Membrane Transporters-Ion Channels

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  1. Serotonin Transporter Inhibitor

    (±)-Duloxetine hydrochloride is a serotonin-norepinephrine reuptake inhibitor targeting the serotonin transporter. This compound exhibits significant analgesic and antidepressant properties, making it valuable in studies related to diabetic neuropathic pain, fibromyalgia, and major depressive disorder. Researchers utilize (±)-Duloxetine hydrochloride to explore its potential therapeutic effects and underlying mechanisms in various neuropathic and mood disorders.
  2. Serotonin Transporter Inhibitor

    (S)-Venlafaxine is a potent serotonin transporter inhibitor that also affects norepinephrine reuptake. This compound is recognized for its antidepressant properties and is utilized in research to investigate mechanisms of mood disorders and neuropharmacology. Its dual inhibitory action on 5-HT and NE transporters makes it a valuable tool for studying depression and anxiety-related pathways.
  3. Fenfluramine Metabolite

    Norfenfluramine is a major brain-penetrant metabolite of Fenfluramine that primarily interacts with 5-HT transporters, facilitating the release of serotonin from neurons. This compound has been observed to exhibit antiepileptic effects in vivo, making it relevant for research in neuropharmacology and the study of serotonin-related disorders. Its efficacy in modulating serotonin levels could provide insights into therapeutic strategies for epilepsy and other neurological conditions.
  4. Serotonin Transporter

    MADAM is a highly selective compound that targets the serotonin transporter (5-HTT) with a Ki value of 1.6 nM. This compound has significant potential as a PET radiotracer, allowing for the visualization of the serotonin transporter in various research applications. Its high affinity for 5-HTT makes it a valuable tool for studying serotonin-related pathways and conditions.
  5. Dual Serotonin and Noradrenaline Monoamine reuptake Inhibitor

    SNRI-IN-1 is a dual serotonin and noradrenaline monoamine reuptake inhibitor that demonstrates significant activity in modulating neurotransmitter levels. With a P-glycoprotein Efflux Ratio of 20, this compound is useful in studying the dynamics of monoamine transport and its implications in mood disorders and cognitive function. Research applications include investigating the effects of dual inhibition on neurotransmission and potential therapeutic benefits in conditions such as depression and anxiety.
  6. Guaiane-type Compound

    Nardoguaianone J is a guaiane-type compound isolated from the roots of Nardostachys chinensis. This compound is known to enhance serotonin transporter (SERT) activity, making it relevant in studies related to serotonin signaling and neurotransmission. Nardoguaianone J is valuable for research into mood regulation, depression, and related neurological disorders.
  7. Serotonin-norepinephrine Reuptake Inhibitor

    Duloxetine-d3 hydrochloride is a deuterium-labeled derivative of Duloxetine hydrochloride, functioning as a serotonin-norepinephrine reuptake inhibitor (SNRI) with a Ki of 4.6 nM. This compound is primarily utilized in research to study the pharmacokinetics and biological effects of Duloxetine in models of major depressive disorder and generalized anxiety disorder. Its stable isotope labeling enables precise tracking in metabolic studies and enhances the understanding of drug metabolism and action mechanisms.
  8. 5-hydroxytryptamine Uptake Inhibitor

    Serotonin azidobenzamidine is a selective inhibitor of 5-hydroxytryptamine (serotonin) uptake, functioning through competitive inhibition. It demonstrates significant biological activity with a Ki value of 130 nM, effectively inhibiting [3H]5-hydroxytryptamine uptake in rat cortical synaptosomes. This reagent is valuable in neuropharmacological research, aiding in the study of serotonin modulation and its effects on various physiological processes.
  9. Venlafaxine Active Metabolite

    Desvenlafaxine succinate is the succinate salt form of the primary active metabolite of Venlafaxine, serving as a selective inhibitor of serotonin and norepinephrine reuptake. It exhibits IC50 values of 47.3 nM for the human serotonin transporter (hSERT) and 531.3 nM for the human norepinephrine transporter (hNET), offering significant potential in modulating neurotransmitter levels. Additionally, Desvenlafaxine succinate demonstrates modest binding affinity at the human dopamine transporter, with 62% inhibition observed at a concentration of 100 μM. This compound is valuable for research in neuropsychiatric conditions and the study of antidepressant mechanisms.
  10. Serotonin Transporter Control

    (1R,4R)-4-(3,4-Dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-amine hydrochloride primarily targets the serotonin transporter, influencing serotonin reuptake mechanisms. This compound serves as a metabolite of the selective serotonin reuptake inhibitor Sertraline, facilitating investigations into its pharmacodynamics and pharmacokinetics. Its relevance in researching mood disorders and antidepressant effects makes it a valuable tool for studies focused on serotonin modulation.
  11. Serotonin Transporter Inhibitor

    (S)-Tomoxetine hydrochloride is a selective serotonin transporter inhibitor known for its ability to modulate serotonin levels in synaptic clefts. With a reported inhibition constant (Ki) of 16.8 nM, it effectively inhibits the reuptake of norepinephrine, thereby influencing neurotransmitter dynamics. This compound is utilized in research focused on neuropharmacology, mood disorders, and the mechanisms of serotonin signaling.
  12. Fluoxetine Derivative

    Norfluoxetine oxalate is an active metabolite of Fluoxetine, functioning primarily as a selective serotonin reuptake inhibitor (SSRI). This compound exhibits significant antidepressant activity, making it a valuable tool in psychiatric research. It is commonly utilized to study the mechanisms of depression and the efficacy of SSRI treatments.
  13. Antidepressant

    (1S,4S)-N-Desmethyl Sertraline hydrochloride is a metabolite of Sertraline, acting primarily as a selective serotonin reuptake inhibitor. This compound exhibits significant antidepressant activity, making it valuable in the study of depression and related disorders. It is utilized in research to investigate serotonin modulation and its effects on mood and behavior.
  14. Serotonin Reuptake Inhibitor

    (S)-Norfluoxetine is a selective serotonin reuptake inhibitor that primarily targets the serotonin transporter. It has been shown to enhance allopregnanolone levels and decrease aggressive behavior in socially isolated murine models. This compound is valuable in research related to neuropharmacology and the understanding of mood and anxiety disorders.
  15. Nervous System Stimulant

    3-Chloroamphetamine hydrochloride is a derivative of amphetamine that acts as a central nervous system stimulant primarily by promoting the release of serotonin and dopamine. This compound exhibits notable effects on mood enhancement and increased energy levels, making it valuable for research into neuropharmacology and the study of stimulant effects on behavior. Its ability to modulate neurotransmitter activity positions it as a useful tool in investigating conditions related to mood disorders and attention.
  16. SERT Inhibitor

    Nardosinonediol is a selective serotonin transporter (SERT) inhibitor. It demonstrates significant modulation of serotonin uptake, making it a valuable tool for studying serotonin-related pathways. This compound is primarily used in research focused on neuropharmacology, mood disorders, and the development of antidepressant therapies.
  17. Serotonin Reuptake Inhibitor

    (Rac)-Dapoxetine hydrochloride is a racemic mixture of Dapoxetine hydrochloride, a selective serotonin reuptake inhibitor (SSRI) that primarily targets serotonin transporters. This compound exhibits notable efficacy in the treatment of premature ejaculation (PE) and is valuable in research aimed at understanding this condition. Its pharmacological profile positions it as a significant tool for studying serotonin-related pathways in human sexual health.
  18. Serotonin Transporter Control

    N-Nitroso fluoxetine is a derivative of fluoxetine that acts as a selective serotonin reuptake inhibitor (SSRI). This compound primarily targets the serotonin transporter, modulating serotonin levels in the synaptic cleft and influencing mood regulation. N-Nitroso fluoxetine is utilized in antidepressant research, contributing to the understanding of serotonin modulation in psychiatric disorders.
  19. Serotonin Reuptake Inhibitor

    DA-8031 is a selective serotonin reuptake inhibitor (SSRI) with oral bioavailability. It demonstrates the ability to modulate serotonin levels, making it a valuable compound for studying conditions related to serotonin dysregulation, particularly premature ejaculation (PE). This compound serves as an important tool for research into therapeutic interventions for PE and related disorders.
  20. Serotonin Reuptake Inhibitor

    Lubazodone is a selective serotonin reuptake inhibitor (SSRI) that primarily targets the serotonin transporter. It exhibits significant antidepressant activity and is utilized in the investigation of various depressive disorders. Research applications include exploring its effects on mood regulation and neurochemical pathways associated with depression.
  21. Stable Isotope

    cis-Dihydro Tetrabenazine-d7 is a deuterium-labeled analog of cis-Dihydro Tetrabenazine, primarily utilized as a stable isotope in research applications. Its incorporation of deuterium enhances the precision of metabolic studies and pharmacokinetic analyses. This reagent is valuable in the investigation of vesicular monoamine transporters and can aid in the understanding of neurological disorders where dopaminergic signaling is implicated.
  22. 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.
  23. Isotope-Labeled Compounds

    Cilnidipine-d3 is a deuterium-labeled derivative of Cilnidipine, primarily acting as a calcium channel blocker. This isotope-labeled compound is valuable for research applications involving pharmacokinetic studies and metabolic profiling. Its use enhances the understanding of Cilnidipine's pharmacological effects and its interactions within biological systems.
  24. Stable Isotope

    Pantoprazole-d4 is a deuterated derivative of Pantoprazole, a potent proton pump inhibitor that targets the H+/K+-ATPase enzyme with an IC50 of 6.8 μM. This stable isotope is utilized primarily in pharmacokinetic studies and metabolic research to enhance the accuracy of drug absorption and distribution analysis. Pantoprazole exhibits anti-secretory and anti-ulcer properties, while its combination with Doxorubicin has been shown to significantly increase tumor growth delay, underscoring its potential utility in cancer research.
  25. Stable Isotope

    Cinnarizine-d8 dihydrochloride is a deuterium-labeled form of the calcium channel blocker Cinnarizine. This stable isotope compound allows for precise tracking and analysis in pharmacokinetic studies. It is primarily utilized in research applications involving metabolic studies and the investigation of drug interactions, enhancing the understanding of pharmacological mechanisms.
  26. Isotope-Labeled Compounds

    Digitoxin-d3 is a deuterated derivative of digitoxin, a cardiac glycoside that primarily targets the Na+/K+ ATPase enzyme, enhancing intracellular calcium levels and improving myocardial contractility. This isotope-labeled compound is utilized in pharmacokinetic studies, providing insights into the metabolism and distribution of digitoxin in biological systems. It serves as a valuable tool for researchers examining heart function and the therapeutic mechanisms of cardiac glycosides.
  27. 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.
  28. Stable Isotope

    Desacetyl Diltiazem-d3 is a deuterium-labeled derivative of Desacetyl Diltiazem, designed to serve as a stable isotope standard in analytical applications. This compound can be employed in pharmacokinetic studies and metabolic labeling to trace drug interactions and bioavailability. Its precise labeling enhances accuracy in mass spectrometry and other analytical techniques, making it an invaluable tool for researchers investigating calcium channel blocking activities and cardiovascular-related pharmacology.
  29. Stable Isotope

    2-[(2-Azidoethoxy-d4)methyl]-4-(2-chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-1,4-dihydropyridine is a deuterium-labeled compound that targets dihydropyridine receptors. This stable isotope variant is significant in researching the pharmacokinetics and metabolic pathways of dihydropyridine derivatives. It is particularly valuable in studies involving the pharmacological effects and interactions of calcium channel blockers, facilitating advanced analysis in medicinal chemistry and drug development.
  30. Calcium Channel Blocker

    Verapamil-d6 hydrochloride is a deuterated derivative of Verapamil, a selective calcium channel blocker. It exhibits potent inhibition of P-glycoprotein (P-gp) and CYP3A4, making it valuable in cardiovascular research, particularly for conditions such as hypertension, arrhythmias, and angina. This isotopically labeled compound aids in pharmacokinetic studies and offers insights into drug metabolism and transport mechanisms.
  31. Stable Isotope

    N-Desalkylflurazepam-d4 is a deuterated analog of N-Desalkylflurazepam, a long-acting metabolite of benzodiazepine compounds, including Flurazepam. This stable isotope is primarily used for research applications involving metabolic studies and pharmacokinetics of benzodiazepines. N-Desalkylflurazepam exhibits inhibitory effects on L-type voltage-gated calcium channels, with reported IC50 values of 55 μM for Cav1.2 and 37 μM for Cav1.3, making it a valuable tool for investigating calcium channel modulation in various biological contexts.
  32. Stable Isotope

    Nifedipine dehydro nitroso-d6 is a deuterium-labeled derivative of Nifedipine dehydro nitroso, primarily utilized as a stable isotope. This compound plays a crucial role in the study of pharmacokinetics and metabolic pathways of calcium channel blockers. Its isotopic labeling facilitates advanced analytical techniques such as mass spectrometry in chemical research applications.
  33. Pregabalin Impurity

    Pregabalin lactam is an impurity of Pregabalin, a compound primarily targeting calcium channels. This metabolite is often utilized in quality control and analytical studies of Pregabalin formulations. Its presence in research can provide insights into compound stability and purity, contributing to a better understanding of Pregabalin's pharmacological profile.
  34. 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.
  35. Pantoprazole Impurity

    Pantoprazole N-oxide is a known impurity associated with the synthesis of Pantoprazole, a proton pump inhibitor (PPI) utilized in the treatment of conditions linked to excessive gastric acid, including gastric ulcers and gastroesophageal reflux disease (GERD). This compound is valuable for analytical research and quality control processes, aiding in the characterization and assessment of Pantoprazole formulations. Its presence in pharmaceutical development highlights the importance of monitoring impurities to ensure product safety and efficacy.
  36. 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.
  37. KM-001 Isomer

    KM-001-E2 is the (S)-enantiomer of KM-001, a selective antagonist of the TRPV3 channel. This compound plays a significant role in investigating the mechanisms underlying skin itching and keratinization disorders. Its application in research may provide insights into TRPV3-related pathophysiology and potential therapeutic strategies for skin conditions.
  38. Drug Isomer

    2-Methylethcathinone hydrochloride is an isomer of the psychoactive compound ethcathinone. It primarily functions as a stimulant, exerting its effects by interacting with monoamine transporters, leading to increased levels of neurotransmitters such as dopamine and norepinephrine. This compound is utilized in research focused on neuropharmacology and the study of designer drugs, contributing to the understanding of their mechanisms of action and potential therapeutic applications.
  39. 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.
  40. Drug Isomer

    2-Methylethcathinone (2-MEC) is an isomer of the psychoactive substance methcathinone, primarily acting as a monoamine transporter inhibitor. This compound exhibits stimulant properties, influencing the release and reuptake of neurotransmitters such as dopamine, norepinephrine, and serotonin. 2-MEC is utilized in research exploring its pharmacological effects, potential therapeutic implications, and the underlying mechanisms of psychostimulants.
  41. Isomer of 4-Bromoamphetamine

    2-Bromoamphetamine hydrochloride is an isomer of 4-Bromoamphetamine, primarily targeting monoamine transporters. This compound exhibits psychoactive properties, influencing neurotransmitter systems such as serotonin and dopamine. It is utilized in scientific research to explore the mechanisms underlying mood regulation and behavioral responses.
  42. VMAT2 Substrate

    FFN 206 dihydrochloride is a selective substrate for the Vesicular Monoamine Transporter 2 (VMAT2), exhibiting an apparent Km of 1.16 μM. This fluorescent probe enables the detection of VMAT2 activity in intact cells via fluorescence microscopy, allowing for the visualization of subcellular localization to VMAT2-expressing acidic compartments while minimizing labeling of other organelles. Its application is essential for studying monoamine transport dynamics and cellular compartmentalization in neurobiological research.
  43. H+, K+-ATPase Inhibitor

    Esomeprazole magnesium, a potent H+, K+-ATPase inhibitor, is utilized in research related to upper intestinal disorders and gastroesophageal reflux disease. Its primary mechanism involves the inhibition of proton pumps, leading to decreased gastric acid secretion. Additionally, Esomeprazole magnesium exhibits properties as an exosome inhibitor by blocking exosome release through the inhibition of vacuolar H+-ATPases, making it valuable for studies on cellular communication and disease progression.
  44. 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.
  45. Anti-malarial Agent

    Quinine hydrochloride dihydrate is an anti-malarial agent primarily known for its inhibitory action on potassium channels. It effectively inhibits wild-type mouse Slo3 (KCa5.1) channel currents in response to voltage pulses, exhibiting an IC50 value of 169 μM. This compound is essential for research into malaria treatment and the study of ion channel modulation in various biological contexts.
  46. 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.
  47. Stable Isotope

    Atazanavir-d9 is a deuterated analog of Atazanavir, a highly selective HIV-1 protease inhibitor. This compound targets the HIV-1 protease enzyme, facilitating the treatment of HIV infections with its ability to inhibit viral replication. Additionally, Atazanavir acts as both a substrate and inhibitor of CYP3A4, as well as an inducer of P-glycoprotein (P-gp). Furthermore, Atazanavir possesses inhibitory activity against SARS-CoV 3CLpro, with an IC50 of 3.49 μM, making it relevant for research in antiviral therapies.
  48. Na+/Ca2+ Channel Blocker

    Flunarizine dihydrochloride is a potent dual blocker of Na+ and Ca2+ channels, specifically targeting T-type calcium channels. This compound exhibits significant anticonvulsant and antimigraine properties, making it valuable for neurological research. Additionally, Flunarizine dihydrochloride demonstrates peripheral vasodilatory effects, enhancing its potential applications in vascular studies.
  49. 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.
  50. 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.

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