Channel blockers potassium channels calcium activated. Medical search. Frequent questions

The blocker of ATP-modulated potassium channels (K(ATP)), glibenclamide (10 microM), and of small conductance calcium-activated potassium channels (SK(Ca)), apamin (30 nM), each failed to affect ODQ-sensitive or -resistant relaxations to DEA NONOate (n=3). (ox.ac.uk)

Discovery of Novel Activators of Large-Conductance Calcium-Activated Potassium Channels for the Treatment of Cerebellar Ataxia. (harvard.edu)
Case Report on: Very Early Afterdepolarizations in HiPSC-Cardiomyocytes-An Artifact by Big Conductance Calcium Activated Potassium Current (Ibk,Ca). Cells. (harvard.edu)
Modulation of small conductance calcium-activated potassium (SK) channels: a new challenge in medicinal chemistry. (ncats.io)
Small-conductance calcium-activated K+ channels are expressed in pancreatic islets and regulate glucose responses. (ncats.io)
Later experiments, in which six different calmodulin-inhibitory drugs were tested on the Ca-activated K conductance of human RBCs, showed that all were potent inhibitors of this conductance and that their effect showed a correlation coefficient of 0.98 with that found on RBC Ca-ATPase, a membrane enzyme known to be activated by calmodulin ( Lackington and Orrego, 1981 ). (conicyt.cl)
Once membrane depolarization is complete, the membrane becomes impermeable to sodium ions again, and the conductance of potassium ions into the cell increases. (medscape.com)

Receptors in the posterior pharynx are then activated to initiate the involuntary phase of deglutition, which involves carefully sequenced contraction of numerous head and neck muscles. (nature.com)
The inward-rectifier potassium channel family (also known as 2-TM channels) include the strong inward-rectifier channels (K ir 2.x), the G-protein-activated inward-rectifier channels (K ir 3.x) and the ATP-sensitive channels (K ir 6.x), which combine with sulphonylurea receptors. (tocris.com)
Activation of micro-opioid receptors by application of morphine or d-Ala(2)-N-Me-Phe(4)-Glycol(5)-enkephalin (DAMGO) potentiates spike frequency adaptation by enhancing the alpha-dendrotoxin-sensitive potassium current. (nih.gov)
An elevation of the intracellular calcium level, which is mediated by N-methyl-D-aspartate receptors and L-type Ca2+ channels both, activates the mitogen-activated protein (MAP) kinase signaling pathway involved in synaptic modification. (asahq.org)
5 MAP kinase has been shown to be activated by calcium influx through both N -methyl-D-aspartate (NMDA) receptors and L-type Ca 2+ channels. (asahq.org)
Conversely, inhibition of PVA neuronal activity using DREADDs (designer receptors exclusively activated by designer drugs) or inactivation of PVA extracellular signal-regulated kinase at the critical time window blunted mechanical hyperalgesia in chronic pain models. (iasp-pain.org)

Potassium channels whose activation is dependent on intracellular calcium concentrations. (harvard.edu)
Changes in intracellular calcium not only modify glial physiology, but they also seem to be involved in complex intercellular communication networks (for review, see Finkbeiner, 1993 ). (jneurosci.org)
Opening these channels hyperpolarizes the smooth muscle, which closes voltage-gated calcium channels and decreases intracellular calcium. (cvpharmacology.com)
It was soon shown that this effect depended on an increase in intracellular calcium (Cai2+) ( Whittam, 1968 ), and that the calcium sensor was located at the inside of the membrane ( Blum and Hoffman, 1972 ). (conicyt.cl)
Most of the drugs that stimulate or inhibit smooth muscle contraction do so by regulating the concentration of intracellular calcium , which is involved in initiating the process of contraction. (britannica.com)

The contribution from cGMP-dependent signalling pathways was examined by exposing arteries to 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (ODQ), a selective inhibitor of soluble guanylyl cyclase, while the contribution through potassium channels was assessed with different sub-type-selective potassium channel blockers. (ox.ac.uk)
Apamin, a selective blocker of the SK channels responsible for part of the slow afterhyperpolarisation reduced, but did not abolish, the amplitude of the post-burst afterhyperpolarisation. (ox.ac.uk)
Potent, reversible, selective K Ca channel inhibitor. (hellobio.com)
Calcium channel blockers (CCBs) are a class of drugs that act by selective inhibition of calcium influx through cellular membranes. (hindawi.com)
This was better defined when recordings were made of single channels in many different preparations in combination with the use of selective blockers. (conicyt.cl)
They work by blocking potassium-selective channels in the nerve membrane, thereby prolonging the electrical impulse in the nerve terminal and increasing the amount of acetylcholine released. (britannica.com)

The expression of c-Fos induced by potassium chloride was also suppressed by dibucaine, tetracaine (concentrations that inhibited 50% of the activity of positive control [IC50s] were 16.2+/-0.2 and 73.2+/-0.7 microM, respectively), and PD 98059, a mitogen-activated/extracellular receptor-regulated kinase inhibitor. (asahq.org)
It has recently been reported that mitogen-activated protein (MAP) kinase (also known as extracellular signal reactive kinase [Erk]) might play an important role in linking membrane depolarization to gene expression in the postsynaptic neurons. (asahq.org)
TASK-1 channels are sensitive to a wide array of physiological and pharmacological mediators that affect their activity such as unsaturated fatty acids, extracellular pH, hypoxia, anaesthetics and intracellular signalling pathways. (ersjournals.com)
This active transport creates a concentration gradient that favors the extracellular diffusion of potassium ions. (medscape.com)

In addition, some clinically used drugs may act via K + channel blockade ( Sanguinetti and Jurkiewicz, 1990 ). (jneurosci.org)
Blockade of potassium channels delay repolarization and prolong the action potential. (pharmacology2000.com)

Apamin-sensitive calcium-activated potassium currents in rabbit ventricles with chronic myocardial infarction. (harvard.edu)
Notably the L-type Ca(2+) channel antagonist, nifedipine, was more effective than apamin at reducing the post-burst afterhyperpolarisation. (ox.ac.uk)
We suggest that Ca(2+) entry through L-type channels during an epileptiform event is selectively coupled to both apamin-sensitive and -insensitive Ca(2+) activated K(+) channels. (ox.ac.uk)
Based on differences in unitary conductances, sensitivity to drugs, and voltage-dependence, this allowed the classification of the channels as small (SK), with unitary conductances of 4 - 14 pS that are blocked by apamin and are insensitive to voltage. (conicyt.cl)

4. The Na(+/)K + ATPase inhibitor ouabain (500 μM) and the K(IR) blocker Ba 2+ (30 μM) neither alone nor in combination inhibited EDHF relaxations. (lu.se)
1 mM), an inhibitor of voltage-gated potassium channels (Kv), failed to modify DEA NONOate-evoked relaxation. (ox.ac.uk)
Dequalinium Chloride (DECA) is a PKC inhibitor and high-affinity blocker CNGA1 channel, and nearly as effective on heteromeric CNGA1+CNGB1 channels. (ncats.io)

Effects of calcium-activated potassium channel modulators on afterhyperpolarizing potentials in identified motor and mechanosensory neurons of the medicinal leech. (harvard.edu)
We show that the Caenorhabditis elegans egl-2 gene encodes an eag K + channel and that a gain-of-function mutation in egl-2 blocks excitation in neurons and muscles by causing the channel to open at inappropriately negative voltages. (jneurosci.org)
Pyramidal neurons in the lateral amygdala discharge trains of action potentials that show marked spike frequency adaptation, which is primarily mediated by activation of a slow calcium-activated potassium current. (nih.gov)
We show here that these neurons also express an alpha-dendrotoxin- and tityustoxin-Kalpha-sensitive voltage-dependent potassium current that plays a key role in the control of spike discharge frequency. (nih.gov)
These results show that micro-opioid receptor activation enhances spike frequency adaptation in lateral amygdala neurons by modulating a voltage-dependent potassium channel containing Kv1.2 subunits, through activation of the phospholipase A(2)-arachidonic acid-lipoxygenases cascade. (nih.gov)
In hypothalamic neurons, modulators such as neuropeptide Y (NPY) and adenosine depress glutamatergic transmission by either a pertussis toxin (PTx)-sensitive G-protein-coupled pathway or by inhibition of voltage-activated calcium channels (VACCs). (jneurosci.org)
These conclusions were, however, apparently contradicted by elegant experiments done on internally-perfused snail neurons, in which neither the injection of calmodulin, nor of the calmodulin-antagonist, trifluoperazine, were able to modify Ca-activated K currents ( Levitan and Levitan, 1986 ). (conicyt.cl)
On the other hand, these recent studies apparently also support the lack of involvement of calmodulin in the gating of the BK channels studied in Helix neurons by Levitan and Levitan (1986) . (conicyt.cl)
The voltage gated Na channels Nav1.7, Nav1.8 and Nav1.9 were found to be selectively up-regulated in rat DRG neurons treated with GM-CSF, which resulted in enhanced excitability. (iasp-pain.org)
GM-CSF activated the Jak2 and Stat3 signaling pathway which promoted the transcription of Nav1.7-1.9 in DRG neurons. (iasp-pain.org)
Here, we showed that GM-CSF promotes bone cancer-associated pain by enhancing excitability of DRG neurons via the Jak2-Stat3-mediated upregulation of expression of nociceptor-specific voltage-gated sodium channels. (iasp-pain.org)
Here, we report that GABAergic (GABA) and dopaminergic (DA) neurons in the ventral tegmental area (VTA) are activated with different temporal patterns during acute and chronic itch. (iasp-pain.org)

Cerebellar ataxia by enhanced Ca(V)2.1 currents is alleviated by Ca2+-dependent K+-channel activators in Cacna1a(S218L) mutant mice. (harvard.edu)
Researchers can save up to 50% on Potassium (K + ) blockers, activators, agonists and antagonists from Hello Bio - they are around half the price of other suppliers. (hellobio.com)
The inhibition could be mimicked by the L-type calcium channel blocker nimodipine (1 μ m ) as well as by protein kinase C (PKC) activators phorbol 12,13-dibutyrate (10 μ m ) and phorbol 12-myristate 13-acetate (500 n m ), and blocked by the PKC inactivator (±)-1-(5-isoquinolinesulfonyl)-2-methylpiperazine (200 μ m ), suggesting a mechanism involving PKC modulation of L-type calcium channels. (jneurosci.org)

KCNQ proteins typically repolarise the plasma membrane of a cell after depolarisation by allowing the export of potassium ions, and are therefore involved in wide-ranging biological functions including cardiac action potentials ( 2 ), neural excitability ( 3 ), and ionic homeostasis in the gastrointestinal tract ( 4 ). (life-science-alliance.org)
Acetylcholine binding causes ion channels to open and allows a local influx of positively charged ions into the muscle fibre, ultimately causing the muscle to contract. (britannica.com)
The concentration gradients are maintained by the sodium/potassium ATP pump (in an energy-dependent process) that transports sodium ions out of the cell and potassium ions into the cell. (medscape.com)
In addition, because the nerve membrane is permeable to potassium ions and impermeable to sodium ions, 95% of the ionic leak in excitable cells is caused by K + ions in the form of an outward flux, accounting for the negative resting potential. (medscape.com)
Ion channels that specifically allow the passage of SODIUM ions. (bvsalud.org)

As a demonstration of the versatility of the Swarm, we also developed an assay measuring cardiac action potential and calcium waveform properties simultaneously under paced conditions using human induced pluripotent stem (iPS) cell-derived cardiomyocytes as an additional counter screen for cardiac toxicity. (frontiersin.org)
The syndrome is caused by changes in the structure and function of certain cardiac ion channels and reduced expression of Connexin 43 (Cx43) in the Right Ventricle (RV), predominantly in the Right Ventricular Outflow Tract (VSVD), causing electromechanical abnormalities. (bvsalud.org)
A variety of specific sodium channel subtypes are involved in serving specialized functions such as neuronal signaling, CARDIAC MUSCLE contraction, and KIDNEY function. (bvsalud.org)

Drugs such as adrenoceptor agonists, muscarinic agonists, nitrates, and calcium channel blockers all affect smooth muscle. (britannica.com)

MK-801 is a non-competitive NMDA-channel blocker and glutamate antagonist that protects the brain of rats from ischaemic damage. (patentpc.com)

influx via the Gardos channel (IK(Ca)) in human erythrocytes. (lu.se)
Increases in excitability could also be achieved by strongly buffering intracellular Ca(2+) or by minimising Ca(2+) influx into the cell, specifically through L-type (but not N-type) voltage operated Ca(2+) channels. (ox.ac.uk)

Similar inhibition is observed with the mouse homolog MEAG, suggesting that inhibition of EAG-like channels may mediate some clinical side effects of this class of antidepressants. (jneurosci.org)
We also discover that activity of KCNQ3 sensitises cancer cells to existing potassium channel inhibitors and that inhibition of KCNQ activity reduces proliferation of GOA cancer cells. (life-science-alliance.org)

Recent studies show that modulation of TASK-1 channels, either directly or indirectly by targeting their regulatory mechanisms, has the potential to control pulmonary arterial tone in humans. (ersjournals.com)
We studied modulation of glutamate-evoked calcium rises in primary astrocyte cultures using fura-2 ratiometric digital calcium imaging. (jneurosci.org)

The KCNQ (potassium voltage-gated channel subfamily Q) family of ion channels encode potassium transporters ( 1 ). (life-science-alliance.org)

TWIK-related acid-sensitive potassium channel 1 (TASK-1 encoded by KCNK3) belongs to the family of two-pore domain potassium channels. (ersjournals.com)
The recently identified 2-pore domain potassium (K2P) channels are believed to be responsible for leak K + currents. (medscape.com)

however, more systematic studies are required to determine which K + channels may be utilized for the clinical treatment of HCC, particularly in the advanced stages of the disease and in cases where patients are resistant to the existing drugs. (spandidos-publications.com)
Kale VP, Amin SG and Pandey MK: Targeting ion channels for cancer therapy by repurposing the approved drugs. (spandidos-publications.com)
Calcium channel blockers (CCBs) are drugs in clinical use for hypertension and other heart pathologies. (hindawi.com)
We modeled: A) the current treatment for LEMS, DAP (a potassium channel blocker), B) a newly developed drug (GV-58) that is a calcium channel gating modifier, and C) a combination of the two drugs. (aps.org)
Potassium-channel openers are drugs that activate (open) ATP-sensitive K + -channels in vascular smooth muscle. (cvpharmacology.com)

Our results are not consistent with the idea that EDHF is K + activating Na + /K + ATPase and K(IR) in this blood vessel. (lu.se)

Involvement of cyclic GMP and potassium channels in relaxation evoked by the nitric oxide donor, diethylamine NONOate, in the rat small isolated mesenteric artery. (ox.ac.uk)
Comes N, Serrano-Albarrás A, Capera J, Serrano-Novillo C, Condom E, Ramón Y Cajal S, Ferreres JC and Felipe A: Involvement of potassium channels in the progression of cancer to a more malignant phenotype. (spandidos-publications.com)

Behavioral and pharmacological studies of these mutants may provide insight into the genetic and mechanistic basis of K + channel dysfunction in vivo . (jneurosci.org)
However, the contribution made to relaxation by potassium channels appears to be unmasked following pharmacological attenuation of cGMP-dependent signalling pathways. (ox.ac.uk)
The Swarm was able to record pseudo-action potentials stably across all 24 objectives and provided pharmacological characterization of diverse sodium channel blockers. (frontiersin.org)

Being effective arterial dilators, potassium-channel openers are used in the treatment of hypertension . (cvpharmacology.com)
Although several potassium-channel openers have been used in research for many years, only one, minoxidil , is approved for humans to treat hypertension. (cvpharmacology.com)

They accomplish this through a number of mechanisms involving automaticity or ion channel dynamics, which in turn affect the propagation of the myocardial electrical impulse via change in conduction velocity or refractory period. (medscape.com)
β-adrenergic receptor blockers increase AV conduction time and increase AV nodal refractoriness, thereby helping to terminate nodal reentrant arrhythmias. (pharmacology2000.com)

The cells were stimulated with either 50 mM KCl or 1 microM ionomycin, and activated MAP kinase was thus immunoprecipitated. (asahq.org)
Higher concentrations of dibucaine and tetracaine were needed to suppress the activation of MAP kinase induced by ionomycin (the IC50 values of dibucaine and tetracaine were 62.5+/-2.2 and 330.5+/-32.8 microM, respectively) compared with potassium chloride (the IC50 values of dibucaine and tetracaine were 17.7+/-1.0 and 70.2+/-1.2 microM, respectively). (asahq.org)

SIGNALS initiated by neurotransmitter release are transferred to the nuclei of the postsynaptic cells to activate specific programs of gene expression, thus influencing synaptic functions. (asahq.org)
We evaluated the effects of varying the spatial distribution of calcium channels and synaptic vesicles in transmission release, studied sub-active zone distribution and function of calcium-activated potassium (BK) channels, predicted changes in action potential shape and its effects on transmitter release. (aps.org)

These SK channels are abundant in the nervous system, where they mediate slow after-hyperpolarizations that modulate excitability. (conicyt.cl)

Mutant EGL-2( gf ) channels exhibited a negative shift in voltage dependence of activation, and both wild-type (WT) and mutant currents were blocked by imipramine. (jneurosci.org)

Very recently, the sequencing of the genes that code for SK, IK and BK channels has allowed a definition of the mechanisms of channel gating and of the participation of calmodulin in it. (conicyt.cl)

Mutations that activate K + channels can lower cellular excitability, whereas those that inhibit K + channels may increase excitability. (jneurosci.org)
Dibucaine and tetracaine at clinical concentrations were found to inhibit the activation of MAP kinase and the expression of c-Fos mediated by L-type Ca2+ channels in PC12 cells. (asahq.org)

Mutations in K + channel sequences can lead to a variety of clinical disorders exemplifying their physiological importance [ 3 ]. (ersjournals.com)
Bestrophin-1 (Best1) is a calcium-activated anion channel identified from retinal pigment epithelium where human mutations are associated with Best's macular degeneration. (en-journal.org)

To evaluate the Swarm screening system, we optimized a series of heterologous optogenetic spiking HEK293 cell assays for several voltage-gated sodium channel subtypes including Nav1.2, Nav1.5, and Nav1.7. (frontiersin.org)

These findings reveal a novel and exploitable role of potassium channels in the advancement of human cancer, and highlight that supplemental treatments for GOAs may exist through KCNQ inhibitors. (life-science-alliance.org)

The relative functional importance of potassium channels and cGMP-dependent pathways in the relaxation of vascular smooth muscle to the novel nitric oxide donor, diethylamine NONOate (DEA NONOate), was investigated in a resistance artery. (ox.ac.uk)
This review summarises our current state of knowledge of the functional role of TASK-1 channels in the pulmonary circulation in health and disease, with special emphasis on current advancements in the field. (ersjournals.com)

See also Beta-Blocker Toxicity and Calcium Channel Blocker Toxicity , as those topics are not covered in this article. (medscape.com)
Adverse effects of beta blocker therapy can lead to fatigue, bronchospasm, depression, impotence, and attenuation of hypoglycemic symptoms in diabetic patients and worsening of congestive heart failure. (pharmacology2000.com)
They are used with a beta-blocker and diuretic to attenuate the reflex tachycardia and retention of sodium and fluid, respectively. (cvpharmacology.com)

Heteromeric channels can also be formed within subfamilies, e.g. (tocris.com)

Potassium (K + ) channels are a large family of membrane proteins that selectively transport K + across the cell membrane. (hellobio.com)

Potassium Channels, Calcium-Activated" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (harvard.edu)

Voltage-sensitive potassium channels play an important role in controlling membrane potential and ionic homeostasis in the gut and have been implicated in gastrointestinal (GI) cancers. (life-science-alliance.org)

We hypothesize that EGL-2( gf ) channels cause behavioral defects through suppression of excitability in critical cells. (jneurosci.org)
Potassium (K + ) channels have an important role in HCC, including regulating the proliferation, migration, invasion and drug resistance of HCC cells. (spandidos-publications.com)
The type III mGluR agonist l -2-amino-4-phosphonobutyrate consistently inhibited 5HT-evoked calcium rises, whereas in a smaller number of cells quisqualate and L-CCG-I showed both inhibitory and additive effects. (jneurosci.org)
To address this challenge, we developed the Swarm TM , a custom designed optical instrument for highly parallelized, multicolor measurements in excitable cells, simultaneously recording changes in voltage and calcium activities at high temporal resolution under optical stimulation. (frontiersin.org)
The presence in human red blood cells (RBCs) of a K permeability that was greatly enhanced by calcium was first reported by Gardós (1958) . (conicyt.cl)
Intermediate (IK) channels, on the other hand, have conductances of 11- 40 pS, are voltage-independent, may be blocked by iberiotoxin and charybdotoxin (Ch Tx), and are found in red and white blood cells, colon, lung, pancreas, and other tissues. (conicyt.cl)

Calcium plays a key role as a second messenger system in astrocytes, both in regulation of many subcellular processes and in long distance intercellular signaling. (jneurosci.org)

Although there are many remaining uncertainties, this review highlights the idea that Best1 is a multifunctional protein, functioning as an anion channel with unique properties as well as a key regulator of various important brain functions. (en-journal.org)
On the other hand, BK channels have an aspartate-rich Ca-sensing region (a «calcium bowl») in the channel protein itself, which confers most of the Ca-sensitivity to the channel, although a second Ca-sensor also seems to be present ( Schreiber and Salkoff, 1997 ). (conicyt.cl)

Teisseyre A, Gąsiorowska J and Michalak K: Voltage-gated potassium channels Kv1.3-potentially new molecular target in cancer diagnostics and therapy. (spandidos-publications.com)
Transcriptional regulation of voltage-gated sodium channels contributes to GM-CSF induced pain. (iasp-pain.org)

K + channels are key regulators of cellular excitability. (jneurosci.org)

Long-acting calcium channel blocker effects may not appear for 18-24 hours, and therefore, children with ingestion should be admitted for 24 hours. (dontforgetthebubbles.com)
Optogenetic assays provide a flexible, scalable, and information rich approach to probe compound effects for ion channel drug targets in both heterologous expression systems and associated disease relevant cell types. (frontiersin.org)
These effects are blocked by beta-adrenergic receptor blockers. (pharmacology2000.com)

All these findings thus seemed to firmly support a role for calmodulin in the gating of these Ca-activated K channels. (conicyt.cl)

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Small conductance calcium-activated potassium channels1

Conductance6

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Inhibitor3

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Nav1.71

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