Potassium Channel

Nigericin sodium salt is an antibiotic, an NLRP3 activator, and a cationic ion carrier. Nigericin sodium triggers the activation of the NALP3 inflammasome, which inhibits Golgi function and suppresses the growth of Gram-positive bacteria.

Halothane (Anestan) is a nonflammable, halogenated, hydrocarbon anesthetic that provides relatively rapid induction with little or no excitement. Analgesia may not be adequate. NITROUS OXIDE is often given concomitantly. Because halothane may not produce sufficient muscle relaxation, supplemental neuromuscular blocking agents may be required.

Minoxidil sulfate (U-58838) is the active metabolite required to exert the vasodilatory and hair growing effects of minoxidil.

Ropivacaine (LEA-103 HCl) is a local anaesthetic drug belonging to the amino amide group.

Cholesterol Myristate (Cholesteryl Myristate) is a natural steroid found in traditional Chinese medicine that interacts with various ion channels, including the GABAA receptor, nicotinic acetylcholine receptor, and the inward-rectifier potassium ion channel.

(±)-Naringenin (Naringenine) is a natural product. It displays vasorelaxant effect on endothelium-denuded vessels via the activation of BKCa channels in myocytes.

Dimethindene (Dimetindeno) is a selective antagonist of H1 receptor and blocks K+ current. Dimethindene exhibits antihistamine and anticholinergic effects.

CHET3 is a TASK-3 inhibitor that can be used to study pain.

UK 66914 is a K(+) channel blocker for the study of cardiac arrhythmias.

Phe-Met-Arg-Phe, amide acetate dose dependently (ED50=23 nM) activates a K+ current in the peptidergic caudodorsal neurons. This peptide appears to localize with neuropeptide Y in some regions of the brain.

AVE1231 is a TASK-1 channel blocker that inhibits TASK-1 and can be used in the study of atrial fibrillation.

Apamin acetate (Apamine acetate) is a selective Ca2+-activated blocker of K+ (SK) channels, an 18-amino acid peptide neurotoxin found in bee toxins.Apamin acetate enhances synapse growth and regeneration following laceration injury to cortical neurons.Apamin acetate has anti-inflammatory and anti-fibrotic effects.

Bisaramil hydrochloride (Bisaramil) is a novel diazabicyclononane antiarrhythmic compound that inhibits the generation of free radicals.Bisaramil hydrochloride blocks sodium currents and inhibits the slow Ca(2+) action potential induced by isoproterenol in K(+)-depolarized muscle.

GAL-021 sulfate is a BKCa channel blocker that inhibits the analgesic effects of opioids and is used in the study of respiratory control diseases.

XE991 is a novel and selective Kv7 (KCNQ) channel blocker.XE 991 dihydrochloride inhibits Kv7.1 (KCNQ1), Kv7.2 (KCNQ2), Kv7.2 + Kv7.3 (KCNQ3) channels, and M-current, and can be used for the study of neurological diseases.

AVE-0118 is a potassium channel blocker and suppresses persistent atrial fibrillation.

Vesnarinone HCl (OPC-8212 HCl) is an orally active phosphodiesterase 3 (PDE3) inhibitor.Vesnarinone HCl modulates calcium and potassium ions, increasing calcium flux and decreasing potassium flux.Vesnarinone HCl is a new positive inotropic compound that enhances myocardial contractility and can be be used in heart failure studies.

BMS-394136 (BMS 394136) is a KV1.5 antagonist for the treatment of cardiovascular diseases such as arrhythmias and atrial fibrillation.

BMS-919373 is a potassium channel Kv1.5 (KCNA5) inhibitor for atrial fibrillation and acute coronary syndrome.

Bupivacaine hydrochloride monohydrate is a potent NMDA receptor inhibitor of sodium, L-calcium, and potassium channels.Bupivacaine hydrochloride monohydrate inhibits SCN5A channels and is commonly used in the study of chronic pain.

Potassium Channel Activator 1 can be used in studies about the treatment of disorders or conditions wherein the dopaminergic system is disrupted such as mood disorders ADHD, schizophrenia, and other psychotic states.

VU6036720 is a potent and selective inhibitor of the isomeric Kir4.1/5.1.VU6036720 inhibits Kir4.1/5.1 activity by decreasing the channel open-circuit probability and single-channel current amplitude.

(+)-KCC2 blocker 1 is a selective blocker of KCC2 (IC50 = 0.4 μM).

Myomodulin acetate is present in two identified aplysia neurons that contain myomodulin A the ARC motor neuron B16 and the abdominal neuron L10.

KT-362 fumarate is a novel compound that acts as an antagonist of calcium channels, potassium channels and sodium channels.KT-362 fumarate causes vasodilation by affecting intracellular calcium mobilization in atrial muscle cells.KT-362 fumarate has a relaxing effect on femoral and basilar artery strips in rabbits.

Sipatrigine (619C89) is an antiepileptic compound with neuroprotective activity through glutamate release, TREK ion channels, TRESK channels, sodium channels, and calcium channel inhibitors in the CNS, and can be used to study TRESK channels.

Aprikalim (RP 52891) is an adenosine triphosphate potassium channel (KATP) opener that protects against nerve damage in a rabbit model of spinal cord ischemia.Aprikalim inhibits vasoconstriction and inhibits the elevation of [Ca2+]i during myocardial paralysis, and can be used to study cardiovascular disease.

GAL-021 an intravenous BKCa-channel blocker.

Linaprazan (AZD0865) inhibits gastric H+,K+-ATPase by K+-competitive binding with an IC50 of 1.0 μM.

BSH-IN-1 is a potent and covalent inhibitor of gut bacterial recombinant bile salt hydrolases (BSHs; IC50s: 108 nM and 427 nM for B. longum BSH and B. theta BSH).

ML353 (VU0478006) is a selective activator of TREK-1 and TREK-2 and a selective ligand (Ki =18.2 nM) for the mGlu5 Silencing Allosteric Modulator (SAM). ML353 has potential as a solution to the intrinsic activity or pharmacological blockade of SAM in vivo.

PD-118057 is a potent ether associated (hERG) potassium channel activator that shows no activity against hERG. PD-118057 inhibits the excitability of the membrane by activating the hERG channel. PD-118057 is a potential compound for the treatment of delayed repolarization in inherited or acquired long QT syndrome and congestive heart failure.

Gut restricted-7 (GR-7) (GR-7) is a covalent and orally active pan-bile salt hydrolase (BSH) inhibitor. It decreases gut bacterial BSHs and decreases deconjugated bile acid levels in the feces of mice.

Maralixibat Chloride (LUM001 chloride), an apical, sodium-dependent, bile acid transport inhibitor, prevents enterohepatic bile acid recirculation.

5-Hydroxydecanoate sodium is a selective ATP-sensitive K+ (KATP) channel blocker with IC50 of about 30 μM. 5-Hydroxydecanoate sodium is a substrate for mitochondrial outer membrane acyl-CoA synthetase with antioxidant property.

Senicapoc (ICA-17043) is a potent inhibitor of the Gardos channel and ameliorates RBC dehydration in the SAD mouse. Senicapoc blocked Ca2+-induced rubidium flux from human RBCs with an IC50 value of 11 ± 2 nM (CLT IC50 = 100 ± 12 nM) and inhibited RBC dehydration with an IC50 of 30 ± 20 nM. Senicapoc is in treatment of Sickle Cell Disease and Sickle Cell Anemia

Nifedipine (Procardia) is a dihydropyridine calcium channel blocking agent. Nifedipine inhibits the transmembrane influx of extracellular calcium ions into myocardial and vascular smooth muscle cells, causing dilatation of the main coronary and systemic arteries and decreasing myocardial contractility. This agent also inhibits the drug efflux pump P-glycoprotein which is overexpressed in some multi-drug resistant tumors and may improve the efficacy of some antineoplastic agents.

Ursodeoxycholic acid (UDCA) can be used to dissolve gallstones and reduce cholesterol absorption.

Tannic acid (Gallotannic acid) is a novel hERG channel blocker.

Amsacrine (AMSA) (mAMSA) an antineoplastic agent which can intercalate into the DNA of tumor cells. Amsacrine also expresses topoisomerase inhibitor activity, specifically inhibiting topoisomerase II.

Tolbutamide (HLS 831) is a sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE.

Glibenclamide (Glyburide) is an antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide.

Clofilium tosylate is a potassium channel blocker. It induces apoptosis of human promyelocytic leukemia (HL-60) cells via Bcl-2-insensitive activation of caspase-3.

Dronedarone (SR 33589) is an amiodarone analogue which has an effective and promising treatment for Atrial fibrillation.

Repaglinide (AG-EE 623ZW) is a benzoic acid derivative that stimulates insulin secretion from the pancreas and is used in the therapy of type 2 diabetes. Repaglinide has been linked to rare instances of clinically apparent acute liver injury.

1. Oleandrin (Folinerin), the principal cardiac glycoside component of PBI-524, can quantitatively account for regulation of BDNF at both the protein and transcriptional levels. 2. Oleandrin are known to inhibit the Na, K-ATPase pump, resulting in a consequent increase in calcium influx in heart muscle. 3. Oleandrin has stronger anti-proliferative activity in undifferentiated CaCO-2 cells (IC50, 8.25 nM) , causes an autophagic cell death and altered ERK phosphorylation in undifferentiated.

Rosuvastatin (ZD 4522) is an antilipemic agent that competitively inhibits hydroxymethyl-glutaryl-coenzyme A (HMG-CoA) reductase. HMG-CoA reductase catalyzes the conversion of HMG-CoA to mevalonic acid, the rate-limiting step in cholesterol biosynthesis. Rosuvastatin belongs to a class of medications called statins and is used to reduce plasma cholesterol levels and prevent cardiovascular disease.

Astemizole (Laridal) is a synthetic piperidinyl-benzimidazol derivative with antiallergic properties, acts as a reversible competitive inhibitor of histamine H1 receptors, with less anticholinergic effects compared to related agents. It is a long-acting, non-sedative antihistaminic used in the treatment of seasonal allergic rhinitis, asthma, allergic conjunctivitis, and chronic idiopathic urticaria.

BAPTA-AM is a calcium chelator that is cell-permeable and selective, blocking hERG, hKv1.3, and hKv1.5 channels (IC50=1.3/1.45/1.23 μM). BAPTA-AM has a 105-fold higher affinity for Ca2+ than for Mg2+, and can be used for the role of calcium in cell signaling.

Prazosin hydrochloride (Vasoflex) reduces peripheral resistance and relaxes vascular smooth muscles as a selective adrenergic alpha-1 antagonist by a mechanism not completely known. Prazosin hydrochloride is a synthetic piperazine derivative with hypotensive antiadrenergic properties, It is used in the treatment of heart failure, hypertension, pheochromocytoma, Raynaud's syndrome, prostatic hypertrophy, and urinary retention.