Potassium Channels

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  1. Antimalarial

    Quinine is a primary alkaloid of various species of Cinchona, optical isomer of Quinidine and an anti-malarial, skeletal, muscle relaxant.
  2. sodium-potassium pump inhibitor

    Digoxin is a sodium-potassium pump inhibitor.
  3. Ion channel blocker

    Vernakalant Hcl is an investigational mixed ion channel blocker that can terminate acute atrial fibrillation (AF) in humans at 2 to 5 mg/kg and may be more atrial-selective than available agents; in treatment of antiarrhythmic.
  4. Kir7.1 potassium channels blocker

    ML418 is a selective, sub-micromolar pore blocker of Kir7.1 potassium channels. The inward rectifier potassium (Kir) channel Kir7.1 (KCNJ13) is a key regulator of melanocortin signaling in the brain, electrolyte homeostasis in the eye, and uterine muscle contractility during pregnancy.
  5. Kv1.3 blocker

    PAP-1 is a selective inhibitor of Kv1.3, voltage-gated potassium channel. PAP-1 (EC50=2 nM) potently inhibits human T effector memory cell proliferation and delayed hypersensitivity.
  6. Potassium Channel Blocker

    TRAM-34 is a highly selective blocker of intermediate conductance Ca2+-activated K+ channels (KCa3.1) (Kd = 20 nM). Exhibits 200-1500-fold selectivity over KV, BKCa, KCa2, Na+, CRAC and Cl- channels. Suppresses the reactivation of lymphocytes by mitogenic stimuli.
  7. HIF-1α inhibitor

    Minocycline hydrochloride is a broad-spectrum tetracycline antibiotic, acting by binding to the bacterial 30S ribosomal subunit and inhibiting protein synthesis.
  8. potassium-competitive acid Blocker

    TAK-438 is a novel potassium-competitive acid blocker.
  9. K+/Na+/Ca+ Channel Blocker

    Dronedarone Hydrochloride is a non-iodinated amiodarone derivative that inhibits Na+, K+ and Ca2+ currents.
  10. Gardos channel blocker

    Senicapoc (ICA-17043) is a potent and selective Gardos channel blocker with IC50 value of 11 nM. It blocks Ca2+-induced rubidium flux from human RBCs with an IC50 value of 11 nM and inhibits RBC dehydration with IC50 of 30 nM.
  11. Vernakalant is an investigational mixed ion channel blocker that can terminate acute atrial fibrillation (AF) in humans at 2 to 5 mg/kg and may be more atrial-selective than available agents.
  12. NMDA receptor antagonist

    Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker.
  13. Amiodarone hydrochloride is an antiarrhythmic drug for inhibition of ATP-sensitive potassium channel with IC50 of 19.1 μM.
  14. KATP channel antagonist

    Mitiglinide is a blood glucose-lowering drugs, stimulating insulin secretion by closing the ATP-sensitive K+ channels in pancreatic beta-cells.
  15. KCa3.1 channel activator

    NS 309 is a positive modulator of small- and intermediate- conductance Ca2+-activated K+ channels (KCa2 and KCa3.1 channels).
  16. Clofilium tosylate, a potassium channel blocker, induces apoptosis of human promyelocytic leukemia (HL-60) cells via Bcl-2-insensitive activation of caspase-3. Antiarrhythmic agent.
  17. K+ (KATP) channel activator

    Y-26763 is a K+ channel opener and active metabolite of Y-27152. Y-26763 is an ATP-sensitive K+ (KATP) channel activator.
  18. potassium channel activator

    SKA-31 is an activator of KCa2 and KCa3.1 calcium-activated potassium channels.
  19. Potassium Channel activator

    Pinacidil monohydrate, an antihypertensive drug, is a potassium channel activator.
  20. Potassium channel blocker

    Dalfampridine is a potassium channel blocker used to help multiple sclerosis patients walk.
  21. Citronellal or rhodinal or 3,7-dimethyloct-6-en-1-al is a monoterpenoid, the main component in the mixture of terpenoid chemical compounds that give citronella oil its distinctive lemon scent.
  22. potassium-competitive acid blocker

    Vonoprazan (TAK-438 free base) is an orally active potassium-competitive acid blocker which inhibits H+, K+-ATPase activity with an IC50 of 19 nM.
  23. Pirmenol hydrochloride inhibits IK.ACh by blocking muscarinic receptors. The IC50 of Pirmenol for inhibition of Carbachol-induced IK.ACh is 0.1 μM.
  24. Peripheral chemoreceptor agonist

    Almitrine mesylate, a peripheral chemoreceptor agonist, inhibits selectively the Ca2+-dependent K+ channel.
  25. μ- opioid receptor agonist

    Trimebutine Maleate is a drug with antimuscarinic and weak mu opioid agonist effects. Trimebutine Maleate modulates the calcium and potassium channels, relieves abdominal pain in patients with irritable bowel syndrome.
  26. hERG channel activator

    NS-1643 is a Human ether-a-go-go related gene (hERG) KV11.1 channel activator (EC50 = 10.5 uM).
  27. Doxapram inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50 of 410 nM, 37 μM, 9 μM, respectively. Doxapram is a respiratory stimulant. Administered intravenously, doxapram stimulates an increase in tidal volume, and respiratory rate.
  28. Potassium channel activator

    NS1619 is a Bkca opener or large-conductance Ca2+-activated potassium (BKCa, KCa1.1) channel activator.
  29. K+ Channel inhibitor

    K+ Channel inhibitor, building block for synthesis of dihydropyrazolopyrimidine inhibitors of Kv1.5 (IKur).
  30. Wnt/beta-catenin inhibitor

    Hexachlorophene is a potent KCNQ1/KCNE1 potassium channel activator with EC50 of 4.61 ?? 1.29 uM; also is an inhibitor of Wnt/beta-catenin signaling.
  31. Kir2 family channels inhibitor

    ML133 hydrochloride is a selective Kir2 family channels inhibitor, with an IC50 of 1.8 μM at pH 7.4 and 290 nM at pH 8.5.
  32. TREK-1/2 Activator

    ML335 is a potent and selective TREK-1/2 Activator. ML335 is an agonist for OPRM1-OPRD1 heterdimerization with an EC50 of 403 nM, and selectivities vs. OPRM1, OPRD1, and HTR5A of 37, 2.7, and >99, respectively.
  33. TREK-1 activator

    ML402 is a selective TREK-1 activator.
  34. potassium channel (non-GIRK1/X) activator

    VU0529331 is a modestly selective non-GIRK1-containing G protein-gated, inwardly-rectifying, potassium channel (non-GIRK1/X) activator, with EC50s of 5.1 ?M and 5.2 ?M for GIRK2 and GIRK1/2 in HEK293 cells, respectively, also effective on GIRK4 homomeric channel.
  35. KCC2 activator

    CLP290 is an orally available activator of the neuron-specific K+-Cl? cotransporter KCC2, displays potential for treatment of a wide range of neurological and psychiatric indications.
  36. KCC2 antagonist

    VU0463271 is a potent KCC2 antagonist, with an IC50 of 61 nM.
  37. hERG channel activator

    PD-118057 is a human ether-a-go-go-related gene (hERG) channel activator that does not cause hERG blockade.
  38. BKCa channel opener

    BMS-191011 (BMS-A) is an opener of the large-conductance, Ca2++-activated potassium (maxi-K) channel, effective in stroke models.
  39. sAHP channel blocker

    UCL 2077 is a selective slow-afterhyperpolarization (sAHP) channel blocker (IC50 = 500 nM in hippocampal neurons in culture), having minimal effects on Ca2+ channels, action potentials, input resistance and the medium after hyperpolarization.
  40. KV7 channel blocker

    DMP-543 (XR-543) is a KV7 channel blocker, also acts as a potent neurotransmitter release enhancer.
  41. ROMK inhibitor

    VU591 hydrochloride is a potent, selective renal outer medullary potassium channel (ROMK or Kir1.1) inhibitor, with an IC50 of 0.24 μM.
  42. K+ channel opener

    Y-27152, a prodrug of the KATP (Kir6) channel opener Y-26763, is a long-acting K+ channel opener with less tachycardia: antihypertensive effects in hypertensive rats and dogs in conscious state.
  43. Kv7 (KCNQ) channels blocker

    XE 991 dihydrochloride, a Kv7 (KCNQ) channels blocker, potently inhibits Kv7.1 (KCNQ1), Kv7.2 (KCNQ2), Kv7.2 + Kv7.3 (KCNQ3) channel, and M-current with IC50s of 0.75 ?M, 0.71 ?M, 0.6 μM, and 0.98 ?M, respectively.
  44. KATP channel activator

    P-1075 is a potent activator of sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6), with an EC50 value of 45 nM for SUR2B-KIR6 channel activation.
  45. Kv7.2/Kv7.4 channels activator

    ML213 is a selective activator of Kv7.2 and Kv7.4 channels, enhances Kv7.2 and Kv7.4 channels with EC50s of 230 and 510 nM, respectively.
  46. Cl- conductance/hKCa3.1 channel activator

    DCEBIO, a derivative of 1-EBIO, is an extremely potent activator of Cl?? secretion in T84 colonic cells.
  47. potassium channel blocker

    Almokalant is a class III antiarrhythmic drug, acts as a potassium channel blocker, and inhibits a specific component (Ikr) of the time-dependent delayed rectifier K+ current.
  48. KCa3.1 activator

    SKA-121 is a selective KCa3.1 activator. SKA-121 exhibits EC50s of 109 nM and 4.4 μM for KCa3.1 and KCa2.3, respectively.
  49. IKs blocker

    HMR 1556, a chromanol derivative, is a IKs blocker with IC50s of 10.5 nM and 34 nM in canine and guinea pig left ventricular myocytes, respectively.
  50. cyanoguanidine KATP opener

    Naminidil is a cyanoguanidine KATP opener.

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