Membrane Transporters-Ion Channels

Items 1301-1350 of 2532

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  1. Benzofuran

    4-APB hydrochloride is a benzofuran derivative that acts as a selective serotonin and dopamine reuptake inhibitor. It exhibits significant biological activity, influencing neurotransmitter release and modulating synaptic signaling. 4-APB hydrochloride is commonly utilized in neuropharmacological research to study the effects of monoamine transporters and their role in various neurological disorders. Its properties make it a valuable tool for investigating serotonin and dopamine-related pathways in both in vitro and in vivo studies.
  2. Drug Derivative

    Metfendrazine is a drug derivative that acts primarily as a monoamine transporter inhibitor. It exhibits significant activity in modulating neurotransmitter levels, making it valuable for research in neuropharmacology and behavioral studies. This compound is particularly relevant for investigations into mood disorders and the mechanisms underlying addiction.
  3. Natural Product

    17-Hydroxy Capsaicin is a natural product derived from chili peppers, exhibiting significant activity as a vanilloid receptor (TRPV1) agonist. This compound is known to modulate pain perception and has demonstrated anti-inflammatory properties. Its applications in research include exploring mechanisms of pain relief and the development of novel analgesics, making it a valuable tool in pharmacological studies.
  4. 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.
  5. 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.
  6. Drug Derivative

    MDPT (tBuONE) is a derivative of 3',4'-Methylenedioxy-N-tert-butylcathinone, primarily targeting monoamine transporters. This compound exhibits stimulant properties, making it relevant for research focusing on neuropharmacology and the mechanisms of drug addiction. Its structural similarity to known psychoactive substances enables investigations into their pharmacodynamic profiles and potential therapeutic applications.
  7. 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.
  8. Endogenous Metabolite

    N-Stearoyl Taurine is an endogenous metabolite that exhibits activity as a fatty acyl amide. It demonstrates the ability to activate members of the transient receptor potential (TRP) family of calcium channels, linking it to various physiological processes. This compound is primarily used in research applications related to lipidomics and neurobiology, particularly in studies investigating the role of amino-acyl endocannabinoids in the central nervous system. Its discovery in rat brain lipid profiles underscores its significance in the exploration of neuronal signaling pathways.
  9. Endogenous Metabolite

    N-Lignoceroyl Taurine is an endogenous metabolite and taurine conjugate of lignoceric acid, identified through lipidomic analysis of bovine brain. This compound exhibits distinct biological activity as a substrate for fatty acid amide hydrolase (FAAH), with levels significantly elevated in FAAH knockout mice, indicating a potential role in lipid metabolism. Additionally, N-Lignoceroyl Taurine has been shown to activate transient receptor potential (TRP) calcium channels, including TRPV1 and TRPV4, highlighting its relevance in neurobiology and cellular signaling research.
  10. Natural Products

    Thevetin A is a cardiac glycoside derived from the plant Cascabela thevetioides. It exhibits potent biological activity by inhibiting Na+/K+ ATPase, leading to increased intracellular calcium levels and enhanced contractility of cardiac muscle. This compound is primarily utilized in cardiovascular research to study its effects on cardiac function and potential therapeutic applications in heart disease.
  11. Endogenous Metabolite

    UCCF-029 free base is a potent activator of the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel. This compound showcases enhanced activity due to the benzannulation of the flavone A-ring at the 7,8-position, serving as a critical structural reference for the development of more effective flavonoid analogues. UCCF-029 demonstrates superior potency compared to apigenin in activating wild-type CFTR and possesses potential for activating the mutant G551D-CFTR, though its efficacy in this regard is not as pronounced as that of apigenin. This reagent is valuable for research into cystic fibrosis and related therapeutic strategies.
  12. Endogenous Metabolite

    ISQ-1 hydrochloride is an isoquinolinone compound that functions as an inhibitor of the IKur potassium channel. It demonstrates potential to influence cardiac electrophysiology by modulating arrhythmic activity in atrial tissues. This reagent is primarily utilized in research focused on cardiac rhythm disorders and electrophysiological studies of heart functions.
  13. Endogenous Metabolite

    D-myo-Inositol-1,4,5,6-tetraphosphate (D-Ins(1,4,5,6)P4) functions primarily as an endogenous metabolite involved in cellular signaling pathways. This compound exhibits a strong inhibitory effect on calcium-activated chloride channels, effectively operating at concentrations of 8-10 μM. It is commonly utilized in research applications focused on signal transduction and ion channel regulation.
  14. Biochemical Reagent

    D-myo-Inositol-4,5-diphosphate sodium is a critical biochemical reagent that functions as a second messenger in cellular signaling pathways. It primarily targets calcium channels, facilitating the release of intracellular calcium when it binds to its receptor on the endoplasmic reticulum. This compound is valuable for research applications investigating signal transduction, calcium homeostasis, and cellular responses in various biological systems.
  15. Endogenous Metabolite

    Stearoyl serotonin is a hybrid compound designed to target the endogenous metabolite systems and is structurally derived from arachidonoyl serotonin. This compound is investigated for its ability to function as a dual antagonist of fatty acid amide hydrolase (FAAH) and the TRPV1 channel, which are critical pathways in the modulation of pain. Preliminary studies suggest that modifications to the arachidonoyl structure, such as the introduction of an 18-carbon stearoyl moiety, may influence TRPV1 channel activity; replacement with saturated fatty acids has demonstrated significant inhibition of capsaicin-induced activation. This positions stearoyl serotonin as a potential candidate for research into pain mechanisms and therapeutic applications.
  16. Endogenous Metabolite

    SU200 is a TRPV1 agonist that modulates intracellular calcium ion concentrations. It induces distinct calcium ion response patterns, displaying notable reactivity and peak efficacy. The effects of SU200 exhibit varying degrees of response delay and variability across different cell types. This compound offers potential avenues for pharmacological development and further research into calcium signaling pathways.
  17. 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.
  18. 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.
  19. 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.
  20. 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.
  21. 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.
  22. 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.
  23. 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.
  24. 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.
  25. AMPA Receptor Modulator

    AMPA Receptor Modulator-2 is a selective modulator of AMPA receptors, demonstrating a pIC50 of 10.1 for TARPγ8-dependent AMPA receptor activity. This compound enhances synaptic transmission and plasticity, making it a valuable tool for research in neuropharmacology and cognitive disorders. Its ability to influence excitatory neurotransmission positions it as a potential candidate for studies related to neurodegenerative diseases and memory enhancement.
  26. Anti-parkinson Agent

    Budipine is an anti-Parkinson agent that acts primarily as an N-methyl-D-aspartate (NMDA) antagonist while also influencing dopaminergic activity. It enhances dopamine release and inhibits monoamine oxidase type B (MAO-B), contributing to its therapeutic effects. As a substrate of P-glycoprotein (P-gp), Budipine's uptake into the brain is mediated by this transport mechanism. This compound is valuable for research into central nervous system disorders, including Parkinson's disease.
  27. AMPA Modulator

    ZCAN262 is an allosteric modulator of AMPA receptors that effectively inhibits AMPA-mediated excitotoxicity. By targeting a specific allosteric binding site, ZCAN262 enhances the regulation of synaptic transmission. This compound is relevant for research focused on neuroprotection and synaptic plasticity, making it a valuable tool in studies of neurodegenerative diseases and cognitive function.
  28. AMPA Receptor Positive Allosteric Modulator

    AMPA receptor modulator-10 is a positive allosteric modulator of the AMPA receptor, specifically targeting the GluA2 subtype with a potent pEC50 of 5.0. This compound enhances glutamate-induced calcium influx and current responses, demonstrating significant potential for reversing memory impairment induced by Scopolamine. AMPA receptor modulator-10 is applicable in research focused on neurological diseases, including schizophrenia, aiming to improve cognitive function and understanding of synaptic plasticity.
  29. AMPA Antagonist

    BDZ-g is a potent and selective antagonist of the AMPA receptor, a key component in excitatory neurotransmission. This compound demonstrates significant biological activity in modulating synaptic transmission, making it valuable for research related to neurological disorders characterized by excessive AMPA receptor activity, such as epilepsy and neurodegenerative diseases. BDZ-g can serve as an important tool in understanding the role of AMPA receptors in various pathophysiological conditions.
  30. D15

    AMPAR Inhibitor.

    D15 is an AMPA receptor (AMPAR) endocytosis inhibitor derived from a 15 amino acid segment of dynamin. It inhibits the interaction of dynamin with amphiphysin 1 and 2, leading to a significant increase in AMPAR excitatory postsynaptic potential (EPSC) amplitude in medium spiny neurons (MSNs) within Sapap3 knockout mice. This peptide has valuable applications in the investigation of neuropsychiatric disorders and related signaling pathways.
  31. AMPA Receptor Modulator

    AMPA Receptor Modulator-3 is an allosteric modulator of the AMPA receptor, exhibiting an EC50 of 4.4 μM. This compound is valuable for investigating the role of AMPA receptors in the mammalian nervous system, particularly in studies related to learning and memory processes. Its modulation of glutamatergic signaling makes it a pertinent tool for neurological research and drug development targeting cognitive functions.
  32. GluR1/2/AMPA Receptor Agonist

    Cl-HIBO is a highly selective agonist for the GluR1 and GluR2 subtypes of AMPA receptors, exhibiting EC50 values of 4.7 μM and 1.7 μM, respectively. This compound demonstrates potent activity as an AMPA receptor agonist with an IC50 of 0.22 μM. Additionally, Cl-HIBO displays desensitizing properties, making it a valuable tool for research in neuropharmacology and studies of synaptic transmission.
  33. AMPA Receptor Activator

    NPEC-caged-(S)-AMPA is a photolabile caged analog of (S)-AMPA, specifically designed to target and activate AMPA receptors. This compound utilizes the NPEC photoprotecting group to selectively release (S)-AMPA upon illumination, enabling precise spatial and temporal control of receptor activation. It serves as a valuable tool in neuroscience research, facilitating studies on synaptic transmission and signal transduction pathways mediated by glutamate receptors.
  34. AMPA Receptor Modulator

    AMPA receptor modulator-11 is a positive allosteric modulator of the AMPA receptor, enhancing synaptic transmission and promoting excitatory neurotransmission. This compound plays a significant role in research related to neuropsychiatric disorders such as depression, schizophrenia, Alzheimer’s disease, and attention deficit hyperactivity disorder (ADHD). Its ability to selectively target AMPA receptors makes it an essential tool for exploring therapeutic strategies in these conditions.
  35. AMPA Receptor Modulator

    JNJ-56022486 is a potent negative modulator of the AMPA receptor, exhibiting a Ki value of 19 nM and selective antagonism for TARP-γ8. This compound demonstrates effective blood-brain barrier permeability, making it suitable for in vivo studies. JNJ-56022486 is primarily utilized in research focused on epilepsy and related neurological disorders, providing a valuable tool for investigating synaptic transmission and excitability in the central nervous system.
  36. AMPA Receptor Antagonist

    CP-465022 hydrochloride is a selective noncompetitive antagonist of the AMPA receptor, exhibiting significant anticonvulsant activity. It effectively inhibits kainate-induced responses in rat cortical neurons with an IC50 of 25 nM. This compound serves as a valuable tool for exploring the physiological and pathophysiological roles of AMPA receptors in various neurological contexts.
  37. 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.
  38. 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.
  39. AMPA Receptor Antagonist

    ZK 187638 is an AMPA receptor antagonist that effectively inhibits kainate-induced currents in cultured hippocampal neurons, demonstrating noncompetitive antagonism with an IC50 of 3.4 μM. This compound is valuable for research applications focused on synaptic transmission, neuroprotection, and the study of excitotoxicity in neurodegenerative disorders.
  40. AMPA Receptor Antagonist

    YM928 is a noncompetitive antagonist of the α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor. This compound effectively inhibits AMPA receptor-mediated neurotoxicity in primary rat hippocampal cultures with an IC50 of 2 μM. Additionally, YM928 blocks AMPA-induced intracellular calcium influx (IC50 of 3 μM) and antagonizes AMPA-induced inward currents (IC50 of 1 μM). It holds potential for research into various neurological disorders.
  41. AMPA Receptor Antagonist

    AMPA receptor antagonist-3 is a selective antagonist of the AMPA receptor, which plays a critical role in excitatory neurotransmission in the central nervous system. This compound is valuable for studying neurological disorders that involve dysregulation of glutamate signaling, such as epilepsy, Alzheimer's disease, and neurodegenerative conditions. Its utility in research enables the exploration of therapeutic strategies targeting excitatory neurotransmission.
  42. AMPA Receptor Antagonist

    LY 215490 is a selective, competitive antagonist of the AMPA receptor, exhibiting inhibitory potency with IC50 values of 4.8 μM against AMPA, 26.4 μM against CGS 19755, and 247 μM against kainate. This compound demonstrates neuroprotective effects, particularly in the context of focal ischaemia. LY 215490 serves as a valuable tool in studying excitatory neurotransmission and its implications in neurodegenerative diseases.
  43. AMPA Receptor Antagonist

    CP-465022 maleate is a potent, selective noncompetitive antagonist of the AMPA receptor, exhibiting anticonvulsant properties. It effectively inhibits kainate-induced responses in rat cortical neurons with an IC50 of 25 nM. This compound serves as a valuable research tool to explore the role of AMPA receptors in both physiological and pathophysiological contexts.
  44. 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.
  45. AMPA Receptor Modulator

    AMPA Receptor Modulator-5 functions as a modulator of AMPA receptors, which are critical for fast excitatory synaptic transmission in the central nervous system. This compound has demonstrated potential in the research of neurological diseases by influencing synaptic plasticity and neurotransmission. Its application extends to studies focused on cognitive functions and neurodegenerative disorders, making it a valuable tool for exploring therapeutic strategies in neuroscience.
  46. AMPA Receptor Blocker

    Gamma-DGG acetate is a competitive antagonist of the AMPA receptor, exerting its effects by inhibiting excitatory glutamatergic neurotransmission. By blocking AMPA receptors, this compound modulates excitatory post-synaptic potentials (e.p.s.p.s) and is valuable in research focused on neurological processes, synaptic plasticity, and related disorders. Its reversible action makes it an essential tool for studying receptor dynamics and synaptic function in various experimental settings.
  47. AMPA Antagonist

    EGIS-8332 is a non-competitive antagonist of the AMPA receptor, effectively inhibiting AMPA-mediated currents in rat cerebellar Purkinje cells. It demonstrates a potent capability to block AMPA- and Quisqualate-induced excitotoxicity in primary cultures of telencephalon neurons, with an IC50 ranging from 5.1 to 9.0 μM. EGIS-8332 exhibits notable anticonvulsant and neuroprotective properties, making it a valuable tool for research in neurological diseases.
  48. σ Receptor Agonist

    threo-Ifenprodil hemitartrate is a sigma (σ) receptor agonist, exhibiting Kis of 59.1 nM and 2 nM for σ1 and σ2 receptors, respectively. This compound also acts as a NR2B subunit-selective NMDA receptor antagonist, with an IC50 of 0.22 μM, and demonstrates inhibition of the hERG potassium channel with an IC50 of 88 nM, indicating potential antiarrhythmic activity. threo-Ifenprodil hemitartrate serves as a valuable tool in neuropharmacology and cardiovascular research.
  49. AMPA Receptor Antagonist

    YM 900 is an AMPA receptor antagonist that selectively inhibits excitatory neurotransmission mediated by AMPA receptors. Its primary mechanism involves blocking the receptor's ion channel, thereby reducing the influx of sodium ions. This compound is valuable in research applications focused on neuroprotection, synaptic plasticity, and the study of neurological disorders related to glutamatergic signaling. Researchers may utilize YM 900 to investigate the role of AMPA receptors in various models of brain function and pathology.
  50. AMPA Receptor Antagonist

    AMPA Receptor Antagonist-2 is a potent antagonist of the AMPA receptor, a subtype of glutamate receptor involved in synaptic transmission. By inhibiting AMPA receptor activity, this compound plays a crucial role in research related to excitatory neurotransmission, neuroprotection, and various neurodegenerative diseases. Its application extends to studying synaptic plasticity and the mechanisms underlying conditions such as epilepsy and chronic pain.

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