Membrane Transporters-Ion Channels

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  1. SGLT2 inhibitor

    EGT1442 is a potent and selective SGLT2 inhibitor.
  2. ATPase inhibitor

    Oligomycin A is a mitochondrial ATPase inhibitor. Oligomycin A inhibits ATP5 (mitochondrial ATPases, F1F0) bound to the cell membrane.
  3. MDR1/P-gp Inhibitor

    PSC-833 is a kind of P-glycoprotein (P-gp) modulator that inhibits P-gp-mediated multidrug-resistance (MDR).
  4. ATPase inhibitor

    Bafilomycin A1 prevents maturation of autophagic vacuoles by inhibiting fusion between autophagosomes and lysosomes in rat hepatoma cell line, H-4-II-E cells.
  5. Cynarin is a phenolic compound found in artichoke. It has antioxidant and choleretic properties. It is a potential immunosuppressive agent.
  6. Resibufogenin is a specific Na+/K+-ATPase inhibitor.
  7. Cinobufagin is a specific Na+/K+-ATPase inhibitor. About as active as ouabain
  8. Sodium channel blocker

    Nicainoprol is a fast-sodium-channel blocking drug, which is a potent antiarrhythmic agent.
  9. T-type Ca2+ channel blocker

    ABT-639 is a novel, peripherally acting, selective T-type Ca2+ channel blocker.
  10. K(Ca) 3.1 channel blocker

    NS6180 is a novel potent and selective KCa3.1 channel inhibitor(IC50= 9 nM) prevents T-cell activation and inflammation.
  11. K+ channel blocker?€?

    E-4031 dihydrochloride is a selective blocker of KV11.1 (hERG) channels; inhibits the rapid delayed-rectifier K+ current (IKr).
  12. CFTR chloride channel inhibitor

    PPQ-102 is a compound that targets intracellular nucleotide binding domain(s) of CFTR and inhibits CFTR- mediated chloride current in a voltage-dependent and reversible manner.
  13. Sodium channel blocker

    Raxatrigine (GSK1014802) is a novel sodium channel blocker and is an effective anticonvulsant agent. In rats, GSK1014802 (20 - 80 mg/kg p.o.) attenuated the deficit in reversal learning induced by phencyclidine (PCP) in a dose-dependent way, which suggested the potential of GSK1014802 in the treatment of cognitive symptoms of schizophrenia. GSK2 was also a potent inhibitor of human MAO-B with pIC50 value of 7.96 but did not inhibit human MAO-A.
  14. EAAT1 inhibitor

    UCPH 101 is a selective non-substrate inhibitor of EAAT1 (IC50 values are 660, >300000 and >300000 nM for EAAT1, EAAT2 and EAAT3 respectively).
  15. AMPA Receptor Antagonist

    NBQX is a potent, selective and competitive AMPA receptor antagonist.
  16. intracellular Ca2+ handling modulator

    Caldaret is an intracellular Ca2+ handling modulator that acts through reverse mode Na+/Ca2+ exchanger inhibition.
  17. TRPV1 receptor antagonist

    A-889425 is a selective TRPV1 receptor antagonist. A-889425 blocks TRPV1 channels with an IC50 of 335 nM (rat) and 34 nM (human).
  18. AMPA receptor modulator

    Farampator has been investigated for its effect on AMPA receptors and researched for potential use in the treatment of schizophrenia and Alzheimer's Disease. It was found to improve short-term memory, but impaired episodic memory.
  19. Sodium channel blocker

    Encainide HCl is a sodium channel blocker and class Ic antiarrhythmic. Encainide is a non-chiral antiarrhythmic and benzanilide derivative.
  20. Sodium channel blocker

    Disopyramide is an antiarrhythmic (class IA) and a sodium channel blocker.
  21. Ca2+ release inhibitor

    Dantrolene sodium is a muscle relaxant that acts by abolishing excitation-contraction coupling in muscle cells, probably by action on the ryanodine receptor.
  22. KCa2.1 channels activator

    GW 542573X is an activator of small-conductance Ca2+-activated K+ channels (KCa2).
  23. SGLT2 inhibitor

    Remogliflozin inhibits the sodium-glucose transport (SGLT2) proteins, which are responsible for glucose reabsorption in the kidney.
  24. ATP synthase inhibitor

    Oligomycin is a macrolide that acts as a specific inhibitor of the mitochondrial ATP-synthase and blocks oxidative phosphorylation.
  25. SERCA inhibitor

    Cyclopiazonic acid is an inhibitor of SERCA (endoplasmic reticulum Ca2+-ATPase) which induces the release of intracellular stored Ca2+, without increasing IP3 levels.
  26. NHE3 inhibitor

    Tenapanor acts as an inhibitor of the sodium-proton exchanger NHE3. This antiporter protein is found in the kidney and intestines, and normally acts to regulate the levels of sodium absorbed and secreted by the body.
  27. H3R antagonist/TRPV1 antagonist

    ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist.
  28. Na(+)/H(+) exchange inhibitor

    ENIPORIDE is a potent Na+/H+ exchange inhibitor.
  29. MCT1 inhibitor

    AZD3965 is a selective inhibitor of monocarboxylate transporter 1 (MCT1) with a binding affinity of 1.6 nM, is 6 fold selective over MCT2 and does not inhibit MCT4 at 10 μM.
  30. TRPV4 blocker

    GSK2193874 was identified as a selective, orally active TRPV4 blocker that inhibits Ca(2+) influx through recombinant TRPV4 channels and native endothelial TRPV4 currents.
  31. proton pump inhibitor

    Tenatoprazole is a prodrug of the proton pump inhibitor (PPI) class, which inhibits proton transport with IC50 of 3.2 uM.
  32. Calcium channel blocker

    (S)-Amlodipine is a (S)-Enantiomer of Amlodipine and a dihydropyridine calcium channel blocker with activity resides mainly in the (-)-isomer.
  33. 20-HETE is a potent vasoconstrictor produced in vascular smooth muscle (VSM) cells.
  34. serotonin reuptake inhibitor

    Azaphen is a potent inhibitor of the reuptake of serotonin.
  35. Glycine reuptake inhibitor

    RG1678 (Bitopertin) is a potent and noncompetitive glycine reuptake inhibitor (GlyT1).
  36. Calcium-Sensing Receptor Antagonist

    Calcium-Sensing Receptor Antagonists I is an antagonist of calcium-sensing parathyroid hormone receptors.
  37. M2 ion channel blocker is capable of inhibiting and blocking the activity of M2 ion channel. Antiviral agents.
  38. Slows neuronal Na+ channel inactivation

    beta-Pompilidotoxin is a peptide with the sequence H2N-Arg.
  39. Na+-glucose transporter inhibitor

    T-1095 is a potent and selective inhibitor of Na+-glucose cotransporters (SGLTs).
  40. TMEM16A Inhibitor

    T16Ainh-A01 is a selective TMEM16A calcium-activated chloride channel inhibitor that strongly inhibits chloride current in salivary gland cells.
  41. ATPase and GTPase inhibitor

    Etidronate Disodium is a bisphosphonate bone resorption inhibitor.
  42. hERG1 potassium channel activator

    KB130015 is a novel activator of hERG1 potassium channels, blocking native and recombinant hERG1 channels at high voltages, but activating them at low voltages.
  43. AMPA antagonist

    YM90K hydrochloride is a selective AMPA receptor antagonist that delays neuronal death in a global ischemia model and cerebral infarction in a focal ischemia model following postischemic administration.
  44. Linoleylethanolamide is an endocannabinoid that also binds to TRPV1 (Ki = 5.60 uM).
  45. TRPA1 activatior/TRPM8 blocker

    Cannabichromene is a major non-psychotropic phytocannabinoid that inhibits endocannabinoid inactivation and activates the transient receptor potential ankyrin-1 (TRPA1). Both endocannabinoids and TRPA1 may modulate gastrointestinal motility.
  46. TRPV1 modulator

    MRS1477 is a TRPV1 positive allosteric modulator.
  47. KV7.2/7.3 activator

    ICA-110381 is a KV7.2/7.3 activator with EC50 of 0.38 uM.
  48. AMPA/kainate receptor antagonist

    Talampanel is a non-competitive antagonist of AMPA-receptor.
  49. TRPV1 antagonist

    Mavatrep is an orally bioavailable TRPV1 antagonist (Ki=6.5 nM), exhibits minimal effect on the enzymatic activity (IC50 > 25 μM) of CYP isoforms 3A4, 1A2, and 2D6.
  50. Calcium Channel Activator

    Bay K 8644 is a potent, selective activator of L-type Ca2+ channel with IC50 of 17.3 nM.

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