Membrane Transporters-Ion Channels

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  1. VSCC blocker

    PD173212 is a selective N-type voltage sensitive calcium channel (VSCC) blocker, with an IC50 of 36 nM in IMR-32 assays.
  2. NAADP antagonist and TPC blocker

    trans-Ned 19, a NAADP antagonist and TPC blocker, suppresses the calcium signal in human umbilical vein endothelial cells (HUVEC) and the rat aorta relaxation in response to low histamine concentrations.
  3. CatSper channels blocker

    HC-056456 is an effective but not perfectly-selective blocker of CatSper channels. The [Na+]i rise is slowed by HC-056456 (IC50~3 ?M).
  4. calcium channel blocker

    ACT-709478 is a potent, selective, orally active, and brain penetrating T-type calcium channel blocker. ACT-709478 is used in the research of generalized epilepsies.
  5. Calcium channel blocker

    Berbamine is a calcium channel blocker.
  6. Calcium channel blocker

    (S)-Amlodipine is a (S)-Enantiomer of Amlodipine and a dihydropyridine calcium channel blocker with activity resides mainly in the (-)-isomer.
  7. Cardiac Na+ channel blocker

    Flecainide is a class 1C antiarrhythmic drug especially used for the management of supraventricular arrhythmia; works by blocking the Nav1.5 sodium channel in the heart, causing prolongation of the cardiac action potential.
  8. Calcium channel blocker

    NNC 55-0396, Mibefradil derivative, is a highly selective T-type calcium channel blocker; displays IC50 values of 6.8 and > 100 μM for inhibition of Cav3.1 T-type channels and HVA currents respectively in INS-1 cells.
  9. N-type calcium channel blocker

    NP118809 is a potent N-type calcium channel blockers(IC50= 0.11 uM) ; good selectivity over L-type calcium channels.
  10. Potassium channel blocker

    Cesium chloride is a potassium channel blocker; inhibits the pacemaker current (If) and the hyperpolarization-activated cationic current (Ih). Prevents activation of caspase-3 and neuronal apoptosis in serum- and potassium-deprived cerebellar granule neurons by inactivating GSK-3β.
  11. 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.
  12. L-type calcium channel blocker

    Amlodipin is L-type calcium channel blocker that displays antihypertensive properties. It inhibits Ca2+-induced contractions in depolarized rat aorta (IC50 = 1.9 nM) and displays vasoprotective effects in cardiovascular disease.
  13. L-type calcium channel blocker

    Amlodipine-besylate is L-type calcium channel blocker that displays antihypertensive properties. It inhibits Ca2+-induced contractions in depolarized rat aorta (IC50 = 1.9 nM) and displays vasoprotective effects in cardiovascular disease.
  14. Calcium channel blocker

    Cilnidipine is a dual blocker of L-type voltage-gated calcium channels in vascular smooth muscle and N-type calcium channels in sympathetic nerve terminals that supply.
  15. K+ channel and CFTR Cl- channel blocker

  16. L-type calcium channel blocker.

    Nifedipine is a L-type calcium channel blocker.
  17. calcium channel blocker

    Nisoldipine(BAY-k 5552; Sular) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC50 of 10 nM.
  18. Sodium channel Blocker

    QX 314 chloride is a membrane impermeable quaternary derivative of lidocaine, a voltage-activated Na+ channel blocker
  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. AMPA Receptor Blocker

    IEM 1754 Dihydrobromide is a voltage-dependent open-channel blocker of AMPA receptors.
  21. TRPA1 channel blocker

    TCS 5861528 is a TRPA1 channel blocker and an antagonizer of AITC- and 4-HNE-evoked calcium influx.
  22. 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.
  23. T-type Ca2+ channel blocker

    ABT-639 is a novel, peripherally acting, selective T-type Ca2+ channel blocker.
  24. 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.
  25. Calcium channel blocker

    Mibefradil is a calcium channel blocker with moderate selectivity for T-type Ca2+ channels displaying IC50s of 2.7 μM and 18.6 μM for T-type and L-type currents, respectively.
  26. Calcium channel blocker

    Mibefradil 2Hcl is calcium channel blocker with moderate selectivity for T-type Ca2+ channels displaying IC50 values of 2.7 uM and 18.6 uM for T-type and L-type channels respectively.
  27. T-type Ca2+ channel blocker

    ABT-639 hydrochloride is a novel, peripherally acting, selective T-type Ca2+ channel blocker.
  28. K+ channel blocker?€?

    E-4031 dihydrochloride is a selective blocker of KV11.1 (hERG) channels; inhibits the rapid delayed-rectifier K+ current (IKr).
  29. 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.
  30. dihydropyridine calcium entry blocker

    Lemildipine is a new dihydropyridine calcium entry blocker.
  31. Calcium channel blocker

    Amlodipine aspartic acid impurity is the impurity of Amlodipine aspartic acid. Amlodipine aspartic acid is a calcium channel blocker with antihypertensive and antianginal properties.
  32. CaCC blocker

    Talniflumate is a calcium-activated chloride channel (CaCC) (hCLCA1/mCLCA3) blocker; reduces mucin synthesis and release in cell culture and animal models.
  33. Ca2+-dependent blocker

    TV-519 free base (K201 free base) is a Ca2+-dependent blocker of sarcoplasmic reticulum Ca2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. Antiarrhythmic and cardioprotective properties.
  34. CARC blocker

    GSK-5498A is a selective small molecule blocker of CARC (IC50, 1 μM); inhibits mediator release from mast cells, and pro-inflammatory cytokine release from T-cells in a variety of species.
  35. Na+ channel blocker

    Ralfinamide mesylate (FCE-26742A mesylate) is an orally available Na+ channel blocker derived from α-aminoamide, with function of suppressing pain.
  36. sodium channel blocker

    Levobupivacaine hydrochloride is a sodium channel blocker.
  37. Nav1.8 channel blocker

    PF-01247324 is a selective and orally bioavailable Nav1.8 channel blocker with an IC50 of 196 nM for recombinant human Nav1.8 channel.
  38. NaV1.7 blocker

    XEN907 is a novel spirooxindole NaV1.7 blocker, inhibits hNaV1.7 with IC50 of 3 nM.
  39. AMPA receptor blocker

    gamma-DGG is a competitive AMPA receptor blocker.
  40. HCN channel blocker

    ZD7288 is a selective hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker.
  41. TRPV4 ion channel blocker

    GSK2798745 is a first-in-class, highly potent, selective, orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocker with IC50s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively.
  42. non-voltage dependent calcium channel blocker

    Carboxyamidotriazole (L 651582) is a blocker of non-voltage dependent calcium channel.
  43. IKs blocker

    JNJ 303 is a potent IKs blocker with an IC50 value of 64 nM.
  44. Calcium channel blocker

    Levamlodipine besylate ((S)-Amlodipine besylate) is a powerful dihydropyridine calcium channel blocker, possessing vasodilation properties and used in the treatment of hypertension and angina.
  45. dual T-type and L-type calcium channel blocker

    Efonidipine Hcl (NZ-105) is a dual T-type and L-type calcium channel blocker (CCB).
  46. Calcium channel blocker

    Verapamil is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor.

  47. potassium currents blocker

    Gliclazide is used as an antidiabetic. It is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. 

  48. blocker of fast Na+-dependent action potentials and voltage-dependent

    Lidocaine N-ethyl bromide is a non-membrane-permeable blocker of fast Na+-dependent action potentials and voltage-dependent, non-inactivating Na+ conductance.
  49. TRPM8 channel blocker

    TC-I 2000 is a TRPM8 channel blocker that inhibits icilin-induced TRPM8 channel activation in rTRPM8-expressing CHO cells

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