Sodium Channels

Items 151-200 of 361

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  1. Paralytic Shellfish Poisoning Toxin

    Gonyautoxin III (GTX-III) is a potent paralytic shellfish poisoning toxin that acts by blocking voltage-gated sodium channels at the axonal level, displaying an IC50 of 14.9 nM. This inhibition disrupts the propagation of nerve impulses, leading to significant neurotoxicity. Gonyautoxin III demonstrates cytotoxic activity against mouse neuroblastoma cells, making it a valuable tool for research focused on cancer biology and neurological disorders.
  2. Sodium Channel Blocker

    N-Depropylpropafenone is a sodium channel blocker and an active metabolite of Propafenone, produced primarily by the CYP450 enzyme system, particularly CYP2D6. It inhibits sodium ion channels, leading to a reduction in myocardial conduction velocity and displaying antiarrhythmic properties. This compound is valuable in the study of cardiac physiology and the mechanisms of arrhythmias.
  3. NaV1.7 Inhibitor

    Sodium Channel-IN-8 is a potent inhibitor of the voltage-gated sodium channel NaV1.7. It has demonstrated significant activity in modulating pain pathways, making it a valuable tool for research into pain mechanisms and therapeutic interventions. This compound is suitable for studies focused on pain management and related neurological disorders.
  4. Stable Isotope

    Licarbazepine-d8 is a deuterium-labeled derivative of Licarbazepine, a potent voltage-gated sodium channel blocker known for its anticonvulsant and mood-stabilizing properties. The stable isotope labeling enhances research applications in pharmacokinetic studies and metabolic investigations of Licarbazepine. This compound is valuable for elucidating the mechanisms of action and efficacy of sodium channel modulation in neurological disorders.
  5. Sodium Channel Inhibitor

    Atelopidtoxin, a sodium channel inhibitor derived from the Panamanian frog Atelopus zeteki, exhibits potent biological activity with an LD50 of 0.016 mg/kg in mice. Its effects include inducing hypotension and ventricular fibrillation in rabbit models, making it a valuable reagent for research focused on cardiovascular physiology and sodium channel function. This compound serves as a significant tool for studies investigating the physiological and pharmacological roles of sodium channels.
  6. Stable Isotope

    Propafenone-d5 Ethyl hydrochloride is a deuterium-labeled derivative of Propafenone hydrochloride, an anti-arrhythmic medication classified as a Class 1C agent. It primarily targets sodium channels to inhibit cardiac arrhythmias, making it effective in managing conditions such as atrial and ventricular arrhythmias. This stable isotope is valuable for pharmacokinetic studies and metabolic investigations in cardiovascular research applications.
  7. Stable Isotope

    Methocarbamol-d3 is a deuterium-labeled analog of Methocarbamol, a centrally acting muscle relaxant that targets the Nav1.4 sodium channel. This stable isotope aids in studies related to muscle spasms and pain syndromes by providing insights into the voltage-dependent inactivation mechanisms of the Nav1.4 channel. Its unique labeling facilitates enhanced tracking and analysis in pharmacokinetic and metabolic studies.
  8. Stable Isotope

    Atomoxetine-d7 is a stable isotope-labeled form of Atomoxetine, a selective norepinephrine reuptake inhibitor. With Ki values of 5, 77, and 1451 nM for norepinephrine, serotonin, and dopamine transporters, respectively, it is known to enhance catecholaminergic neurotransmission and elevate dopamine and norepinephrine levels in the prefrontal cortex. Additionally, Atomoxetine functions as a potent blocker of voltage-gated sodium channels. This reagent is applicable in research focused on attention-deficit hyperactivity disorder (ADHD) and related neural mechanisms.
  9. NaV1.7 Inhibitor

    GNE-3565 is a potent NaV1.7 inhibitor belonging to the arylsulfonamide class, exhibiting subnanomolar potency for channel blockade with mixed subtype selectivity. This compound is primarily utilized in research focusing on pain mechanisms and is instrumental in studying pain pathways and the development of novel analgesics.
  10. Sodium Channel Inhibitor

    CL-424032 is a selective sodium channel inhibitor that modulates neuronal excitability. It has demonstrated efficacy in reducing action potential firing in various neuronal models. This compound serves as a valuable tool in the study of neuropathic pain and various cardiovascular disorders, making it relevant for research in neurobiology and pharmacology.
  11. Sodium Channel Inhibitor

    LG 83-6-05 is a selective inhibitor of sodium channels, exhibiting potent effects on sodium ion permeability. This compound is primarily utilized in research focused on cardiac rhythm disorders, as it can help elucidate the role of sodium channels in arrhythmogenesis and related pathophysiological conditions. Additionally, LG 83-6-05 may serve as a valuable tool in the development of therapeutic strategies targeting sodium channel dysfunction.
  12. Antiarrhythmic Agent

    Pentisomide is an orally active antiarrhythmic agent that primarily targets sodium channels. It exhibits Vaughan-Williams class I antiarrhythmic activity, making it useful in the management of various arrhythmias. This compound is valuable for research applications exploring cardiac electrophysiology and the mechanisms of arrhythmia modulation.
  13. Sodium Channel Inhibitor

    (R)-(+)-Bupivacaine hydrochloride is a selective inhibitor of voltage-gated sodium channels. By blocking these channels on nerve cell membranes, it effectively inhibits sodium ion influx, thereby preventing the generation and conduction of nerve impulses, which results in local anesthetic activity. This compound is particularly relevant in the study of acute pain mechanisms and pain management strategies in research settings.
  14. Sodium Channel Modulator

    PF-05661014 is a selective sodium channel modulator that primarily targets the Nav1.3 and Nav1.7 currents. By stabilizing inactivated channels through its interaction with the D4 voltage-sensor domain (VSD), PF-05661014 serves as an important tool in the study of sodium channel modulation. This reagent is valuable for research applications focused on understanding the role of sodium channels in various physiological and pathological processes.
  15. Sodium Channel blocker

    Ralitoline is a sodium channel blocker with an IC50 of 2 μM. It exhibits anticonvulsant activity, making it a valuable tool for research in epilepsy and related neurological disorders. Ralitoline's ability to modulate sodium channel activity supports its potential in pharmacological studies aimed at understanding seizure mechanisms and developing therapeutic interventions.
  16. Deuterated Licarbazepine

    Licarbazepine-d3 is the deuterated form of Licarbazepine, a potent blocker of voltage-gated sodium channels. This compound exhibits significant anticonvulsant properties and mood-stabilizing effects, making it valuable in neurological research and the study of mood disorders. Licarbazepine-d3 is utilized in various applications, including metabolic studies and pharmacokinetic investigations, leveraging its isotopic labeling for enhanced analytical sensitivity.
  17. Sodium Channel Inhibitor

    Propafenone-d7 hydrochloride is a deuterated derivative of Propafenone, primarily acting as a sodium channel inhibitor. It exhibits significant anti-arrhythmic activity, making it valuable in the study of cardiac arrhythmias. This compound can be utilized in pharmacokinetic studies and metabolic tracing in research applications related to cardiac electrical activity and drug metabolism.
  18. Sodium Channel Blocker

    NaV1.7 blocker-801 is a selective blocker of voltage-gated sodium channel NaV1.7, crucial for neuronal excitability and pain signaling. This compound is primarily used in the investigation of pain pathways and neurological disorders, offering insights into potential therapeutic strategies for conditions such as neuropathic pain and other related diseases. Researchers can utilize NaV1.7 blocker-801 to explore its effects on neuronal activity and pain modulation in various experimental settings.
  19. Sodium Channel Control

    Lamotrigine N2-Oxide is a metabolite of the anticonvulsant agent Lamotrigine, targeting sodium channels to modulate neuronal excitability. This compound is primarily utilized in the study of epilepsy and related neurological disorders, providing insights into the pharmacological profiles of sodium channel modulators. Its role in research facilitates a better understanding of mechanisms underlying anticonvulsant activity and the potential development of novel therapeutic strategies.
  20. Stable Isotope

    Mexiletine-d6 is a deuterated form of Mexiletine, an orally bioavailable antiarrhythmic compound known for its ability to alleviate myotonia and neuropathic pain. This reagent functions primarily by blocking sodium channels, demonstrating an IC50 of 75±8 μM for tonic block and 23.6±2.8 μM for use-dependent block. Its unique isotopic labeling makes Mexiletine-d6 suitable for applications in cardiovascular and neurological research, allowing for enhanced tracing and understanding of molecular interactions in biological systems.
  21. Pyrethroid Insecticide

    Zeta-Cypermethrin is a type II pyrethroid insecticide that primarily targets voltage-gated sodium channels in neuronal cells. Its mechanism leads to delayed channel closure, resulting in sustained nerve excitation and convulsions. Notably, Zeta-Cypermethrin promotes high metabolic resistance in Drosophila, which can be assessed through screening, and demonstrates in vitro genotoxicity in human peripheral blood lymphocytes, making it relevant for studies in neurotoxicity and resistance mechanisms.
  22. Sodium Channel Antagonist

    (5R)-BW-4030W92 is a sodium channel antagonist that targets voltage-gated sodium channels in a non-selective and use-dependent manner. This compound exhibits significant biological activity by inhibiting sodium channel-mediated excitability, making it of interest in research on pain management, epilepsy, and neuroprotection. Its pharmacological properties provide a valuable tool for investigating the role of sodium channels in various physiological and pathological processes.
  23. TRPM8 Channel Blocker

    AMTB hydrochloride is a selective antagonist of the TRPM8 channel, effectively inhibiting icilin-induced TRPM8 activation with a pIC50 of 6.23. This reagent is valuable in the study of overactive bladder conditions and painful bladder syndrome. Additionally, AMTB hydrochloride exhibits non-selective inhibition of voltage-gated sodium channels, providing a broader context for its use in electrophysiological research.
  24. Stable Isotope

    Zonisamide-13C2,15N is a deuterated derivative of Zonisamide, designed to serve as a stable isotope for various research applications. Its primary mechanism targets multiple neuronal pathways, primarily focusing on inhibiting voltage-gated sodium channels and modulating neurotransmitter release. This stable isotope variant is invaluable in pharmacokinetic studies, metabolic labeling, and tracer applications, enabling enhanced tracking of Zonisamide in biological systems.
  25. Isotope-Labeled Compound

    Dibucaine-d9 is a deuterium-labeled derivative of dibucaine, a potent sodium channel inhibitor. It serves as a selective inhibitor of pseudocholinesterase (SChE), making it valuable for studying cholinergic signaling. This isotope-labeled compound is particularly useful in pharmacokinetic studies and metabolic profiling, providing insights into drug metabolism and safety evaluation in chemical research.
  26. Stable Isotope

    Atomoxetine-d5 is a deuterium-labeled derivative of Atomoxetine, a selective norepinephrine reuptake inhibitor that demonstrates Ki values of 5, 77, and 1451 nM for norepinephrine (NE), serotonin (5-HT), and dopamine (DA) transporters, respectively. This compound enhances catecholaminergic neurotransmission and increases DAEX and NEEX levels in the prefrontal cortex (PFC). Atomoxetine-d5 is valuable for research applications related to attention-deficit hyperactivity disorder (ADHD) and the study of sodium channel (VGSC) modulation.
  27. Cypermethrin Isomer

    (1R,2S,1'R)-Cypermethrin is a specific isomer of the pyrethroid pesticide Cypermethrin, classified as Class II due to its moderate toxicity. This compound exhibits significant neurotoxic activity by interacting with voltage-gated sodium channels, leading to prolonged neuronal depolarization. (1R,2S,1'R)-Cypermethrin is primarily employed in research focusing on its effects on nervous system function and insecticidal action. Its ability to cross the blood-brain barrier allows for studies on its impact on both invertebrate and vertebrate models.
  28. Tropane

    Tropacocaine hydrochloride is a tropane derivative that acts primarily as a local anesthetic by blocking sodium channels in neuronal membranes. Its key biological activity includes analgesic effects, making it valuable in pain research and studies of neuronal signaling. Tropacocaine hydrochloride is utilized in investigations of tropane-based compounds and their pharmacological profiles in the context of neurological studies.
  29. Drug Derivative

    Piridocaine hydrochloride is a derivative of ortho-aminobenzoic acid and functions as a local anesthetic agent. It primarily acts by blocking sodium channels, thereby inhibiting action potential propagation in excitable membranes. This compound plays a significant role in research related to pain management, neuromuscular function, and pharmacological studies of anesthetics. Its unique pharmacological profile makes it a valuable tool for investigating local anesthetic mechanisms and applications in various biological systems.
  30. Drug Impurity

    Ranolazine impurity 10 is a chemical impurity associated with the cardiovascular drug Ranolazine, which primarily targets sodium channels. This impurity is significant for analytical and quality control purposes in pharmaceutical research and development, aiding in the assessment of the drug's purity and safety profile. Its identification and quantification are critical for compliance with regulatory standards in the drug manufacturing process.
  31. Phosphate Ester Prodrug

    Fosphenytoin is a phosphate ester prodrug that acts as a rapid-acting antiepileptic agent, primarily targeting sodium channels to stabilize neuronal membranes. It demonstrates significant efficacy in the acute management of seizures, particularly in emergency settings. Fosphenytoin's formulation allows for convenient intravenous and intramuscular administration, reducing the risk of local adverse reactions and facilitating effective treatment in acute care situations.
  32. Drug Impurity

    N-(2,6-dimethylphenyl)-2-(ethyl(methyl)amino)acetamide hydrochloride is a recognized impurity associated with the sodium channel inhibitor Lidocaine. This compound may serve as a reference standard for quality control and analytical studies within pharmacological research. It can aid in the assessment of drug purity and the validation of analytical methods used in drug development and manufacturing processes.
  33. Alkaloid

    Lipoaconitine is a natural alkaloid known for its regulatory effects on voltage-gated sodium channels. It exhibits notable biological activity, including analgesic and anti-inflammatory properties, making it a valuable tool for research in pain management and neurobiology. Its unique pharmacological profile provides insights into the mechanisms underlying sodium channel modulation and potential therapeutic applications.
  34. Drug Derivative

    Flumethrin is a synthetic pyrethroid insecticide that acts primarily by modulating sodium channels in the nervous system of insects, leading to paralysis and death. This compound exhibits potent insecticidal activity against a wide range of pests, making it valuable in agricultural and veterinary applications. Flumethrin is primarily utilized in research settings to study insect behavior, insecticide resistance, and neurological pathways relevant to pest control strategies.
  35. Tocainid Analog

    2-Amino-N-phenylpropanamide hydrochloride is an analog of Tocainid, an antiarrhythmic agent that modulates cardiac sodium channels. This compound exhibits potential in cardiac research by influencing ion channel function and demonstrating effects on arrhythmia management. It serves as a valuable tool for studies related to cardiovascular pharmacology and the development of novel antiarrhythmic therapies.
  36. Drug Derivative

    Leucinocaine is a drug derivative that acts as a local anesthetic by inhibiting sodium channel activity, thereby blocking nerve impulse conduction. Its primary biological activity involves pain relief in localized areas, making it useful for various clinical and research applications in pain management and anesthetic studies. This compound can also serve as a valuable tool in neuropharmacological research and the development of new analgesic agents.
  37. Drug Impurity

    Lidocaine impurity 12 is a known impurity of the local anesthetic Lidocaine, which primarily acts as a sodium channel blocker. This compound is valuable for research involving drug formulation and stability studies, as it aids in understanding the impact of impurities on pharmacological profiles. Its characterization is essential for ensuring the quality and safety of Lidocaine-containing formulations.
  38. Drug Derivative

    Nav1.7-IN-17 is a derivative compound targeting the voltage-gated sodium channel NaV1.7. This compound demonstrates significant inhibitory activity, making it a valuable tool for studying pain mechanisms and nociception. Its application is particularly relevant in pain research and the development of novel analgesics.
  39. Anesthetic Agent

    Clibucaine is a piperidine derivative with potent local anesthetic properties. It functions by blocking sodium channels, thereby inhibiting neuronal excitability and transmission of pain signals. This compound is primarily utilized in pain management applications, particularly for localized pain relief during surgical procedures and other medical interventions.
  40. Antiarrhythmic Agent

    Droxicainide hydrochloride is an antiarrhythmic agent primarily targeting sodium channels. It is effective in the management of ventricular arrhythmias and is utilized in research to investigate cardiac electrophysiology. The compound is valuable for studying interactions in cardiac tissues and assessing the effects of sodium channel modulation on heart rhythm disorders.
  41. Furin Inhibitor

    BOS-318 is a highly selective and cell-permeable inhibitor of furin, exhibiting an IC50 value of 1.9 nM. This compound demonstrates the ability to protect epithelial sodium channels (ENaC) from activation by neutrophil elastase. BOS-318 is a valuable tool for research focused on cystic fibrosis and related pulmonary conditions.
  42. 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.
  43. 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.
  44. 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.
  45. NMDA Receptor Antagonist

    Remacemide hydrochloride is a weak uncompetitive antagonist of the NMDA receptor, exhibiting IC50 values of 68 μM for MK-801 binding and 76 μM for NMDA-induced currents. As a moderate inhibitor of sodium channels, this compound demonstrates anticonvulsant properties, making it a valuable tool in the study of neuropharmacology. Research applications include investigating mechanisms underlying seizure disorders and testing potential therapeutic approaches for neurological conditions.
  46. AMPA Receptor Antagonist

    Irampanel is an AMPA receptor antagonist that selectively blocks excitatory neurotransmission by inhibiting AMPA receptor activity. Additionally, it acts as a voltage-dependent sodium channel blocker, leading to a decrease in neuronal excitability. This compound has demonstrated efficacy in reducing kainate-induced currents in rat cortical neurons, making it a valuable tool for research applications related to neuropharmacology and the investigation of excitatory synaptic transmission.
  47. AMPA Receptor Antagonist

    Irampanel hydrochloride is a potent antagonist of the AMPA receptor, acting primarily on excitatory glutamate signaling pathways. This compound effectively blocks voltage-dependent sodium channels and inhibits kainic acid-induced currents in rat cortical neurons. It is primarily used in research applications focused on neuroprotection, synaptic plasticity, and the study of neurodegenerative diseases.
  48. NET Inhibitor

    Nisoxetine is a potent and selective inhibitor of the norepinephrine transporter (NET) with a Kd of 0.76 nM. This compound exhibits antidepressant properties and functions as a local anesthetic, in addition to blocking voltage-gated sodium channels. Its mechanisms make it valuable for research in neuropharmacology and the investigation of depression and pain pathways.
  49. Sodium-Calcium Exchanger Inhibitor

    KB-R7943 is a selective inhibitor of the sodium-calcium exchanger, exhibiting an IC50 value of 5.1 µM. This compound is utilized as a valuable tool in studies involving cardiac and renal failure models, facilitating research into calcium homeostasis and its implications in heart and kidney function.
  50. Sodium Channel Inhibitor

    Benzamil is a sodium channel inhibitor, functioning as a non-selective blocker of epithelial sodium channels (ENaC) and a Na+/Ca2+ exchanger (NCX) inhibitor with an IC50 value of approximately 100 nM. Its pharmacological properties include the enhancement of myogenic vasoconstriction. Additionally, Benzamil inhibits TRPP3-mediated Ca2+-activated currents, exhibiting an IC50 of 1.1 μM. This compound is valuable for research applications focused on cardiovascular physiology and electrolyte transport mechanisms.

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