Membrane Transporters-Ion Channels

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  1. AMPA Receptor Antagonist

    NBQX is a potent, selective and competitive AMPA receptor antagonist.
  2. TRPV1 antagonist

    AMG 517 is a potent and selective TRPV1 antagonist.
  3. 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).
  4. Calcium channel antagonist

    Felodipine is a 1,4-dihydropyridine antagonist and calcium channel protein inhibitor.

  5. TRPM8 antagonist

    M8-B is an antagonist of transient receptor potential melastatin 8 (TRPM8) that blocks activation by cold, icilin (Item No. 10137), or menthol in vitro (IC50s = 7.8, 26.9, and 64.3 nM, respectively).
  6. Beta1-Adrenergic receptor antagonist

    Talinolol is a beta(1)-adrenergic receptor antagonist and a probe drug for P-glycoprotein (P-gp) activity in humans.

  7. 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.
  8. 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.
  9. TRPV1 antagonist

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

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

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

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

    Mitiglinide is a blood glucose-lowering drugs, stimulating insulin secretion by closing the ATP-sensitive K+ channels in pancreatic beta-cells.
  14. 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).
  15. NMDA receptor antagonist

    DNQX is a non-N-methyl-D-aspartate (non-NMDA) receptor complex antagonist.
  16. 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.
  17. TRPA1 Antagonist

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

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

    AMG-333 is a potent and selective TRPM8 Antagonist.
  20. 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.
  21. 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.
  22. Calcium channel antagonist

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

    Dooku1, an analog of Yoda1, is a selective antagonist of the endogenous Piezo1 channel.
  24. 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.
  25. 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.
  26. TRPV1 receptor antagonist

    SB-366791 is a novel, potent, and selective, cinnamide TRPV1 antagonist.
  27. 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).
  28. AMPA/kainate antagonist

    CNQX disodium salt, water-soluble form of AMPA/kainate antagonist CNQX (GLXC-11053).
  29. 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.
  30. TRPV1 antagonist

    A-1165442 is a potent, competitive and orally available TRPV1 antagonist with an IC50 of 9 nM for human TRPV1.
  31. NAADP antagonist

    Ned 19 is a selective membrane-permeant non competitive NAADP antagonist and inhibits NAADP-mediated Ca2+ signaling, with an IC50 of 65 nM.
  32. AMPA/kainate antagonist

    Fanapanel hydrate (ZK200775 hydrate) is a highly selective AMPA/kainate antagonist with little activity against NMDA; have Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively.
  33. T-type Ca2+ channel antagonist

    TTA-Q6(isomer) is an isomer of TTA-Q6. TTA-Q6 is a selective T-type Ca2+ channel antagonist.
  34. AMPAR antagonist

    Philanthotoxin 74 dihydrochloride (PhTx 74) is an AMPAR antagonist; inhibits GluR3 and GluR1 with IC50s of 263 and 296 nM, respectively.
  35. AMPA (CP-AMPA) receptors antagonist

    Naspm (1-Naphthyl acetyl spermine), a synthetic analogue of Joro spider toxin, is a calcium permeable AMPA (CP-AMPA) receptors antagonist.
  36. non-competitive AMPAR antagonist

    CFM-2 is a selective non-competitive AMPAR antagonist.
  37. L-type calcium antagonist

    Barnidipine (Mepirodipine) 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.
  38. TRPV1 antagonist

    PF-04745637 is a TRPV1 antagonist.
  39. antagonist of Vanilloid receptor type 1

    A-784168 is a potent and selective antagonist of Vanilloid receptor type 1 (TRPV1).
  40. Ampa Receptor Antagonist

    ATPO is a potent and Selective Ampa Receptor Antagonist.
  41. 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.
  42. 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).
  43. proton pump antagonist

    Pumaprazole is a reversible proton pump antagonist.
  44. calcium channel antagonist

    SM-6586 is a calcium channel antagonist and inhibitor of Na+/H+ and Na+/Ca2+ exchange transport, potentially for the treatment of cerebrovasular diseases and hypertension.
  45. dihydropyridine Ca2+ antagonist

    CV-159 is a unique dihydropyridine Ca2+ antagonist with an anti-calmodulin (CaM) action, and has antiinflammatory activities.
  46. AMPA receptor antagonist

    SYM 2206 is a novel, potent, non-competitive AMPA receptor antagonist.
  47. calcium-sensing receptor (CaR) antagonist

    SB-423562 is a short-acting calcium-sensing receptor (CaR) antagonist.
  48. AMPA antagonist

    Becampanel (AMP397) is the first competitive AMPA antagonist and an antiepileptic agent.
  49. glutamate receptor subtype antagonist

    Zonampanel (YM 872) is a selective antagonist of the glutamate receptor subtype, α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptor.
  50. AMPA/kainate antagonist

    Fanapanel (ZK200775) is a highly selective AMPA/kainate antagonist with little activity against NMDA; have Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively.

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