Angiotensin II receptor blockBeta-blockersAntagonistsSerum potassiumCCBsCurrentsActivated Potassium CurrentInhibitionInhibitorsActivation of potassium channelsExtracellularNeuronsElectrophysiologyAlpha blockersCardiacPoreVoltage-dependent2020Pharmacology and Experimental TherapeuticsConductanceVasoconstrictionLQTSEuropean Journal of PharmacologyContractionsSodium channelsToxinInhibitsConcentrationRelaxationProlongationMicePatientsCardiovascularMutationsSelectivityPropranololConductionOpenerArticleCurrentContributionGenesSulfonylureasDrugsDependentTherapeuticsMelatonin2000Proteins10.1371TreatmentInvolvement
Angiotensin II receptor block3
- We conducted a meta-analysis to explore the benefits of angiotensin-converting enzyme inhibitors (ACEIs)/angiotensin II receptor blockers (ARBs) combined with calcium channel blockers (CCBs) on metabolic, renal, and cardiovascular outcomes in hypertensive patients. (unboundmedicine.com)
- Angiotensin-converting enzyme (ACE) inhibitors and angiotensin II receptor blockers (ARBs) keep your blood vessels from narrowing as much and allows blood to move through them with less pressure. (medlineplus.gov)
- Treatment is strict glucose control, angiotensin inhibition (using angiotensin-converting enzyme [ACE] inhibitors or angiotensin II receptor blockers [ARBs]), and control of blood pressure and lipids. (msdmanuals.com)
Beta-blockers5
- Some drugs (eg, beta-blockers) have potential adverse effects when discontinued abruptly and should be given parenterally in the perioperative period. (medscape.com)
- Beta-blockers provide the single best therapy for prevention of ischemia during the perioperative period. (medscape.com)
- Beta blockers help your heart beat slower and with less force. (medlineplus.gov)
- Beta blockers are typically used only as a backup option or if you also have certain other conditions. (medlineplus.gov)
- Beta Blockers: Do They Cause Weight Gain? (medlineplus.gov)
Antagonists4
- The transient potassium-induced contraction was inhibited less effectively by the calcium antagonists. (aspetjournals.org)
- Dungan, K. W. Pharmacological and toxicological properties of two new β-adrenergic receptor antagonists Journal of Pharmacology and Experimental Therapeutics (1965), 149(2), 161-73. (aksci.com)
- The most common of drugs used are GABAA receptor antagonists and potassium channel blockers (notably 4-aminopyridine). (ox.ac.uk)
- No patient had a history of symptomatic ventricular arrhythmia or was receiving antiarrhythmic agents, calcium channel antagonists, or β-blockers. (elsevierpure.com)
Serum potassium3
- A significant increase of serum potassium was observed. (unboundmedicine.com)
- Following surgery, a marked control of his hypertension with calcium channel blockers and normalization of the serum potassium, renin or aldosterone levels were reached. (bioscientifica.com)
- There was no significant change in serum potassium concentration during magnesium administration. (elsevierpure.com)
CCBs4
- Calcium channel blockers (CCBs) are drugs in clinical use for hypertension and other heart pathologies. (hindawi.com)
- Calcium channel blockers (CCBs) are a class of drugs that act by selective inhibition of calcium influx through cellular membranes. (hindawi.com)
- Calcium entry blockers, or calcium channel blockers - CCBs for short - are vasodilators, or medications that promote dilation of blood vessels. (osmosis.org)
- Calcium channel blockers (CCBs) are a class of drugs that cause vasodilation, and are mainly used to treat high blood pressure and angina pectoris . (osmosis.org)
Currents6
- Examples of voltage-gated channel blockers include: Linopirdine XE-991 Spooky toxin (SsTx) Potassium channel Potassium channel opener Amiodarone also blocks CACNA2D2-containing voltage gated calcium channels works by selectively blocking the rapid component of the delayed rectifier outward potassium current (IKr) blocks potassium channels of the hERG-type Primarily inhibits outward voltage-gated Kv2.1 potassium channel currents. (wikipedia.org)
- Apamin-sensitive calcium-activated potassium currents in rabbit ventricles with chronic myocardial infarction. (harvard.edu)
- Cerebellar ataxia by enhanced Ca(V)2.1 currents is alleviated by Ca2+-dependent K+-channel activators in Cacna1a(S218L) mutant mice. (harvard.edu)
- In the present study, two new peptides, phrixotoxins PaTx1 & PaTx2 (29-31 amino acids), which potently block A-type potassium currents, have been purified from the venom of the tarantula Phrixotrichus auratus. (smartox-biotech.com)
- 6. It was concluded that phrixotoxins, are new & specific blockers of Kv4.3 & Kv4.2 potassium currents, & hence of I(to1) that will enable further studies of Kv4.2 & Kv4.3 channel &/or I(to1) expression. (smartox-biotech.com)
- We previously reported that physiological concentrations of some estrogens partially suppress the hERG channel currents by interacting with the S6 residue F656 and increase the sensitivity of hERG blockade by E-4031. (elsevierpure.com)
Activated Potassium Current1
- Case Report on: Very Early Afterdepolarizations in HiPSC-Cardiomyocytes-An Artifact by Big Conductance Calcium Activated Potassium Current (Ibk,Ca). Cells. (harvard.edu)
Inhibition6
- It is a non-selective competitive beta-adrenergic receptor blocker that also exhibits Class III antiarrhythmic properties by its inhibition of potassium channels. (aksci.com)
- Conclusions: Our data suggest that voltage-dependent K+ channel inhibition with 4-aminopyridine treatment restores blood pressure and increases survival in the Wistar rat model of anaphylactic shock. (uaeu.ac.ae)
- Muscarinic agents also can induce epileptiform synchronization in vitro, and include potassium channel inhibition amongst their cellular actions. (ox.ac.uk)
- Inhibition of K + -conductance through the human ether-a-go-go related gene (hERG) channel leads to QT prolongation and is associated with cardiac arrhythmias. (elsevierpure.com)
- Loperamide's inhibition of the INa channel and hERG-mediated IKr are the most likely basis for this cardiac electrophysiological toxicity at overdose exposures. (bvsalud.org)
- The cardiac toxic effects of loperamide at the overdoses could be aggravated by co-medication with other drug(s) causing ion channel inhibition. (bvsalud.org)
Inhibitors3
- Owing to their superior pharmacokinetic and pharmacodynamic profiles, potassium-competitive acid blockers (P-CABs) score over proton pump inhibitors (PPIs) in the treatment of gastric acid-related disorders and may provide clinical benefit in the management of these conditions. (helicojournal.org)
- As the specific mechanisms behind this phenomenon are unknown, spermatozoa from mice were screened for sensitivities to inhibitors known to affect specific channels involved in volume regulation of somatic cells. (smartox-biotech.com)
- The main groups include sodium channel blockers, calcium current inhibitors, gamma-aminobutyric acid (GABA) enhancers, glutamate blockers, carbonic anhydrase inhibitors, hormones, and drugs with unknown mechanisms of action (see the image below). (medscape.com)
Activation of potassium channels2
- This finding suggests that G protein-coupled estrogen receptor mediates the increase in frequency of ureteral phasic contractions induced by E2 via activation of potassium channels, while E2 alters the amplitude of these contractions through an unknown mechanism. (edu.au)
- The inhibitory action of ChTX suggests part of the cGMP-insensitive component involves the activation of potassium channels, a suggestion supported by the inhibitory actions of 4-AP and IbTX in the absence of cGMP. (ox.ac.uk)
Extracellular1
Neurons3
- Accordingly, the voltage-dependent potassium current is likely to play a leading role in the temperature-dependent changes in the firing patterns in Aplysia neurons. (kjpp.net)
- Effects of calcium-activated potassium channel modulators on afterhyperpolarizing potentials in identified motor and mechanosensory neurons of the medicinal leech. (harvard.edu)
- Many structures and processes are involved in the development of a seizure, including neurons, ion channels, receptors, glia, and inhibitory and excitatory synapses. (medscape.com)
Electrophysiology1
- We used intracellular quaternary ammonium blockers, electrophysiology and X-ray crystallography to locate the voltage-dependent gate in MthK potassium channels from Methanobacterium thermoautotrophicum. (cornell.edu)
Alpha blockers1
- Bitherapy by calcium channel blockers and alpha blockers was given. (peertechzpublications.org)
Cardiac6
- Potassium channel blockers used in the treatment of cardiac arrhythmia are classified as class III antiarrhythmic agents. (wikipedia.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)
- KATP channels also are found in the heart where they are involved in the response to cardiac ischemia: they also are blocked by phentolamine. (ox.ac.uk)
- Our results suggest that this may be because Kir6.2, which is expressed in the heart, forms the pore of the cardiac KATP channel. (ox.ac.uk)
- This is especially so for long QT syndrome (LQTS), which is caused by perturbation of ion channel function, and can lead to fainting, malignant arrhythmias and sudden cardiac death. (worktribe.com)
- These rare diseases are often the underlying cause of sudden cardiac death in young individuals and result from mutations in several genes encoding ion channels or proteins involved in their regulation. (cdc.gov)
Pore2
- The former is an ATP-sensitive K+-selective pore, whereas SUR1 is a channel regulator that endows Kir6.2 with sensitivity to sulfonylureas. (ox.ac.uk)
- Kinetic analysis of tetrabutylammonium block of single MthK channels combined with X-ray crystallographic analysis of the pore with tetrabutyl antimony unequivocally determined that the voltage-dependent gate, like the C-type inactivation gate in eukaryotic channels, is located at the selectivity filter. (cornell.edu)
Voltage-dependent3
- 4-aminopyridine or related voltage-dependent K + channel blockers could be a useful additional therapeutic approach to treatment of refractory anaphylactic shock. (uaeu.ac.ae)
- These results imply that channels potentially involved in volume regulation of murine spermatozoa include the voltage-dependent Kv1.4 (also known as KCNA1), Kv1.5 (KCNA5), Kv4.1 (KCND1), Kv4.2 (KCND2), Kv4.3 (KCND3), mink (KCNE1), & acid-sensitive TASK2 (KCNK5) & TASK3 (KCNK9). (smartox-biotech.com)
- The voltage-dependent gate in MthK potassium channels is located at the selectivity filter. (cornell.edu)
20201
- Atlanta, Ga. (31 August 2020, 7am ET) - UCB, a global biopharmaceutical company, today announced the publication of the Phase 3 study results of VIMPAT ® (lacosamide) CV as adjunctive treatment for uncontrolled primary generalized tonic-clonic seizures (PGTCS), in the Journal of Neurology, Neurosurgery & Psychiatry. (ucb-usa.com)
Pharmacology and Experimental Therapeutics2
- Thank you for sharing this Journal of Pharmacology and Experimental Therapeutics article. (aspetjournals.org)
- Message Body (Your Name) thought you would be interested in this article in Journal of Pharmacology and Experimental Therapeutics. (aspetjournals.org)
Conductance3
- 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)
- The single-channel conductance is unaffected. (ox.ac.uk)
- Discovery of Novel Activators of Large-Conductance Calcium-Activated Potassium Channels for the Treatment of Cerebellar Ataxia. (harvard.edu)
Vasoconstriction1
- Potassium channel blockers, such as 4-aminopyridine, induce vasoconstriction. (uaeu.ac.ae)
LQTS3
- specific beta-blocker agents may provide greater protection than other agents in specific LQTS genotypes. (tau.ac.il)
- blockers are the mainstay treatment for patients with LQTS, functioning by reducing heart rate and arrhythmogenesis. (worktribe.com)
- blocker medication, propranolol, had a marginal effect on APD in the LQTS-hiPSC-CMs. (worktribe.com)
European Journal of Pharmacology2
Contractions1
- Studies were performed on isolated cerebral and peripheral arterial segments from the rat to define contractile receptors for 5-hydroxytryptamine (5-HT) and to elucidate the responses to calcium channel blockers in relation to their effects on potassium-induced contractions. (aspetjournals.org)
Sodium channels2
- These action potentials start automatically when sodium channels slowly let in a stream of sodium ions, which causes the membrane potential of the pacemaker cells to become more positive. (osmosis.org)
- The firing of an action potential by an axon is accomplished through sodium channels. (medscape.com)
Toxin1
- K v 1, K v 2 and K v 3 channel subfamilies are insensitive to this toxin. (smartox-biotech.com)
Inhibits1
- The researchers discovered that the compound VU573 (pictured) inhibits mosquitoes' inward-rectifying potassium channels. (chemistryviews.org)
Concentration1
- Also the (tonic) contraction induced by high potassium concentration was attenuated, with the same relative potency as in the presence of 5-HT except for cyproheptadine, which was less efficient than nimodipine. (aspetjournals.org)
Relaxation5
- Based on the solutions of these equations and potassium channel blocker experiments, we found that, as temperature increases, the maximum value of the potassium channel relaxation time constant, Ք n (t) increases, but the maximum value of the probabilities of openings for activation of the potassium channels, n(t) decreases. (kjpp.net)
- 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)
- 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)
- 1 mM), an inhibitor of voltage-gated potassium channels (Kv), failed to modify DEA NONOate-evoked relaxation. (ox.ac.uk)
- However, the contribution made to relaxation by potassium channels appears to be unmasked following pharmacological attenuation of cGMP-dependent signalling pathways. (ox.ac.uk)
Prolongation1
- Potassium channel blockers exhibit reverse use-dependent prolongation of the action potential duration. (wikipedia.org)
Mice1
- Numerous experiments have been carried out in mice and rabbits using hyaluronic acid, tacrolimus, cyclosporin A, melatonin, vitamin B12, methylprednisolone, riluzole and potassium and calcium channel blockers. (intechopen.com)
Patients2
Cardiovascular1
- Journal of Cardiovascular Pharmacology , 18 (2), 190-197. (elsevierpure.com)
Mutations2
- LQTS2 is caused by mutations in KCNH2, a gene whose protein product contributes to IKr (also known as HERG), which is the predominant repolarizing potassium current in CMs. (worktribe.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)
Selectivity2
- Blockers bind in an aqueous cavity between two putative gates: an intracellular gate and the selectivity filter. (cornell.edu)
- Thus, these blockers directly probe gate location--an intracellular gate will prevent binding when closed, whereas a selectivity filter gate will always allow binding. (cornell.edu)
Propranolol1
- All three drugs showed tachycardia that was antagonized by a β-blocker, propranolol. (elsevierpure.com)
Conduction2
- Potassium channel blockers are agents which interfere with conduction through potassium channels. (wikipedia.org)
- Since these agents do not affect the sodium channel, conduction velocity is not decreased. (wikipedia.org)
Opener1
- These results indicate that NIP-121 has a potent and long-lasting antihypertensive effect that may largely be produced by its activity as a potassium channel opener. (elsevierpure.com)
Article1
- Therefore, it is important to know the value of the lowest possible estimate in this survey that is considered reliable, so as not to present data in a journal article or paper that may be unreliable. (cdc.gov)
Current1
- However, APD could be significantly reduced by up to 19% with compounds that enhanced the IKr current by direct channel binding or by indirect mediation through the PPAR? (worktribe.com)
Contribution1
- 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)
Genes1
Sulfonylureas1
- Sulfonylureas, such as gliclazide, are ATP-sensitive potassium channel blockers. (wikipedia.org)
Drugs2
- Some antiepileptic drugs work by acting on combination of channels or through some unknown mechanism of action. (medscape.com)
- How Do Beta Blocker Drugs Affect Exercise? (medlineplus.gov)
Dependent2
- Potassium channels whose activation is dependent on intracellular calcium concentrations. (harvard.edu)
- Electrophysiological experiments revealed that melatonin decreased salt-induced K + efflux (a critical determinant of plant salt tolerance) in a dose- and time-dependent manner and reduced sensitivity of the plasma membrane K + -permeable channels to hydroxyl radicals. (edu.au)
Therapeutics1
- в журнале International Journal of Peptide Research and Therapeutics , издательство Springer Verlag (Germany) , том 23, № 2, с. (ac.ru)
Melatonin1
- These beneficial effects of melatonin were abolished by NADPH oxidase blocker DPI. (edu.au)
20001
- a very potent inhibitor of the rat Kv1.3 voltage-gated potassium channel Lenz TL, Hilleman DE (July 2000). (wikipedia.org)
Proteins1
- The beta cell KATP channel is a complex of two proteins: Kir6.2 and SUR1. (ox.ac.uk)
10.13711
- PLoS ONE 6(3): e17176 and is available at: 10.1371/journal.pone.0017176. (purdue.edu)
Treatment3
- Dalfampridine, A potassium channel blocker has also been approved for use in the treatment of multiple sclerosis. (wikipedia.org)
- A treatment option for downbeat nystagmus (DBN), a common form of acquired fixation nystagmus that often occurs with cerebellar degeneration, is low doses of the potassium channel blocker 4-aminopyridine (4-AP). (herts.ac.uk)
- Sodium channel blockers such as mexiletine, flecainide, and ranolazine could be treatment options in LQT3. (tau.ac.il)
Involvement1
- this means that at higher heart rates, when there is increased involvement of the slow K channels, dofetilide has less of an action potential-prolonging effect. (wikipedia.org)