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. K+ channel blocker?€?

    E-4031 dihydrochloride is a selective blocker of KV11.1 (hERG) channels; inhibits the rapid delayed-rectifier K+ current (IKr).
  9. potassium-competitive acid Blocker

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

    Dronedarone Hydrochloride is a non-iodinated amiodarone derivative that inhibits Na+, K+ and Ca2+ currents.
  11. 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.
  12. 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.
  13. NMDA receptor antagonist

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

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

    NS 309 is a positive modulator of small- and intermediate- conductance Ca2+-activated K+ channels (KCa2 and KCa3.1 channels).
  17. 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.
  18. 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.
  19. KCa2.1 channels activator

    GW 542573X is an activator of small-conductance Ca2+-activated K+ channels (KCa2).
  20. hERG channel activator

    NS-1643 is a Human ether-a-go-go related gene (hERG) KV11.1 channel activator (EC50 = 10.5 uM).
  21. 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.
  22. Potassium channel activator

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

    K+ Channel inhibitor, building block for synthesis of dihydropyrazolopyrimidine inhibitors of Kv1.5 (IKur).
  24. 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.
  25. 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.
  26. 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.
  27. KCNQ2/Q3 potassium channel activator

    ICA-069673 is a KCNQ2/Q3 potassium channel activator with an IC50 of 0.69 μM.
  28. SMN2 splicing modulator

    Branaplam (LMI070) is a highly potent, selective and orally active small molecule SMN2 splicing modulator.
  29. KCC2 inhibitor

    VU 0240551 is a small molecule inhibitor of the neuronal K-Cl cotransporter, KCC2 (IC50 = 560 nM for K+ uptake assay in KCC2-overexpressing cells).
  30. Potassium Channel inhibitor

    Azimilide(NE-10064) is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.
  31. IKs blocker

    JNJ 303 is a potent IKs blocker with an IC50 value of 64 nM.
  32. HERG activator

    RPR-260243 is a novel activator of HERG; modifies HERG currents inhibited by dofetilide (IC50 = 58 nM); little effect on HERG current amplitude and no significant effects on steady-state activation parameters or on channel inactivation processes.
  33. ROMK inhibitor

    MK-7145 is a ROMK inhibitor, with an IC50 of 0.045 μM.
  34. mitoKATP channels

    BMS-191095 is an activators of mitochondrial ATP-sensitive potassium (mitoKATP) channels.
  35. KATP activator

    Levcromakalim ((-)-Cromakalim) is an ATP-sensitive K+ channel (KATP) activator.
  36. Amiodarone is an antiarrhythmic drug for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM.

  37. hERG potassium channel inhibitor

    Cisapride(R 51619) is a nonselective 5-HT4 receptor agonist, it is also a potent hERG potassium channel inhibitor.
  38. potassium channel inhibitor

    VU591 is a potent, selective renal outer medullary potassium channel (ROMK or Kir1.1) inhibitor, with an IC50 of 0.24 μM.
  39. TREK-1 activator

    ML402 is a selective TREK-1 activator.
  40. 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.
  41. 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.
  42. KCC2 antagonist

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

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

    BMS-191011 (BMS-A) is an opener of the large-conductance, Ca2++-activated potassium (maxi-K) channel, effective in stroke models.
  45. 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.
  46. KV7 channel blocker

    DMP-543 (XR-543) is a KV7 channel blocker, also acts as a potent neurotransmitter release enhancer.
  47. 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.
  48. 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.
  49. 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.
  50. 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.

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