Membrane Transporters-Ion Channels

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  1. Calcium Channel Antagonist

    Bepridil hydrochloride hydrate is a non-selective, long-acting calcium channel antagonist that also inhibits sodium and potassium channels. It exhibits antianginal properties and functions as a type I antiarrhythmic agent. Additionally, Bepridil hydrochloride hydrate inhibits the cardiac sodium-calcium exchanger (NCX1), making it valuable for research into cardiovascular disorders.
  2. Sodium Channel Inhibitor

    Riluzole hydrochloride is a sodium channel inhibitor that exhibits anticonvulsant properties. It functions primarily as a use-dependent Na+ channel blocker and also has the capability to inhibit GABA uptake, with an IC50 of 43 μM. This compound is commonly utilized in neurological research applications, particularly in studies focused on epilepsy and neuroprotection.
  3. Calcium Channel Blocker

    Amlodipine maleate is a dihydropyridine calcium channel blocker that primarily targets voltage-dependent L-type calcium channels. By inhibiting calcium influx, it serves as an effective antianginal agent and contributes to the management of hypertension. Amlodipine maleate is utilized in research applications related to cardiovascular health, hypertension, and potential anticancer effects.
  4. Sodium Channel Inhibitor

    Ropivacaine hydrochloride is a potent sodium channel inhibitor that effectively disrupts impulse conduction by reversibly blocking sodium ion influx in nerve fibers. Additionally, it inhibits the K2P TREK-1 potassium channel with an IC50 of 402.7 μM in COS-7 cell membranes. This compound is primarily applied in the management of neuropathic pain in various in vivo research contexts.
  5. ENaC Blocker

    Benzamil hydrochloride is a selective blocker of the epithelial sodium channel (ENaC) and serves as an inhibitor of the Na+/Ca2+ exchanger (NCX) with an IC50 of approximately 100 nM. This compound also enhances myogenic vasoconstriction and inhibits TRPP3-mediated Ca2+-activated currents at an IC50 of 1.1 μM. Benzamil hydrochloride is employed in various research applications aimed at studying ion channel regulation and cardiovascular physiology.
  6. Potassium Channel Inhibitor

    Cloperastine fendizoate is a potent inhibitor of the hERG potassium channels, exhibiting concentration-dependent inhibition with an IC50 value of 27 nM. This compound is primarily utilized in research applications focusing on cardiac ion channel function and related arrhythmia studies. Its effects on potassium currents make it valuable for investigating the electrophysiological properties of cardiac tissues and potential therapeutic interventions.
  7. Sodium Channel Inhibitor

    Propoxycaine hydrochloride is a sodium channel inhibitor that disrupts voltage-gated sodium channel activity, leading to a reduction in ionic flux essential for the initiation and propagation of action potentials. This compound is primarily utilized in research to investigate sensory nerve function and analgesic mechanisms, resulting in local anesthetic effects characterized by a loss of sensation.
  8. Potassium Channel Inhibitor

    Tetraethylammonium chloride is a non-selective inhibitor of potassium channels, effectively blocking their function. This compound is recognized as a substrate for organic cation transporter 1 (OCTN1), which may be relevant in transport-related studies. Additionally, tetraethylammonium chloride exhibits potential antitumor properties, making it a valuable tool in cancer research and investigations into ion channel dynamics.
  9. Antiestrogen

    Triphenylethylene is an antiestrogen agent that primarily functions by inhibiting L-type Ca2+ channels. This compound displays weak estrogenic activity and has been shown to relax duodenal intestinal muscle. Triphenylethylene is useful in research applications focusing on estrogen receptor modulation and the investigation of calcium channel dynamics in smooth muscle tissues.
  10. FTO Inhibitor

    Meclofenamic acid is a highly selective inhibitor of the fat mass and obesity-associated (FTO) enzyme, which plays a crucial role in the regulation of m(6)A RNA methylation. By competing with FTO for binding to m(6)A-containing nucleic acids, it modulates RNA metabolism and influences cellular processes related to metabolism and obesity. Additionally, Meclofenamic acid exhibits non-selective blockade of gap junctions and inhibits the potassium channels hKv2.1 and hKv1.1, with IC50 values of 56.0 µM and 155.9 µM, respectively. This compound is valuable for research applications focused on obesity, metabolic regulation, and ion channel physiology.
  11. Anticonvulsant Agent

    Methsuximide is an anticonvulsant agent that primarily targets T-type calcium channels. It is effective in managing petit mal seizures, as well as psychomotor and focal motor attacks. This compound is utilized in neurological research to investigate seizure mechanisms and the pharmacological modulation of epilepsy. Its selective action on calcium currents makes it a valuable tool for studying seizure activity and potential therapeutic interventions.
  12. Chemical Compound

    N-Bromoacetamide is a chemical compound that functions by irreversibly modulating sodium channel inactivation at the cytoplasmic membrane. This action also leads to a reduction in the rapid inactivation of potassium currents. It is primarily utilized in research focused on ion channel dynamics and electrophysiological studies.
  13. Antidepressant

    Depramine, a tricyclic antidepressant, primarily targets neurotransmitter reuptake mechanisms, elevating levels of norepinephrine and serotonin in the synaptic cleft. It exhibits significant biological activity through the inhibition of acetylcholinesterase, Mg2+-ATPase, and Na+/K+ ATPase. Depramine is utilized in research focused on depression and related mood disorders, facilitating studies on neurotransmitter dynamics and cellular signaling pathways involved in antidepressant efficacy.
  14. Local Anaesthetic

    Isobutamben is an amino ester-type local anaesthetic that primarily targets sodium channels to inhibit nerve conduction. It exhibits potent analgesic effects, making it useful in various surgical and dental procedures. Its ability to provide localized pain relief positions Isobutamben as a valuable tool in both clinical and research settings focused on pain management and anaesthesia.
  15. Topical Anesthetic

    Quinisocaine is a local anesthetic primarily targeting sodium channels to inhibit nerve signal propagation. It is utilized in the investigation of pain mechanisms and pruritus in various research contexts. This compound provides valuable insights into anesthetic mechanisms and can facilitate studies on pain management efficacy.
  16. T-channels Inhibitor

    1-Octanol is a saturated fatty alcohol that selectively inhibits T-type calcium channels, demonstrating an IC50 of 4 μM for native T-currents. This compound serves as a valuable tool in pharmacological research aimed at understanding calcium signaling pathways. Additionally, its properties as a biofuel with diesel-like characteristics make it an interesting candidate for energy applications.
  17. Nav1.7 Inhibitor

    Nav1.7-IN-22 is a selective inhibitor of the voltage-gated sodium channel Nav1.7. By blocking the activity of Nav1.7, this compound effectively inhibits abnormal electrical signal generation and conduction in sensory neurons. Nav1.7-IN-22 is utilized in research focused on pain mechanisms, providing insights into potential therapeutic applications for pain management.
  18. Stable Isotope

    Norquetiapine-d8 is a stable isotope labeled version of Norquetiapine, which acts as a selective inhibitor of HCN1 channels with an IC50 of 13.9 μM. This compound effectively inhibits noradrenaline reuptake and serves as a partial agonist at the 5-HT1A receptor (Ki = 45 nM), while also antagonizing presynaptic α2 (Ki = 237 nM), 5-HT2C (Ki = 107 nM), and 5-HT7 (Ki = 76 nM) receptors. Furthermore, Norquetiapine exhibits state-dependent blockade of the human cardiac sodium channel Nav1.5 and demonstrates partial anti-inflammatory activity in LPS-injected C57BL/6 mice, making it useful for research on depression and inflammation.
  19. Stable Isotope

    Cyclopiazonic acid-13C20 is a stable isotope-labeled derivative of Cyclopiazonic acid, a selective inhibitor of endoplasmic reticulum calcium ATPases (ECAs) and has demonstrated efficacy against human respiratory syncytial virus (RSV) with an EC50 value of 4.13 μM. This compound is shown to inhibit the antagonistic effects of serotonin receptors in rat thoracic aorta, induce p53-dependent apoptosis, and exhibit reproductive toxicity in mouse testes, as well as inhibit the biological activation of aflatoxin B. Cyclopiazonic acid-13C20 is valuable for research applications in calcium signaling, viral infections, and toxicology studies.
  20. Insecticide

    Fenpropathrin is a synthetic pyrethroid insecticide that primarily targets insect sodium channels, resulting in prolonged depolarization and subsequent paralysis of pests. This compound demonstrates significant insecticidal activity, effectively controlling a variety of agricultural pests. Additionally, research indicates that Fenpropathrin exposure may be linked to the development of parkinsonian symptoms, making it a subject of interest in neurotoxicology studies. Its utility in both agricultural and biomedical research applications highlights its importance in understanding insecticide mechanisms and potential health impacts.
  21. Fenvalerate Isomer

    Esfenvalerate is a synthetic pyrethroid insecticide, specifically targeting the fenvalerate isomer. It exhibits neurotoxic activity in insects by interfering with sodium channel function, leading to paralysis and death. This makes Esfenvalerate valuable in agricultural research for pest management and studying the mechanisms of insecticide resistance in pest populations.
  22. Pesticide

    Alpha-Cypermethrin is a synthetic pyrethroid insecticide primarily targeting voltage-gated sodium channels in insect membranes. It exhibits potent activity against various arthropods, including house flies, making it a valuable tool in agricultural and pest control research. Its efficacy and mode of action facilitate studies on insect resistance, behavioral responses, and integrated pest management strategies.
  23. Pyrethroid Compound

    (+)-trans-Permethrin is a pyrethroid compound that acts on voltage-gated sodium channels in insect neurons, disrupting nerve signal transmission. This synthetic derivative of natural pyrethrins, found in Chrysanthemum species, exhibits potent insecticidal activity. Its applications include entomological research, pest control studies, and investigations into insect resistance mechanisms.
  24. Pesticide

    (-)-cis-Permethrin is a pyrethroid insecticide known for its neurotoxic action on insects. It primarily targets voltage-gated sodium channels, leading to paralysis and death in a variety of pest species. This compound is commonly utilized in agricultural and urban pest management applications, offering effective control against numerous insect infestations.
  25. Pyrethroid

    (-)-trans-Permethrin is a pyrethroid insecticide targeting sodium channels in nerve cells, resulting in prolonged neurotoxicity to pests. It is effective in providing protection against various insects, including black flies, in agricultural settings. This compound is widely used in studies related to insect control and pest management in livestock.
  26. Insecticide

    τ-Fluvalinate is an insecticide primarily targeting the nervous system of pests. It selectively binds to the open state of voltage-dependent sodium channels, specifically Varroa destructor (VdNaV1) and Apis mellifera (AmNaV1), exhibiting EC50 values of 160 nM and 60 nM, respectively. Its higher affinity for AmNaV1 results in sublethal toxicity to honeybees, making τ-Fluvalinate a valuable tool for investigating Varroa destructor infestations in honeybee colonies and studying the impacts of insecticides on non-target species.
  27. Insecticide

    Tralomethrin is a synthetic pyrethroid insecticide that acts on the nervous system of insects by inhibiting sodium channels, resulting in paralysis and death. It is effective against a variety of agricultural and public health pests, making it valuable for integrated pest management practices. Research applications include evaluating its efficacy in pest control, investigating potential environmental impacts, and studying resistance mechanisms in target insect populations.
  28. Insecticide

    Cyhalothrin is a synthetic pyrethroid insecticide designed to disrupt the function of sodium channels in insect nerve cells. It exhibits potent insecticidal activity against a broad spectrum of pests while maintaining low toxicity to mammals. This compound is widely used in agricultural and vector control applications, making it essential for studies related to pest management and the development of sustainable agricultural practices.
  29. Pyrethroid Insecticide

    Cismethrin is a pyrethroid insecticide that targets sodium channels in the nervous system, inducing neurotoxicity through Type I effects. This compound effectively disrupts neuronal signaling in insects, leading to paralysis and death. Cismethrin is utilized in entomological research and pest control studies to understand insecticide mechanisms and resistance.
  30. Insecticide

    (Rac)-Bifenthrin is a pyrethroid insecticide that targets the nervous system of insects by modulating the function of sodium channels. It exhibits potent insecticidal activity against a wide range of pests, making it effective for use in both urban and agricultural environments. Its mechanism of action leads to paralysis and death in targeted insect populations, facilitating its application in pest management and control strategies.
  31. Insecticide

    Tetrachlorantraniliprole is an anthranilic diamide insecticide that targets insect ryanodine receptors, leading to disruption of calcium channels and subsequent muscle paralysis. This compound exhibits significant insecticidal activity against a range of agricultural pests, making it valuable for crop protection research. Its mechanism of action provides insight into the development of novel pest control strategies that minimize environmental impact.
  32. Stable Isotope

    Barnidipine-d5 is a deuterium-labeled analog of Barnidipine, functioning as an L-type calcium antagonist with a strong affinity for [3H] initrendipine binding sites (Ki = 0.21 nmol/l). This compound exhibits selective action on calcium antagonist receptors and serves as an effective antihypertensive agent, primarily reducing peripheral vascular resistance through its vasodilatory effects. Barnidipine-d5 is suitable for research applications focused on cardiovascular pharmacology and calcium channel modulation.
  33. Calcium Channel

    C18 LPA (PA(18:0e/0:0)) targets calcium channels and serves as a bioactive phospholipid involved in signal transduction via G protein-coupled receptors (GPCRs). This compound promotes smooth muscle contraction, chemotaxis, cytoskeletal rearrangement, and is implicated in neurotransmitter release and cell proliferation. Increased levels of C18 LPA in human plasma are correlated with ovarian cancer and atherosclerosis, indicating its potential utility as a biomarker in oncological and cardiovascular research.
  34. HCN Channel Blocker

    Ivabradine impurity 1 is a derivative of Ivabradine, a hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker. This compound has been utilized in research to investigate the modulation of cardiac rhythms and treatment of conditions such as angina and heart failure. Its biological activity contributes to the understanding of ion channel interactions and cardiac electrophysiology.
  35. Overoxidized By-product of Lansoprazole

    Lansoprazole N-oxide is the overoxidized by-product derived from the synthesis of the proton pump inhibitor Lansoprazole. This compound is of interest for studies related to gastrointestinal disorders, including duodenal and gastric ulcers, reflux esophagitis, and Zollinger–Ellison syndrome. Researchers may utilize Lansoprazole N-oxide to deepen the understanding of proton pump inhibition and its implications in these conditions.
  36. Drug Metabolite

    15-Hydroxy Lubiprostone is an active metabolite of the laxative drug Lubiprostone, primarily targeting chloride channels. This compound exhibits biological activity by promoting fluid secretion in the intestinal lumen, thereby facilitating bowel movements. It is mainly utilized in research applications focused on gastrointestinal pharmacology and the mechanisms of action related to chloride channel activation.
  37. Overoxidized By-product of Lansoprazole

    Lansoprazole sulfone N-Oxide is an overoxidized by-product generated during the synthesis of the proton pump inhibitor Lansoprazole. This compound is relevant for research into gastrointestinal conditions, such as duodenal and gastric ulcers, reflux esophagitis, and Zollinger–Ellison syndrome. Its study may provide insights into the metabolic pathways and potential therapeutic implications related to proton pump inhibition.
  38. Bupivacaine metabolite

    Bupivacaine N-oxide hydrochloride is a metabolite of the local anesthetic Bupivacaine, which primarily acts as an NMDA receptor inhibitor. It also exhibits significant activity by blocking sodium, L-calcium, and potassium channels, particularly SCN5A channels with an IC50 of 69.5 μM. This compound is relevant for research into chronic pain mechanisms and provides insight into the pharmacological action of Bupivacaine and its derivatives.
  39. Active Metabolite of T-1095

    T-1095A is the active metabolite of T-1095, functioning as a sodium-glucose cotransporter (SGLT) inhibitor. This compound demonstrates significant biological activity in the regulation of glucose reabsorption in the renal system and is primarily utilized in research related to diabetes and metabolic disorders. Its mechanism of action aids in the investigation of glucose homeostasis and associated therapeutic strategies.
  40. Sodium Channel Inhibitor

    Decarbamoylsaxitoxin is a potent sodium channel inhibitor that selectively blocks the influx of sodium ions in excitable tissues, such as nerve and skeletal muscle cells, thus preventing action potential generation. As a hydrolysis product of saxitoxin, Decarbamoylsaxitoxin exhibits similar neurotoxic effects, including the ability to inhibit veratridine- and ouabain-induced neuroblastoma cell swelling and lysis. This reagent is valuable for research involving mechanisms of paralytic shellfish poisoning and sodium channel pharmacology.
  41. Drug Metabolite Control

    Nicorandil pyridine oxide is a metabolite of Nicorandil, which acts as an activator of the sulfonylurea receptor 2B (SUR2B) and the ATP-sensitive potassium channel Kir6.2. This compound serves as a crucial tool for drug metabolite control, offering insights into the pharmacokinetics and therapeutic mechanisms of Nicorandil. Its biological activity is important for researchers studying cardiovascular effects and the modulation of ion channels in various biological systems.
  42. EBP Inhibitor

    EBP-IN-1 is a selective inhibitor of emopamil binding protein (EBP) that effectively crosses the blood-brain barrier. This compound demonstrates an IC50 of 8.2 μM against human ERG potassium channels in CHO cells, leading to the inhibition of EBP's sterol isomerase activity and subsequent accumulation of Zymostenol. EBP-IN-1 has been shown to promote oligodendrocyte differentiation in human cortical organoids, making it a valuable tool for research into multiple sclerosis and related neurological disorders.
  43. VGSC Blocker

    KC 12291 hydrochloride is a potent blocker of voltage-gated sodium channels (VGSC). It effectively reduces sustained Na+ current amplitude, demonstrating notable anti-ischemic properties. This compound exhibits significant cardioprotective effects in both in vitro and in vivo studies, making it a valuable tool for cardiac research and the investigation of sodium channel-related pathophysiology.
  44. Sodium Channels Blocker

    Phrixotoxin 3 is a selective blocker of voltage-gated sodium channels, demonstrating IC50 values of 0.6 nM for NaV1.2, 42 nM for NaV1.3, 72 nM for NaV1.4, 288 nM for NaV1.1, and 610 nM for NaV1.5. This compound modulates sodium channel activity by shifting gating kinetics in a depolarized direction while inhibiting the inward sodium current. Phrixotoxin 3 is valuable for research focusing on ion channel modulation, neurophysiology, and the investigation of sodium channel-related pathologies.
  45. Sodium Current Blocker

    F-15845 hydrobromide is a potent persistent sodium current blocker, primarily targeting voltage-gated sodium channels. It demonstrates significant cardioprotective properties and anti-ischemic activity, providing both short- and long-term protection following myocardial infarction. This compound is valuable for investigating functional impairments in the myocardium and exploring therapeutic strategies related to cardiac health.
  46. Sodium Channel Antagonist

    Hainantoxin-IV is an antagonist of voltage-gated sodium channels, specifically targeting tetrodotoxin-sensitive (TTX-S) subtypes. This compound exhibits potent inhibitory activity through its interaction with key residues His28 and Lys32, which facilitate binding to the sodium channel. Hainantoxin-IV, characterized by an inhibitor cystine knot motif, is valuable in research applications exploring sodium channel modulation and related neurophysiological processes.
  47. AMPAR Agonist

    (S)-(-)-5-Fluorowillardiine hydrochloride is a selective agonist of the alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR). This compound exhibits significant biological activity by enhancing synaptic transmission and promoting excitatory neurotransmission in the central nervous system. It is valuable for research applications focused on studying synaptic plasticity, neurophysiology, and potential therapeutic interventions in neurological disorders related to glutamate signaling.
  48. AMPA Receptor Modulator

    AMPA Receptor Modulator-8 selectively modulates AMPA receptors, exhibiting an IC50 of 0.02 nM for TARP-γ2. This compound plays a significant role in the investigation of neurological disorders such as epilepsy, Alzheimer's disease, and Parkinson's disease. Its precise action on AMPA receptor dynamics makes it a valuable tool for advancing research in neuropharmacology and therapeutic development.
  49. AMPA-type Receptors Positive Allosteric Modulator

    S 18986 is a selective positive allosteric modulator of AMPA-type receptors, demonstrating significant brain penetration and oral bioavailability. This compound enhances cognitive function in rodent models, evidenced by its ability to activate the release of noradrenaline and acetylcholine in the rat hippocampus. S 18986 has shown efficacy in improving memory performance in object-recognition tests, making it a valuable tool for research into cognitive enhancement and neuropharmacology.
  50. AMPA Receptor Antagonist

    Selurampanel is a competitive antagonist of the AMPA receptor, demonstrating an IC50 of 190 nM. This compound exhibits significant penetration of the blood-brain barrier, making it suitable for in vivo studies. Selurampanel is primarily employed in research related to epilepsy, providing insights into neuroprotective mechanisms and potential therapeutic applications.

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