Membrane Transporters-Ion Channels

Items 351-400 of 2532

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  1. ATPase and GTPase inhibitor

    Etidronate Disodium is a bisphosphonate bone resorption inhibitor.
  2. 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.
  3. 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.
  4. Linoleylethanolamide is an endocannabinoid that also binds to TRPV1 (Ki = 5.60 uM).
  5. 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.
  6. TRPV1 modulator

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

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

    Talampanel is a non-competitive antagonist of AMPA-receptor.
  9. TRPC4/C5 inhibitor

    ML204 is a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels.
  10. (-)-Menthol is a key component of peppermint oil that binds and activates transient receptor potential melastatin 8 (TRPM8), a Ca2+-permeable nonselective cation channel, to increase [Ca2+]i. Antitumor activity.
  11. 5-HT3 receptor inhibitor

    Eucalyptol is a bicyclic monoterpene that has been found in Eucalyptus and other plants. It is an inhibitor of 5-HT3 receptor ,potassium channel, TNF-α and IL-1β.
  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. AMPA Receptor Inhibitor

    Aniracetam is an ampakine and nootropic of the racetam chemical class purported to be considerably more potent than piracetam.
  15. Protein kinase inhibitor

    Apigenin, found in many plants, is a natural product belonging to the flavone class that is the aglycone of several naturally-occurring glycosides. Apigenin acts as a monoamine transporter activator, one of the few chemicals demonstrated to possess this property. Apigenin is a ligand for central benzodiazepine receptors that competitively inhibited the binding of flunitrazepam with a Ki of 4μM, exerting anxiolytic and slight sedative effects.

  16. Artemisinin and its derivatives are a group of drugs that possess the most rapid action of all current drugs against Plasmodium falciparum malaria.
  17. SGLT2 inhibitor

    EGT1442 is a potent and selective SGLT2 inhibitor.
  18. Bupivacaine is a more potent inhibitor of cAMP production than are chemically related local anesthetics that are less prone to produce cardiovascular toxicity.
  19. 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.
  20. Diethylstilbestrol is a synthetic nonsteroidal estrogen that was first synthesized in 1938. It is also classified as an endocrine disruptor.
  21. Diltiazem is a nondihydropyridine (non-DHP) member of the class of drugs known as calcium channel blockers, used in the treatment of hypertension, angina pectoris, and some types of arrhythmia.
  22. Proton pump inhibitor

    Esomeprazole sodium is a proton pump inhibitor which reduces acid secretion through inhibition of the H+ / K+ ATPase in gastric parietal cells.
  23. TRP agonist

    Evodiamine is a chemical extracted from the Tetradium family of plants. It acts primarily as a thermogenic and stimulant.
  24. Kir6.2/SUR inhibitor

    Glimepiride is a potent Kir6.2/SUR inhibitor with IC50 of 3.0 nM, 5.4 nM, and 7.3 nM for SUR1, SUR2A and SUR2B, used in the treatment of type 2 diabetes mellitus.
  25. K+ channel and CFTR Cl- channel blocker

  26. 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).
  27. Hydralazine hydrochloride is a hydrochloride salt of hydralazine (Apresoline) that is a direct-acting smooth muscle relaxant with an IC50 of 1.9 mM.
  28. Ivermectin is a broad-spectrum antiparasitic avermectin medicine.
  29. proton pump inhibitor

    Lansoprazole(AG 1749) is a proton pump inhibitor which prevents the stomach from producing acid.
  30. Lidocaine (Alphacaine) is an anasthetic and class Ib antiarrhythmic agent. Blocks voltage-gated sodium channels in the inactivated state.
  31. Lubiprostone is a bicyclic fatty acid metabolite analog of Prostaglandin E1. It activates specific chloride channels in the gastrointestinal tract to stimulate intestinal fluid secretion, and increase gastrointestinal transit.
  32. PDE4 inhibitor

    Luteolin is a PDE4 inhibitor, phosphodiesterase inhibitor, and an interleukin 6 inhibitor, affecting xylazine/ketamine-induced anesthesia in mice. Luteolin acts as a monoamine transporter activator, and is one of the few chemicals demonstrated to possess this property.
  33. Manidipine is a dihydropyridine compound and calcium channel protein inhibitor and antagonist.
  34. Minoxidil (U-10858) is a selective ATP dependent K+ (Kir6) channel activator.
  35. Nateglinide(Starlix) is an insulin secretagog agent that lowers blood glucose levels by stimulating insulin secretion from the pancreas.
  36. Kir6 (KATP) channel opener

    Nicorandil (SG-75) is potassium channel activator.
  37. L-type calcium channel blocker.

    Nifedipine is a L-type calcium channel blocker.
  38. 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.
  39. ATPase Inhibitors

    Omeprazole is a cell-permeable, selective proton pump inhibitor.
  40. CFTR Inhibitor

    Oridonin (Isodonol), an entkaurane diterpenoid isolated from Rabdosia rubescens, is an important traditional Chinese herbal remedy.
  41. Phenytoin is a sodium channel protein inhibitor.
  42. Phenytoin sodium (Dilantin) is a sodium channel protein inhibitor.
  43. P-gp inhibitor

    P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.
  44. Atagabalin is related to gabapentin, which similarly binds to the α2δ calcium channels (1 and 2).
  45. Serotonin transporter inhibitor

    Imipramine Hydrochloride is a tricyclic antidepressant. Inhibits the serotonin and norepinephrine transporters but has little effect on the dopamine transporter.
  46. SGLT2 Inhibitor

    Luseogliflozin is an orally active second-generation sodium-glucose co-transporter 2 (SGLT2) inhibitor developed by Taisho Pharmaceutical for the treatment of patients with type 2 diabetes mellitus (T2DM).
  47. 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).
  48. CFTR inhibitor

    IOWH032 is a CFTR inhibitor.
  49. P-gp inhibitor

    ONT-093 is an orally bioavailable P-glycoprotein pump inhibitor, for the potential reversal of multidrug resistance in patients undergoing cancer chemotherapy.
  50. P-gp inhibitor

    Laniquidar is a third-generation P-gp inhibitor, which has been used in clinic trials for modulating multidrug resistance transporters.

Items 351-400 of 2532

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