium blockers. *Oxazolidinediones: Ethadione. *Paramethadione. *Trimethadione; Succinimides: Ethosuximide#. *Mesuximide. * ...
... are agonists of the prostacyclin receptor, which leads to vasodilation in the pulmonary circulation.[1] ...
... the release through presynaptic effects through a voltage dependent inhibition of high voltage activation of calcium channels. ... GABAB agonist: baclofen[edit]. Baclofen (β-p-chlorophenyl-GABA) has some analgesic properties and has been traditionally used ... GABA acts via binding to its receptors which include the ligand gated ion channels, GABAA and GABAC and the G-protein couple ... restoration of GABAergic synaptic activity and region-specific restoration of GABAA receptor associated chloride channel ...
Ion channel. modulators. Calcium blockers. *Alcohol (ethanol). *Gabapentin. *Gabapentin enacarbil. *Mirogabalin. *Pregabalin ... Agonists: Carbocyclic thromboxane A2. *I-BOP. *Thromboxane A2. *U-46619 ...
... δ subunit-containing voltage-gated calcium channels (VGCCs).[19] However, it is weaker relative to phenibut in this action (Ki ... baclofen is in the range of 100-fold more potent by weight as an agonist of the GABAB receptor in comparison to phenibut, and ... "R-phenibut binds to the α2-δ subunit of voltage-dependent calcium channels and exerts gabapentin-like anti-nociceptive effects ... another GABAB receptor agonist, γ-hydroxybutyric acid (GHB), has been associated with euphoria, abuse, and addiction.[13] These ...
Agonists and antagonists[edit]. Specific antagonists include istradefylline (KW-6002) and SCH-58261, while specific agonists ... "IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.. ... Also recently discovered A2B has Gq → DAG and IP3 → Release calcium → activate calmodulin → activate myosin light chain kinase ... Tecadenoson is an effective A1 adenosine agonist, as is selodenoson. In the heart[edit]. The A1, together with A2A receptors of ...
N-type calcium-channel blocker.. Intrathecal.. Protein binding = 50%; half-life = 2.9-6.5 hours; excretion = urine (,1%).[122] ... Full agonist at kappa opioid receptors, partial agonist/antagonist at the mu opioid receptors.[39]. IM, IV, SC.. Protein ... Binds to the α2δ-1 subunit of voltage gated calcium ion channels in the spinal cord. May also modulate NMDA receptors and ... Partial agonist at the mu opioid receptor; agonist at delta opioid receptor; antagonist at kappa opioid receptor.. Sublingual, ...
... calcium channel blockers (isradipine) and growth factors (GDNF).[56] Preclinical research also targets alpha-synuclein.[129] A ... Dopamine agonists. Several dopamine agonists that bind to dopamine receptors in the brain have similar effects to levodopa.[74] ... There have been preliminary indications that the use of anti-inflammatory drugs and calcium channel blockers may be protective. ... Apomorphine, a non-orally administered dopamine agonist, may be used to reduce off periods and dyskinesia in late PD.[74] It is ...
Calcium channel blockers. *renin-angiotensin system *ACE inhibitors. *Angiotensin II receptor antagonists ... "Miscellaneous Sympathomimetic Agonists". In Brunton LL, Chabner BA, Knollmann BC (eds.). Goodman & Gilman's Pharmacological ... National Geographic Channel. Archived from the original on 8 July 2016.. *^ United Nations Office on Drugs and Crime (2007). ...
NMDA agonists therefore exhibit fast Mg2+ unbinding kinetics, increasing channel open probability with depolarization. This ... and calcium (Ca2+) ions into the cell and potassium (K+) out of the cell.[5][6][7][8] Ca2+ flux through NMDA receptors in ... Thus, the channel acts as a "coincidence detector" and only once both of these conditions are met, the channel opens and it ... Mg2+ blocks the NMDA receptor channel in a voltage-dependent manner. The channels are also highly permeable to Ca2+. Activation ...
These drugs include statins, HIV protease inhibitors, many calcium channel blockers, lidocaine, the benzodiazepines, and ... Agonists: 2-(1-Hexynyl)-N-methyladenosine. *2-Cl-IB-MECA. *2'-MeCCPA ... The drug binds to glutamate-gated chloride channels (GluCls) in the membranes of invertebrate nerve and muscle cells, causing ... Yates DM, Wolstenholme AJ (August 2004). "An ivermectin-sensitive glutamate-gated chloride channel subunit from Dirofilaria ...
Pregabalin (Lyrica) acts on the voltage-dependent calcium channel to decrease the release of neurotransmitters such as ... 5-HT1A receptor partial agonists, such as buspirone and tandospirone.. *Serotonin-norepinephrine reuptake inhibitors (SNRIs), ...
Ion channel. modulators. Calcium blockers. *Gabapentin. *Gabapentin enacarbil. *Pregabalin. *Ziconotide. Sodium blockers. * ... Agonists: Carbocyclic thromboxane A2. *I-BOP. *Thromboxane A2. *U-46619 ...
Calcium channel blockers. *renin-angiotensin system *ACE inhibitors. *Angiotensin II receptor antagonists ... α-Adrenergic receptor agonists[edit]. Main article: α-Adrenergic receptor agonist. Common or widely marketed[edit]. * ... whereas phenylephrine and oxymetazoline are direct agonists. The effects are not limited to the nose, and these medicines may ...
... κ-opioid receptor agonist and μ-opioid receptor antagonist.[4][5][6] ... Ion channel. modulators. Calcium blockers. *Gabapentin. *Gabapentin enacarbil. *Pregabalin. *Ziconotide. Sodium blockers. * ...
However, β2 adrenergic receptor agonists are not recommended to treat ARDS because it may reduce survival rates and precipitate ... and activation of ATP-sensitive potassium channels.[50] In those with severe sepsis and septic shock, this sequence of events ... impaired calcium transport, and low production of adenosine triphosphate (ATP), can cause myocardial depression, reducing ...
Prolactin modulators: Prolactin inhibitors: D2 receptor agonists (e.g., bromocriptine, cabergoline); Prolactin releasers: D2 ... Calcium channel blockers. *Dotarizine. *Lomerizine. *Verapamil. *Flunarizine. Progestogens. *Flumedroxone acetate. ...
"IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.. ... a selective agonist for PGE2 receptor subtype 3". Journal of Leukocyte Biology. 68 (2): 187-93. PMID 10947062.. ... "Isoforms of the EP3 subtype of human prostaglandin E2 receptor transduce both intracellular calcium and cAMP signals". ... "Functional interaction of the carboxylic acid group of agonists and the arginine residue of the seventh transmembrane domain ...
Prolactin modulators: Prolactin inhibitors: D2 receptor agonists (e.g., bromocriptine, cabergoline); Prolactin releasers: D2 ... "IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.. ... positive regulation of cytosolic calcium ion concentration. • digestion. • phospholipase C-activating G-protein coupled ... agonist character of chimeric galanin peptides". The Journal of Pharmacology and Experimental Therapeutics. 287 (2): 448-56. ...
Alpha2 Agonists, Central-Acting. Class Summary. These agents decrease central adrenergic output. ... Calcium Channel Blockers. Class Summary. These agents block calcium channels in vascular smooth muscle, which leads to ... Isradipine is a dihydropyridine calcium channel blocker. It binds to calcium channels with high affinity and specificity and ... inhibits calcium flux into cardiac and smooth muscle. The resultant effect is arteriole dilation, which reduces systemic ...
Calcium channel blocker (CCB) toxicity is one of the most lethal prescription drug overdoses; therefore, understanding the ... encoded search term (Calcium Channel Blocker Toxicity) and Calcium Channel Blocker Toxicity What to Read Next on Medscape. ... Calcium Salts. Class Summary. These agents theoretically increase calciums concentration gradient, overcoming the channel ... Varpula T, Rapola J, Sallisalmi M, Kurola J. Treatment of serious calcium channel blocker overdose with levosimendan, a calcium ...
The cannabinoid agonist Win55,212-2 inhibits calcium channels by receptor-mediated and direct pathways in cultured rat ... and P/Q-type Ca2+ channels. Concentrations of agonist greater than 1 microM inhibited Ca2+ channels directly. ... The effects of the cannabinoid receptor agonist Win55,212 on Ca2+ channels were studied in rat hippocampal neurons grown in ... Win55,212-2 inhibited whole-cell Ba2+ currents through Ca2+ channels by both CB1 receptor-mediated and direct mechanisms. The ...
All roads lead to presynaptic calcium channel inhibition by the ghrelin receptor: Separate agonist-dependent and -independent ... All roads lead to presynaptic calcium channel inhibition by the ghrelin receptor: Separate agonist-dependent and -independent ...
... channels (Cav2.2) in sympathetic neurons. In addition to acetate and propionate, we show that β-hydroxybutyrate (BHB), a ... acetate and propionate are agonist, have emerged as important G-protein-coupled receptors influenced by diet and gut flora ... metabolite produced during ketogenic conditions, is also an FFA3 agonist. This contrasts with previous interpretations of BHB ... β-Hydroxybutyrate modulates N-type calcium channels in rat sympathetic neurons by acting as an agonist for the G-protein- ...
Effects of the calcium channel agonist, BAY K 8644, on electrical activity in mouse pancreatic B-cells.. ... Effects of the calcium channel agonist, BAY K 8644, on electrical activity in mouse pancreatic B-cells. ... Pharmacological analysis of the effects of Bay K 8644 and organic calcium antagonists on the mouse isolated distal colon par ... Ca2+ entry through L-type voltage-sensitive Ca2+ channels stimulates the release of human chorionic gonadotrophin and placental ...
Calcium Channel Agonists. Membrane Transport Modulators. Molecular Mechanisms of Pharmacological Action. Vasoconstrictor Agents ... Known or suspected disorders of calcium metabolism associated with hypercalcaemia. *Known or suspected severe renal ...
Calcium Channel Agonists. Membrane Transport Modulators. Molecular Mechanisms of Pharmacological Action. Vasoconstrictor Agents ... Subjects with known/suspected disorders of calcium metabolism associated with hypercalcemia within the last 10 years, based on ...
Calcium Channel Agonists / pharmacology* * Codon, Terminator* * Gene Expression Regulation / drug effects* * HEK293 Cells ...
Calcium-Regulating Hormones and Agents. Calcium Channel Agonists. Membrane Transport Modulators. Molecular Mechanisms of ...
Calcium-Regulating Hormones and Agents. Calcium Channel Agonists. Membrane Transport Modulators. Molecular Mechanisms of ... Use of alpha2-agonists, beta-blockers, or more than 2 anti-hypertensive medications at screening ... Vitamin D supplements, calcium supplements, estrogen replacement therapy, corticosteroids (inhaled/oral), or hydroxymethyl ...
... rapidly potentiates N and L calcium channel currents in cerebellar granule neurons by an unknown mechanism. Here, we show that ... the L channel alpha1C subunit is tyrosine phosphorylated in response to IGF-1. Moreover, expression of kinase-dead c-Src in ... Calcium Channel Agonists / pharmacology* * Calcium Channels, L-Type / drug effects * Calcium Channels, L-Type / genetics ... Insulin-like growth factor 1 (IGF-1) rapidly potentiates N and L calcium channel currents in cerebellar granule neurons by an ...
... calcium channel blockers; dopamine receptor agonists and antagonists; narcotic antagonists; protease inhibitors; respiratory ... calcium channel blockers; dopamine receptor agonists and antagonists; narcotic antagonists; protease inhibitors; respiratory ... calcium channel blockers; dopamine receptor agonists and antagonists; narcotic antagonists; protease inhibitors; respiratory ... Other possible drugs for use in the invention include all alpha-adrenergic agonists and blockers; beta-adrenergic agonists and ...
calcium channel agonist Agents that increase calcium influx into calcium channels of excitable tissues. ... calcitriol (CHEBI:17823) has role calcium channel agonist (CHEBI:38807) calcitriol (CHEBI:17823) has role calcium channel ... calcium channel modulator A membrane transport modulator that is able to regulate intracellular calcium levels. ...
Effects of intrathecal L-and N-type calcium channel blockers on the antinociception evoked by opioid agonists in the rat tail ... Animals , Rats , Male , Analgesics, Opioid/agonists , Analgesics/metabolism , Benzomorphans/pharmacology , Calcium Channel ... The intrathecal administration of an N-type calcium channel blocker with a delta-opioid agonist seems to be the most effective ... The effects of intrathecal administration of nimodipine or omega-conotoxin GVIA(L- and N-type calcium channel blockers, ...
Kappa agonists, Opioid receptor ligands, Drugs acting on the nervous system, Analgesic, Calcium channel blockers Categories. ‹ ...
Bay was released continually from scaffolds within the physiological range required for agonist activity (1-10 microM). Patch ... Calcium Channel Agonists, Calcium Channels, L-Type, Cell Line, Tumor, Delayed-Action Preparations, Drug Stability, Lactic Acid ... Characterizing the efficacy of calcium channel agonist-release strategies for bone tissue engineering applications. ... Characterizing the efficacy of calcium channel agonist-release strategies for bone tissue engineering applications. ...
Using a Na+-rich, Ca2+-free pipette solution a novel single channel current was recorded in addition to the conventional Na+ an ... 0/Calcium Channel Agonists; 0/Calcium Channel Blockers; 0/Calcium Channels, L-Type; 0/Ion Channels; 55985-32-5/Nicardipine; ... Calcium Channel Agonists / pharmacology. Calcium Channel Blockers / pharmacology*. Calcium Channels, L-Type / drug effects, ... 2582115 - Two types of calcium channels in the somatic membrane of new-born rat dorsal root gangl.... 24215285 - Effect of ...
Calcium Channel Agonists / pharmacology*. Cell Differentiation / drug effects, physiology*. Cell Division / drug effects, ... 0/Antineoplastic Agents; 0/Calcium Channel Agonists; 0/Macrophage-1 Antigen; 302-79-4/Tretinoin; 32222-06-3/Calcitriol ...
The Action of Calcium Channel Agonists on the Mammalian Ventricular Myocardium D. Bose, L. V. Hryshko, J. K. Saha, R. A. ... atherosclerosis biochemistry blood pressure calcium heart metabolism pathophysiology physiology research ultrasound Editors and ...
Beta2-Agonists; Calcium Channel Blockers; Constipation Drugs; Disease-modifying drugs for Multiple Sclerosis; HMG-CoA Reductase ...
β2-adrenergic agonists, calcium channel blockers, benzodiazepines, dopamine.. *Estrogens, narcotic analgesics, nitrates, ... The treatment of comorbidities (eg, with calcium channel blockers, anticholinergics, and nonsteroidal anti-inflammatory drugs ( ... Simple antacids neutralize gastric acid-that is, sodium, calcium, magnesium, and aluminum salts. ...
β1 agonists stimulate adenylyl cyclase activity and opening of calcium channel (cardiac stimulants; used to treat cardiogenic ... Prenalterol Xamoterol β2 agonists stimulate adenylyl cyclase activity and closing of calcium channel (smooth muscle relaxants; ... Beta adrenergic agonists or beta agonists are medications that relax muscles of the airways, causing widening of the airways ... In general, pure beta-adrenergic agonists have the opposite function of beta blockers: beta-adrenoreceptor agonist ligands ...
9 results for Category equals CALCIUM CHANNEL AGONISTS Info. Please enable JavaScript in your browser. Row Number. Result. ...
CALCIUM CHANNEL AGONISTS. Embodiments of calcium channel agonists, as well as methods of making and using the calcium channel ... MODIFIED LIGAND-GATED ION CHANNELS AND METHODS OF USE. This document relates to materials and methods for controlling ligand ... gated ion channel (LGIC) activity. For example, modified LGICs including at least one... ...
Calcium channel agonists: Nifedipine, diltiazen,amlodipine. Definition. Action: Blocks calcium influx during slow channel ... Action: B2 adrenergic receptor agonist causes bronchodilation.. ADE:Basodilation, tachycardia, palpitations, tremor, CNS stim. ... Action: B2 adrenergic receptor agonist causes bronchodilation.. ADE: Vasodilation, tachycardia, palpitations, tremor, CNS ... Action: B2 adrenergic receptor agonist causes bronchodilation.. ADE: Basodilation, tachycardia, palpitations, tremor, CNS ...
Intracellular calcium strongly potentiates agonist-activated TRPC5 channels. J. Gen. Physiol. 133, 525-546. ... This release is independent of action potentials but dependent on the activation of Cav3.1 T-type calcium channels and calcium ... Functional organization of TRPC-Ca2+ channels and regulation of calcium microdomains. Cell Calcium 40, 495-504. ... Pani, B., and Singh, B. B. (2009). Lipid rafts/caveolae as microdomains of calcium signaling. Cell Calcium 45, 625-633. ...
Calcium Channel AgonistsIBA 05/2000. 1. Verapamil (Calan)FDA LinkGeneric 05/2000. ... Calcium Channels (Calcium Channel)IBA 09/2008 - 10/2002. 3. L-Type Calcium Channels (Dihydropyridine Receptor)IBA 01/2006 - 05/ ... Q-Type Calcium Channels (Q-Type Calcium Channel)IBA 10/2002. 1. domoic acidIBA 09/2002. ...
... cardiovascular preparations including calcium channel blockers such as nifedipine; beta-agonists such as dobutamine and ... parathyroid hormone and agonists, parathyroid hormone antagonists, prostaglandin antagonists, pentigetide, protein C, protein S ... antidiuretic hormone agonists, antidiuretic hormone antagonists, bradykinin antagonists, CD4, ceredase, CSFs, enkephalins, FAB ...
1985) Three types of neuronal calcium channel with different calcium agonist sensitivity. Nature 316:440-443. ... 1992) Multiple types of high-threshold calcium channels in rabbit sensory neurons: high-affinity block of neuronal L-type by ... 1986) Widespread distribution of dihydropyridine-sensitive calcium channels in the central nervous system. Molecular Pharmacol ... an L-type channel blocker, and ω-conotoxin-GVIA, an N-type channel blocker. Whereas conotoxin (1 μm) depressed the Ca2+ rise ...
  • The effects of intrathecal administration of nimodipine or omega-conotoxin GVIA (L- and N-type calcium channel blockers, respectively) alone or followed by DAMGO , DADLE or bremazocine (mu-, delta - and kappa- opioid agonists , respectively) were studied on the rat tail flick test. (
  • The mechanism by which calcium channel blockers affect neuromuscular transmission is not well established. (
  • 3 In patients without known defects of neuromuscular transmission, the calcium channel blockers felodipine and nifedipine have been found to produce features of myasthenia gravis including dysphagia, ptosis, and generalized weakness after long-term use ranging from 18 months to 12 years. (
  • 5 , 6 Thus, although not absolutely contraindicated, calcium channel blockers should be used with caution in patients with myasthenia gravis. (
  • Nifedipine and barnidipine act as calcium channel blockers, and are widely prescribed for pressure control of prehypertension and stage 1 hypertension. (
  • thus, diag- -agonists, calcium channel blockers, mal heart rate response in some nosis relies heavily on results of labo- or xanthine derivatives. (
  • The mESC-CM beating arrest assay was not responsive to potassium channel blockers and showed a lower sensitivity to sodium channel blockers and Na + /K + ATPase inhibitors compared to the hiPSC-CM MEA assay. (
  • Calcium channel blockers and a β-adrenergic receptor agonist showed comparable potencies in both models. (
  • Tender, swollen, or bleeding gums (caused by calcium channel blockers). (
  • Constipation (caused by calcium channel blockers and central alpha agonists). (
  • The high blood pressure medication beta blockers and the medication calcium channel blockers prescribed to lower blood pressure seem to increase the risk of corrective cataract surgery according to a study published in the British Journal of Ophthalmology. (
  • How do calcium channel blockers work for high blood pressure? (
  • To treat blood high blood pressure, calcium channel blockers (sometimes called CCBs for short, or calcium antagonists) don't let calcium into certain muscle cells in your heart and blood vessels, so it's harder for electrical signals to pass. (
  • Discusses toxicity of calcium channel blockers, beta-blockers, cardiac glycosides and alpha-2 agonists. (
  • Several different types of drugs are available: alpha-blockers, ACE inhibitors, diuretics, central agonists, calcium channel blockers and angiotension II receptor blockers, according to WebMD. (
  • May cause conduction defects with calcium channel blockers, digoxin. (
  • A range of drug options are used for treatment of hypertension, such as thiazide diuretics, ACE inhibitors, angiotensin receptor blockers, calcium channel blockers and beta blockers. (
  • Among the most important and most widely used medications are thiazide diuretics , calcium channel blockers , ACE inhibitors , angiotensin II receptor antagonists (ARBs), and beta blockers . (
  • [5] Although clinical evidence shows calcium channel blockers and thiazide-type diuretics are preferred first-line treatments for most people (from both efficacy and cost points of view), an ACE inhibitor is recommended by NICE in the UK for those under 55 years old. (
  • In the United States, the JNC8 (Eighth Joint National Committee on the Prevention, Detection, Evaluation, and Treatment of High Blood Pressure) recommends thiazide-type diuretics to be one of the first-line drug treatments for hypertension, either as monotherapy or in combination with calcium channel blockers , ACE inhibitors , or angiotensin II receptor antagonists . (
  • Calcium channel blockers block the entry of calcium into muscle cells in artery walls. (
  • The 8th Joint National Committee (JNC-8) recommends calcium channel blockers to be a first-line treatment either as monotherapy or in combination with thiazide -type diuretics, ACE inhibitors , or angiotensin II receptor antagonists for all patients regardless of age or race. (
  • [11] The AASK trial showed that ACE inhibitors are more effective at slowing down the decline of kidney function compared to calcium channel blockers and beta blockers . (
  • [7] Results from the ALLHAT trial showed that thiazide -type diuretics and calcium channel blockers were both more effective as monotherapy in improving cardiovascular outcomes compared to ACE inhibitors for this subgroup. (
  • It may therefore be possible to lower anal sphincter pressure using calcium channel blockers and cholinergic agonists without side effects. (
  • however, treatment of acute pancreatitis using calcium channel blockers did not produced consistent results. (
  • Antagonists reduce or block the signals of agonists. (
  • While competitive antagonists bind to the agonist or ligand binding site of the receptor reversibly, non-competitive antagonists can either bind to the ligand site or other site called the allosteric site. (
  • The calcium channel antagonists receptor from rabbit skeletal muscle. (
  • Agents used to delay premature uterine activity include magnesium sulfate, beta-mimetics, oxytocin antagonists, calcium channel inhibitors, and adrenergic beta-receptor agonists. (
  • 7. The method of claim 1 , wherein the pharmaceutical formulation further includes a compound selected from the group consisting of steroid agonists, partial agonists and antagonists. (
  • Tocolytic therapy includes calcium channel blocking agents, beta-adrenergic receptor agonists, magnesium sulfate, and cyclooxygenase inhibitors. (
  • How do central agonists work to treat high blood pressure? (
  • Thus, activation of cannabinoid receptors inhibits N- and P/Q-type Ca2+ channels. (
  • Activation of cannabinoid receptors inhibited only a fraction of the whole-cell Ca2+ channel current (17+/-2%) even though more than half of the whole-cell Ba2+ current was carried by N- and P/Q-type Ca2+ channels. (
  • Free fatty acids receptor 3 (FFA3, GPR41) and 2 (FFA2, GPR43), for which the short-chain fatty acids (SCFAs) acetate and propionate are agonist, have emerged as important G-protein-coupled receptors influenced by diet and gut flora composition. (
  • There are two families of P2 receptors, P2X receptors, which are ligand-gated ion channels, and P2Y receptors, which belong to the group of G protein-coupled receptors. (
  • For calcium influx and intracellular Ca 2+ release, respectively, the density of dihydropyridine receptors (DHPRs) and ryanodine receptors (RyRs) was examined, using high-affinity (-)-enantiomers of dihydropyridine and ryanodine labelled with fluorophores. (
  • Current therapies for acute migraine consist primarily of the serotonin1 B /1 D receptor agonists (more commonly known as triptans), such as sumatriptan, that have been shown in experimental studies to block CGRP release and action, inhibiting trigeminovascular nociceptive transmission. (
  • Other newer potential pharmacological approaches to managing chronic constipation include selective calcium channel agonists (lubipristone) or 5HT3 serotonin receptor agonists (tegaserod). (
  • Agents that increase calcium influx into calcium channels of excitable tissues. (
  • The effects may result from activation of an unknown membrane receptor and the adenylate cyclase/cAMP pathway, which enhances Ca 2+ influx across the L-type Ca 2+ channel. (
  • He suspects that opening up the channels leads to greater calcium influx during action potentials. (
  • For people in the end stages of ALS, boosting calcium influx might make things worse, Armstrong suggested. (
  • A class of drugs that act by selective inhibition of calcium influx through cellular membranes. (
  • Depletion of Ca2+ stores in the sarcoplasmic reticulum results in the opening of store operated cation channels (SOCCs) on the plasma membrane, allowing Ca2 + influx into the cell and refilling of the stores. (
  • In conclusion, voltage-sensitive L-type Ca 2+ channels for ion influx and RyRs for Ca 2+ release are present in the cells of the skin of female and male chickens. (
  • The intrathecal administration of an N-type calcium channel blocker with a delta -opioid agonist seems to be the most effective combination to produce antinociception in the rat tail flick test. (
  • Mutagenesis of the mouse delta opioid receptor converts (-)-buprenorphine from a partial agonist to an antagonist. (
  • Isradipine is a dihydropyridine calcium channel blocker. (
  • Initial management for a symptomatic calcium channel blocker overdose includes cardiovascular support with intravenous (IV) fluids and, if necessary, vasopressors. (
  • Additionally, high-dose insulin has been established as an effective therapy for calcium channel blocker overdose with cardiogenic shock. (
  • Civamide (Winston Laboratories) is a vanilloid receptor agonist and neural calcium channel blocker. (
  • A sodium-channel blocker infusion test did not result in the typical ECG pattern of Brugada syndrome (BS), and the test attenuated J-point elevation in the inferolateral leads. (
  • Also potent CYP2D2 inhibitor (IC 50 = 87 nM) and L-type calcium channel blocker. (
  • Ion channels are membrane proteins that are used by the cell as signal transducers and as a pathway for the rapid entry of some regulatory compounds such as calcium ions. (
  • In the meantime, Armstrong is testing the channel-opening compounds in a mouse model of TDP-43 pathology. (
  • Disclosed are compounds of Formula A, or a salt thereof: Formula (A), wherein: Het, Q and R1A to R4A are defined herein, which compounds have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. (
  • A receptor's agonist does not bind to its allosteric binding site. (
  • If the non-competitive antagonist binds to the allosteric site and an agonist binds to the ligand site, the receptor will remain unactivated. (
  • Small organic molecules that act as allosteric activators of the calcium sensing receptor (CaSR) in the PARATHYROID GLANDS and other tissues. (
  • Calcium is given to reverse hypotension and improve cardiac conduction defects. (
  • These agents block calcium channels in vascular smooth muscle, which leads to vasodilatation. (
  • The cannabinoid agonist Win55,212-2 inhibits calcium channels by receptor-mediated and direct pathways in cultured rat hippocampal neurons. (
  • The effects of the cannabinoid receptor agonist Win55,212 on Ca2+ channels were studied in rat hippocampal neurons grown in primary culture. (
  • β-Hydroxybutyrate modulates N-type calcium channels in rat sympathetic neurons by acting as an agonist for the G-protein-coupled receptor FFA3. (
  • Insulin-like growth factor 1 (IGF-1) rapidly potentiates N and L calcium channel currents in cerebellar granule neurons by an unknown mechanism. (
  • Moreover, expression of kinase-dead c-Src in neurons or acute block of Src family kinases with a cell-permeable inhibitor specifically blocks L channel potentiation. (
  • By opening Cl − channels, GABA generally hyperpolarizes the membrane potential, decreases neuronal activity, and reduces intracellular Ca 2+ of mature neurons. (
  • Drugs that open up calcium channels in those neurons restore both this communication and the fishes' ability to swim properly. (
  • However, he cautioned that high calcium levels can be toxic to neurons. (
  • To investigate the selective toxicity of emodepside, we performed transgenic experiments in which the nematode SLO-1 channel was swapped for a mammalian ortholog, human KCNMA1. (
  • Strains expressing the human KCNMA1 channel were preferentially sensitive to the mammalian channel agonists NS1619 and rottlerin. (
  • Calcium currents in embryonic and neonatal mammalian skeletal muscle. (
  • It binds to calcium channels with high affinity and specificity and inhibits calcium flux into cardiac and smooth muscle. (
  • Calcium gluconate moderates nerve and muscle performance and facilitates normal cardiac function. (
  • The drug's beta-agonist effects include bronchodilatation, chronotropic cardiac activity, and positive inotropic effects. (
  • The time constant of the first latency histogram was about two orders of magnitude larger than those in cardiac L-type Ca2+ channels and decreased with depolarization. (
  • Comparing the cardiac effects of the dihydropyridinederivative H 160/51 with those of the "Ca-agonist" Bay K8644. (
  • Therefore, tissue-selective calcium agonists have the potential to combat cardiac failure and endocrinological disorders. (
  • We explored TFP actions on cardiac SR Ca release in cells and single type-2 ryanodine receptor (RyR2) channel activity in bilayers. (
  • Substances that bind to and sequester CALCIUM ions. (
  • IPSCs in this type of synapses originate from the presynaptic release of glycine that interacts with the post-synaptic GlyRs and induces opening of the anion-selective channels ( Betz, 1991 ). (
  • Non-selective conductance in calcium channels of frog muscle: Calcium selectivity in a single-file pore. (
  • A membrane transport modulator that is able to regulate intracellular calcium levels. (
  • 1 , 2 Verapamil also prevents potassium outflow at the motor end plate and causes a decrease in intracellular ionized calcium levels. (
  • The behavior of a single channel can be monitored because, when open, the channel passes ~10 6 ions/sec. (
  • They lower the threshold for CaSR activation by extracellular calcium ions and diminish PARATHYROID HORMONE (PTH) release from parathyroid cells. (
  • Chemical agents that increase the permeability of CELL MEMBRANES to CALCIUM ions. (
  • Properties of single calcium-activated potassium channels in cultured rat muscle. (
  • The high sensitivity of MRS 2179 has revealed, for the first time in the human gastrointestinal tract, that a P2Y 1 receptor present in smooth muscle probably mediates this mechanism through a pathway that partially involves apamin-sensitive calcium-activated potassium channels. (
  • SLO-1 belongs to a family of channels that are highly conserved across the animal phyla and regulate neurosecretion, hormone release, muscle contraction, and neuronal network excitability. (
  • Williams ME, Feldman DH, McCue AF, Brenner R, Velicelebi G, Ellis SB, Harpold MM: Structure and functional expression of alpha 1, alpha 2, and beta subunits of a novel human neuronal calcium channel subtype. (
  • Instrumental to this assignment were the toxins that blocked N- and P/Q-types, the major mediators of presynaptic calcium entry. (
  • They are believed to act at both the presynaptic and postsynaptic levels via blockade of L-type calcium channels. (
  • Concentrations of agonist greater than 1 microM inhibited Ca2+ channels directly. (
  • Bay was released continually from scaffolds within the physiological range required for agonist activity (1-10 microM). (
  • The current density of ist was 0.33 pA pF-1 at -60 mV, as estimated from the number of channels per membrane patch, the open probability and the unitary amplitude. (
  • The beta subunit of voltage-dependent calcium channels contributes to the function of the calcium channel by increasing peak calcium current, shifting the voltage dependencies of activation and inactivation, modulating G protein inhibition and controlling the alpha-1 subunit membrane targeting. (
  • Bay K8644 is a chemical compound that functions as a calcium channel agonist. (
  • Bay K8644 targets voltage-sensitive dihydropyridine (DHP) calcium channels (L-Type). (
  • Agonists Bay-K8644 and CGP-28392 open calcium channels reconstituted from skeletal muscle transverse tubules. (
  • A competitive antagonist will attach itself to the same binding site of the receptor that the agonist will bind to. (
  • This type of binding is reversible as increasing the concentration of agonist will outcompete the concentration of antagonist, resulting in receptor activation. (
  • This means only after the agonist binds to the receptor can the antagonist block the receptor's function. (
  • Nicardipine-sensitive Na+-mediated single channel currents in guinea-pig sinoatrial node pacemaker cells. (
  • A dihydropyridine (Bay k 8644) that enhances calcium currents in guinea pig and calf myocardial cells. (
  • Proteasome inhibition was observed under nicardipine treatment that contributed to the up-regulation in cytosolic calcium. (
  • In conclusion, CaMKII down-regulation/proteasome inhibition/cytosolic calcium up-regulation/cathepsin B activation/trypsinogen activation axis was present in pancreatic acinar cells injury under nicardipine treatment. (
  • DI-fusion Effects of the calcium channel agonist, BAY K 8644, on. (
  • Effects of the calcium channel agonist, BAY K 8644, on electrical activity in mouse pancreatic B-cells. (
  • The experimental channel agonists FPL 64176 and Bay K 8644 both returned swimming speed and distance to normal in the mutant fish. (
  • 12. The method of claim 1, wherein the PPARα agonist is delivered into the organ's blood supply while the organ is being perfused by a cardiovascular system. (
  • These agents theoretically increase calcium's concentration gradient, overcoming the channel blockade and driving calcium into the cells. (
  • Sidedness of reconstituted calcium channels from muscle transverse tubules as determined by D600 and D890 blockade. (
  • AIMS To investigate the effect of oral and topical calcium channel blockade and a topical cholinomimetic on anal sphincter pressure. (
  • Here, we show that the L channel alpha1C subunit is tyrosine phosphorylated in response to IGF-1. (
  • The alpha-2/delta subunit of voltage-dependent calcium channels regulates calcium current density and activation/inactivation kinetics of the calcium channel. (
  • Acts as a regulatory subunit for P/Q-type calcium channel (CACNA1A), N-type (CACNA1B), L-type (CACNA1C OR CACNA1D) and possibly T-type (CACNA1G). (
  • Powers PA, Liu S, Hogan K, Gregg RG: Skeletal muscle and brain isoforms of a beta-subunit of human voltage-dependent calcium channels are encoded by a single gene. (
  • Collin T, Wang JJ, Nargeot J, Schwartz A: Molecular cloning of three isoforms of the L-type voltage-dependent calcium channel beta subunit from normal human heart. (
  • Trying various drugs to affect the calcium channels in the fish, Armstrong discovered that opening L-type voltage-dependent calcium channels restored movement. (
  • A long-held tenet of neuromuscular transmission is that calcium-dependent neurotransmitter release is mediated by N-type calcium channels in frog but P/Q-type channels in mammals. (
  • Cloning and heterologous expression of this P/Q-type channel confirmed a block by ω-conotoxin GVIA raising the likelihood that all vertebrates, including frog, use the P/Q-type calcium channel for neuromuscular transmission. (
  • The calcium channel isoform mediating neuromuscular transmission in fish remains an open question, but zebrafish is ideally suited to address this question due to the combination of paired motor neuron-target muscle recording technique ( Wen and Brehm, 2005 , 2010 ) and our identification of a calcium channel mutant line with greatly compromised synaptic transmission. (
  • Using paired nerve-muscle recordings we found that, as it is in frogs, evoked release at the NMJ is effectively blocked by ω-conotoxin GVIA, pointing to a N-type channel as the principle mediator of neuromuscular transmission in zebrafish. (
  • However, positional cloning from the zebrafish mutant line tb204a identified a mutation in a P/Q-type calcium channel as responsible for compromised neuromuscular transmission. (
  • Modulation of calcium channels of twitch skeletal muscle fibres of the frog by adrenaline and cyclic adenosine monophosphate. (
  • Of particular significance has been the distinction between the calcium channel isoforms mediating synaptic transmission at certain peripheral and central synapses. (
  • In addition, similar to the mechanism of action of gabapentin, a commonly used medication for neuropathic pain, phenibut may decrease the activity of voltage-dependent calcium ionic channels [ 1 , 2 ]. (
  • Phenibut ( β -phenyl- γ -aminobutyric acid) is a gamma-aminobutyric acid subtype b (GABA-B) agonist that has both anxiolytic and nootropic activity. (
  • Transient receptor potential melastatin subtype 8 (TRPM8) is a mild cold‐sensing nonselective cation channel that is activated by menthol. (
  • Rat aortic ring experiments were carried out to investigate the role of nitric oxide (NO) in the reciprocal regulation model of receptor and store operated calcium entry. (
  • The work described in this thesis set out to determine the extent to which Ca2 + entry through the store operated pathway contributes to agonist-induced contraction. (
  • It is the first positive inotropic agent shown to act specifically and directly on calcium channels. (
  • 8. The method of claim 7 , wherein the compound is selected from the group consisting of steroid agonists and partial agonists. (
  • Two types of calcium channels in single smooth muscle cells from rabbit ear artery studied with whole-cell and single-channel recordings. (
  • Calcium chloride moderates nerve and muscle performance by regulating the action potential excitation threshold. (
  • Hyposmotically activated chloride channels in cultured rabbit non-pigmented ciliary epithelial cells. (