Membrane Transporters-Ion Channels

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  1. AMPA and Kainate antagonist

    GYKI-52466 dihydrochloride is selective non-competitive AMPA receptor antagonist (IC50 values are 10-20, ~ 450 and >> 50 μM for AMPA- , kainate- and NMDA-induced responses respectively).
  2. TRPV1 antagonist

    SB-705498 is a potent, selective and orally bioavailable TRPV1 antagonist.
  3. ATPase antagonist

    PF 3716556 is H+,K+-ATPase inhibitor (pIC50 = 6 in human recombinant ion-leaky assays).
  4. NMDA receptor antagonist

    Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker.
  5. Voltage-gated sodium channels antagonist

    Proparacaine HCl is a voltage-gated sodium channels antagonist with ED50 of 3.4 mM.
  6. KATP channel antagonist

    Mitiglinide is a blood glucose-lowering drugs, stimulating insulin secretion by closing the ATP-sensitive K+ channels in pancreatic beta-cells.
  7. TRPV1 antagonist

    AMG 517 is a potent and selective TRPV1 antagonist.
  8. TRPV1 antagonist

    NJ-17203212 is a novel and selective TRPV1 antagonist, with IC50 of 65 nM and 102 nM for human TRPV1 and rat TRPV1.
  9. AMPA Receptor Antagonist

    NBQX is a potent, selective and competitive AMPA receptor antagonist.
  10. AMPA antagonist

    CP 465022 is a selective, non-competitive AMPA antagonist with IC50 of 25 nM in rat cortical neurons that displays potent anticonvulsant activity.
  11. 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).
  12. NMDA receptor antagonist

    DNQX is a non-N-methyl-D-aspartate (non-NMDA) receptor complex antagonist.
  13. 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.
  14. Calcium-Sensing Receptor Antagonist

    Calcium-Sensing Receptor Antagonists I is an antagonist of calcium-sensing parathyroid hormone receptors.
  15. AMPA antagonist

    Tezampanel is an antagonist at the AMPA and kainate families of ionotropic glutamate receptors, with selectivity for the GluR5 subtype of the kainate receptor.
  16. 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.
  17. AMPA/kainate receptor antagonist

    Talampanel is a non-competitive antagonist of AMPA-receptor.
  18. 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.
  19. TRPM8 antagonist

    RQ-00203078 is a highly selective, potent and orally available TRPM8 antagonist (IC50 values are 5.3 and 8.3 nM for rat and human channels respectively), exhibits >350-fold selectivity for TRPM8 over TRPV4, TRPV1 and TRPA1.
  20. TRPV1 receptor antagonist

    SB-366791 is a novel, potent, and selective, cinnamide TRPV1 antagonist.
  21. AMPA/kainate antagonist

    CNQX is a competitive, non-NMDA glutamate receptor antagonist (IC50s = 0.3 and 1.5 uM for AMPA and kainate receptors, respectively, versus IC50 = 25 uM for NMDA receptors).
  22. AMPA/kainate antagonist

    CNQX disodium salt, water-soluble form of AMPA/kainate antagonist CNQX (GLXC-11053).
  23. Calcium Channel /TRP5 antagonist

    Lomerizine dihydrochloride is a antagonist at L-type and T-type Ca 2+ channels and TRp5 channels used to treat migraines and vertigo.
  24. TRPA1 Antagonist

    AM-0902 is a potent and selective Transient Receptor Potential A1 (TRPA1) Antagonist.
  25. AMPA antagonist

    GYKI53655 Hydrochloride is a non-competitive AMPA and kainate receptor antagonist. CAS: 143692-18-6 (Free Base); 143692-48-2 (HCl).
  26. TRPM8 Antagonist

    AMG-333 is a potent and selective TRPM8 Antagonist.
  27. L-type calcium-channel antagonist

    Etripamil (MSP-2017) is a short-acting L-type calcium-channel antagonist with a rapid onset of action designed for intranasal administration, used to treat Paroxysmal Supraventricular Tachycardia (PSVT). Etripamil (MSP-2017) slows atrioventricular nodal conduction and prolongs atrioventricular nodal refractory periods by inhibiting calcium ion influx through the calcium slow channels in the atrioventricular node cells.
  28. 5-HT receptor /dopamine receptors antagonist

    Metergoline is a psychoactive drug of the ergoline chemical class which acts as a ligand for various serotonin and dopamine receptors.
  29. Calcium channel antagonist

    Aranidipine (MPC1304) is a Ca2+ channel antagonist with potent and long-lasting antihypertensive effects.
  30. Piezo1 channel antagonist

    Dooku1, an analog of Yoda1, is a selective antagonist of the endogenous Piezo1 channel.
  31. L-type calcium antagonist

    Barnidipine hydrochloride (Mepirodipine hydrochloride) is an L-type calcium antagonist (CaA) with high affinity for [3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors.
  32. Calcium Channel antagonist

    Fantofarone is a highly potent Calcium Channel antagonist.
  33. 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.
  34. TRPM8 antagonist

    TRPM8 antagonist 2 is a potent and selective TRPM8 antagonist, with an IC50 of 0.2 nM, used in the research of neuropathic pain syndromes.
  35. TRPM8 antagonist

    AMG2850 is a potent, orally bioavailable and selective transient receptor potential melastatin 8 (TRPM8) antagonist.
  36. calcium antagonist

    Palonidipine is a calcium antagonist which is potential for the therapy of angina-pectoris and hypertension.
  37. TRPC4/TRPC5 antagonist

    HC-070 is an antagonist of TRPC4/TRPC5, with IC50s of 9.3 nM and 46 nM for hTRPC5 and hTRPC4 in cells, respectively.
  38. TRPV1 antagonist

    AMG9810 is a selective and competitive vanilloid receptor 1 (TRPV1) antagonist with IC50 values of 24.5 and 85.6 nM for human and rat TRPV1, repectively.
  39. TRPA1 antagonist

    TRPA1 Antagonist 1 is a methylene phosphate prodrug which converts to its active parent drug, a TRPA1 antagonist with an IC50 of 8 nM.
  40. Transmembrane glutamine flux antagonist

    V-9302 is a competitive antagonist of transmembrane glutamine flux.
  41. AMPA receptor antagonist

    LY3130481 is an AMPA receptor antagonist that is dependent upon transmembrane AMPA receptor regulatory protein (TARP) γ-8, selective inhibits AMPA/TARP γ-8 with an IC50 of 65 nM.
  42. calcium antagonist

    UK51656 is a calcium antagonist with IC50 of 4 nM.
  43. TRPM8 antagonist

    TC-I 2014 (compound 5) is a potent and orally active Benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonist, with IC50 values of 0.8 nM, 3.0 nM and 4.4 nM for canine, human and rat channels respectively.
  44. KCC2 antagonist

    VU0463271 is a potent KCC2 antagonist, with an IC50 of 61 nM.
  45. TRPV4 antagonist

    GSK3395879 is a selective and orally bioavailable transient receptor potential vanilloid-4 (TRPV4) antagonist with an IC50 of 1 nM for hTRPV4.
  46. Ca2+ antagonist

    Iganidipine is a Ca2+ antagonist.
  47. Ca2+ antagonist

    TDN345 is a Ca2+ antagonist, used for the treatment of vascular and senile dementia including Alzheimer's disease.
  48. TRPV1 receptor antagonist

    JYL 1421 is a TRPV1 receptor antagonist, with an IC50 of 8 nM.
  49. TRPV4 antagonist

    HC-067047 is a potent and selective TRPV4 antagonist and reversibly inhibits currents through the human, rat, and mouse TRPV4 orthologs with IC50 values of 48 nM, 133 nM, and 17 nM, respectively.
  50. TRPV4 antagonist

    RN-1734 is selective antagonist of the TRPV4 channel, completely antagonizes 4αPDD-mediated activation of TRPV4 with comparable, low micromolar IC50s for all three species (hTRPV4: 2.3 μM, mTRPV4: 5.9 μM, rTRPV4: 3.2 μM).

Items 1-50 of 76

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