Sodium Channels

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  1. Glucokinase Activator

    Glucokinase activator 3 is a potent activator of glucokinase (GK) with an AC50 of 38 nM. This compound has demonstrated significant efficacy in reducing blood glucose levels in diet-induced obese (DIO) mice, highlighting its potential in type 2 diabetes research. Additionally, glucokinase activator 3 has been shown to inhibit the hERG channel and sodium channels in patch clamp assays, providing insight into its pharmacological profile.
  2. Analgesic Agent

    (+)-Mepivacaine is an amide-type local anesthetic that exhibits potent analgesic and vasoconstrictive properties. By selectively binding to voltage-gated sodium channels on neuronal cell membranes, it effectively inhibits sodium influx, leading to a temporary loss of sensation in targeted areas. This compound is widely utilized in various research applications, particularly in studies focused on pain management and anesthesia.
  3. Antiarrhythmic Agent

    (S)-Propafenone is an antiarrhythmic agent that functions primarily as a sodium channel blocker. This compound exhibits beta-blocking properties and demonstrates class 1 antiarrhythmic activity, making it valuable in the study of cardiac arrhythmias. Its efficacy in modulating myocardial excitability and conduction makes it an important tool for research applications aimed at understanding arrhythmic disorders and developing therapeutic strategies.
  4. Sodium Channel Blocker

    Zilvetrigine is a sodium channel blocker that selectively inhibits voltage-gated sodium channels. This compound exhibits analgesic properties, making it valuable for pain management research. Its mechanism of action can be explored in studies related to neuropathic pain and other conditions mediated by sodium channel activity.
  5. Cardioactive Agent

    DPI 201-106 is a cardiotonic agent that exerts its effects through a synergistic mechanism involving both sarcolemmal and intracellular pathways. It selectively modulates voltage-gated sodium channels (VGSCs), leading to a significant positive inotropic effect. This compound is useful for research applications focused on cardiac function and the modulation of ion channel activity in cardiac tissues.
  6. Sodium Channel Blocker

    Tocainide hydrochloride is a sodium channel blocker that inhibits the activity of voltage-gated sodium channels, effectively reducing neuronal excitability in pain pathways. This compound is primarily used in research related to pain mechanisms and the treatment of conditions such as tinnitus. Tocainide hydrochloride functions as a primary amine analog of lidocaine, providing insights into sodium channel modulation and its therapeutic potential.
  7. Sodium Channel Inhibitor

    Licarbazepine-d4 is a deuterated derivative of Licarbazepine, functioning as a sodium channel inhibitor. This compound exhibits anticonvulsant and mood-stabilizing properties, making it a valuable tool in the study of neurological disorders. It is particularly useful for researchers investigating the mechanisms of epilepsy and mood regulation.
  8. 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.
  9. Na+ Channel Blocker

    RSD-921 is a potent sodium (Na+) channel blocker exhibiting significant anti-arrhythmic properties. It acts with state- and voltage-dependent inhibition on the open states of cardiac, skeletal muscle, and neuronal Na+ channels. Additionally, RSD-921 has a low affinity for κ-opioid receptors and shows weak κ-agonistic activity in vitro. This reagent is valuable for research focusing on cardiac arrhythmias and the modulation of Na+ channels in various biological models.
  10. Stable Isotope

    Cyhalothrin-d5 is a deuterated version of Cyhalothrin, a synthetic pyrethroid insecticide that primarily targets voltage-gated sodium channels in insect nerves. This stable isotope is essential for chemical research and environmental studies, particularly in trace analysis and bioaccumulation studies of pesticides. Cyhalothrin-d5 allows for precise quantification in analytical applications, enhancing the understanding of pest management and its ecological impacts.
  11. Drug Impurity

    Flecainide Impurity 3 is a known impurity of the antiarrhythmic agent Flecainide, which primarily targets sodium channels to exert its pharmacological effects. This compound is crucial for quality control in the pharmaceutical industry, allowing researchers to assess the purity and stability of Flecainide formulations. Its identification and quantification are essential for ensuring compliance with regulatory standards in drug development and manufacturing.
  12. Antiarrhythmic Agent

    R-(–)-Flecainide is an orally active antiarrhythmic agent that primarily targets voltage-gated sodium channels to inhibit ectopic ventricular activity. It effectively stabilizes cardiac cell membranes and is utilized in the management of various cardiac arrhythmias. Research applications include studies on cardiac electrophysiology and drug interactions in arrhythmogenic conditions.
  13. S-isomer Of Ranolazine

    (S)-Ranolazine is the S-isomer of the antianginal agent Ranolazine, which primarily targets the cardiomyocyte sodium channels. It demonstrates significant biological activity in reducing myocardial ischemia and angina by modulating ion currents and improving cardiac energy metabolism. This compound is used in cardiovascular research to explore mechanisms of action related to cardiac function and ischemia.
  14. Antiarrhythmic Agent

    Propafenone, a sodium channel blocker, functions as an antiarrhythmic agent by modulating cardiac ion currents. It displays significant binding affinity for β receptors (IC50 = 32 nM) and effectively inhibits the transient outward current (Ito) and sustained delayed rectifier potassium current (Isus) with IC50 values of 4.9 μM and 8.6 μM, respectively. Additionally, Propafenone demonstrates potential in anticancer research by suppressing the proliferation of esophageal cancer cells through the induction of mitochondrial dysfunction and apoptosis.
  15. Antiepileptic Agent

    Rufinamide is an oral antiepileptic agent that primarily inhibits sodium channel activation, leading to reduced neuronal hyperexcitability and anticonvulsant effects. This compound is particularly relevant in the study of Lennox-Gastaut syndrome, providing insights into its mechanisms and potential therapeutic strategies. Rufinamide's efficacy in mitigating seizures makes it a valuable tool for research in epilepsy and related neurological disorders.
  16. Sodium Channel Inhibitor

    Mepivacaine hydrochloride is a sodium channel inhibitor that selectively binds to voltage-gated sodium ion channels in neuronal cell membranes. By inhibiting sodium influx and membrane depolarization, it provides significant local anesthetic effects. This compound is widely used in research applications related to nerve conduction studies and pain management investigations.
  17. Muscarinic Receptor Antagonist

    Afacifenacin is a potent and orally active muscarinic receptor antagonist that targets the bladder afferent pathway. It exerts its biological activity by inhibiting sodium channels, leading to increased bladder volume and a reduction in the frequency of urination and incontinence. This compound is valuable for research focused on overactive bladder (OAB) and related urological conditions.
  18. Na+ Channel Activator

    Brevetoxin-3 (PbTx-3) is a potent allosteric activator of voltage-gated Na+ channels. It demonstrates high affinity for site 5 on these channels, effectively inhibiting their inactivation and prolonging the mean open time. This compound is valuable for research into airway hyperresponsiveness and lung inflammation, as repeated exposure has been shown to induce these conditions. Brevetoxin-3 serves as a critical tool for studying sodium channel modulation and its implications in respiratory pathophysiology.
  19. Sodium Channel Activator

    3-Deoxyaconitine is a diterpenoid alkaloid identified as a sodium channel activator. It exhibits significant biological activity by modulating ion channel dynamics, making it a valuable tool for research into neuronal signaling and pain pathways. This compound can be utilized in studies focusing on the physiological and pharmacological roles of sodium channels.
  20. Bacterial Inhibitor

    Methyl Paraben is a bacterial inhibitor primarily used as a preservative in various applications due to its stability and non-volatility. It has been shown to enhance histamine release and modulate cellular immune responses, in addition to blocking sodium channels. Its properties make it valuable for studies exploring microbial inhibition and the mechanisms of ischemia-reperfusion injury.
  21. Dopamine Receptor Inhibitor

    Fluphenazine dihydrochloride is a potent dopamine receptor antagonist primarily targeting dopamine D2 receptors in the mesolimbic, nigrostriatal, and tuberoinfundibular pathways. This phenothiazine derivative also exhibits the ability to inhibit neuronal voltage-gated sodium channels. Its key biological activities include the suppression of Methylphenidate-induced stereotyped behaviors and climbing in murine models. Fluphenazine dihydrochloride is widely utilized in research related to psychosis, diabetic peripheral neuropathy, and may also have implications for the inhibition of SARS-CoV-2.
  22. Sodium Channel Inhibitor

    Oxybuprocaine hydrochloride is a sodium channel inhibitor that reversibly blocks sodium channels, effectively preventing the propagation of painful nerve impulses in tissues such as the cornea, conjunctiva, and sclera. This compound is primarily utilized in ophthalmology and otolaryngology for its anesthetic properties, providing localized pain relief during various medical procedures. Its ability to inhibit nerve signal transmission makes it valuable for both diagnostic and therapeutic applications in ocular and ear, nose, and throat treatments.
  23. Sodium Channel Inhibitor

    Propafenone hydrochloride is a sodium channel inhibitor primarily used as an anti-arrhythmic agent. It effectively treats conditions related to rapid heartbeats, including atrial and ventricular arrhythmias. This compound is useful in research applications focused on cardiac rhythm disturbances and the pharmacological modulation of ion channels.
  24. Sodium Channel Inhibitor

    Triamterene is a sodium channel inhibitor that selectively blocks epithelial Na+ channels (ENaC) in a voltage-dependent manner. It exhibits mild diuretic properties and is utilized in the management of conditions related to fluid retention. Additionally, Triamterene serves as an inhibitor of the TGR5 receptor, contributing to its diverse biological effects and applications in research related to renal and metabolic processes.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. 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.
  33. 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.
  34. 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.
  35. 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.
  36. 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.
  37. Antimicrobial Agent

    Halazone is an antimicrobial sulfonamide derivative that functions as an inhibitor of carbonic anhydrase II, exhibiting a Kd value of 1.45 µM. This compound effectively protects sodium channels from inactivation, making it a valuable agent in microbiological studies. Halazone's primary application lies in the disinfection of drinking water, rendering it crucial for research focused on waterborne pathogens and public health safety.
  38. Local Anaesthetic

    Amylocaine is a local anesthetic that primarily targets voltage-gated sodium channels, leading to reversible insensitization of nerve tissues. It is effective in suppressing or relieving pain in various clinical settings, particularly in spinal anesthesia. Amylocaine is utilized for its analgesic properties in procedures requiring localized pain management.
  39. Neural Blockade Agent

    Trimecaine is a local neural blockade agent that primarily targets sodium channels to inhibit neuronal excitability. It exhibits significant depressant effects on the cerebral cortex and the ascending reticular formation of the brainstem, leading to a reduction in sensory and motor nerve conduction. This compound is utilized in research applications focusing on pain management, anesthesia, and neurophysiological studies.
  40. SCN2A synthesis reducer

    Elsunersen is an antisense oligonucleotide designed to selectively reduce the expression of the SCN2A gene, which encodes the voltage-gated sodium channel Nav1.2. This compound is instrumental in researching SCN2A developmental and epileptic encephalopathy (SCN2A-DEE), a neurological disorder characterized by severe seizures and developmental impairments. By targeting SCN2A, Elsunersen facilitates the exploration of therapeutic approaches for conditions arising from SCN2A mutations.
  41. Local Anaesthetic Compound

    Hydroxytetracaine is a local anesthetic compound that primarily acts by blocking voltage-gated sodium channels, thereby inhibiting nerve impulse conduction. It is used to suppress or relieve localized pain in various medical procedures. Its effectiveness makes it a valuable tool in both clinical and research applications involving pain management and anesthesia.
  42. Antiarrhythmic Agent

    Mexiletine hydrochloride is an orally active antiarrhythmic agent that primarily functions by inhibiting sodium channels, with an IC50 value of 75±8 μM for tonic block and 23.6±2.8 μM for use-dependent block. This compound has demonstrated efficacy in the management of myotonia and neuropathic pain, making it a valuable tool in both cardiovascular and neurological research. Its ability to modulate ion channel activity allows for insights into the mechanisms of arrhythmias and other related disorders.
  43. Antiarrhythmic Agent

    Disopyramide phosphate is a class IA antiarrhythmic agent that primarily targets cardiac sodium channels, effectively blocking the fast inward sodium current. This compound prolongs cardiac action potentials, making it suitable for the treatment of both ventricular and atrial arrhythmias. In addition, disopyramide phosphate inhibits HERG-encoded potassium channels and exhibits significant negative inotropic effects, contributing to its complex pharmacological profile in heart rhythm management. Its diverse biological activities make it valuable for research in electrophysiology and cardiac pharmacology.
  44. Voltage-operated Sodium Channels Blocker

    Mebeverine hydrochloride is a musculotropic agent acting primarily as a voltage-operated sodium channels blocker. It effectively inhibits intestinal peristalsis and reduces intracellular calcium accumulation, making it valuable for research on gastrointestinal motility disorders. Its ability to modulate sodium channels also supports studies related to excitability in smooth muscle tissues.
  45. Sodium Channel Inhibitor

    Ropivacaine mesylate acts primarily as a sodium channel inhibitor, serving as a long-acting amide local anesthetic. It effectively blocks impulse conduction by reversibly inhibiting sodium ion influx in nerve fibers, making it suitable for procedures requiring spinal block anesthesia. Additionally, Ropivacaine has been identified as an inhibitor of the K2P potassium channel TREK-1, exhibiting an IC50 value of 402.7 μM in COS-7 cell membranes. This compound is relevant for research into pain management and neuronal activity modulation.
  46. Sodium Channel Blocker

    Ajmaline is a sodium channel blocker and a class 1A anti-arrhythmic agent. It effectively inhibits HERG currents with an IC50 of 1 μM in HEK293 cells and 42.3 μM in Xenopus oocytes. This compound is utilized in research focused on ventricular tachyarrhythmia and other cardiac rhythm disorders, contributing to a better understanding of arrhythmic conditions.
  47. Sodium Channel Inhibitor

    Mepivacaine is an amide-type local anesthetic that functions as a sodium channel inhibitor. By binding to specific voltage-gated sodium ion channels in neuronal cell membranes, Mepivacaine effectively inhibits sodium influx and membrane depolarization. This agent is primarily utilized in various research applications within the fields of pain management and anesthesia.
  48. Antitussive Agent

    Benzonatate (PEGn) is a non-narcotic antitussive agent that exerts its effects primarily through sodium channel blockade and local anesthetic activity on respiratory stretch receptors. It is commonly utilized in research involving cough reflex modulation and respiratory control mechanisms. This compound is valuable for studies aimed at understanding cough pathology and developing cough suppression therapies.
  49. 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.
  50. 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.

Items 301-350 of 361

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