Isotope-Labeled Compounds

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  1. Stable Isotope

    Z-Doxepin-d3 Hydrochloride is a deuterated stable isotope of the active metabolite 7-Hydroxychlorpromazine hydrochloride, known for its dopaminergic activity. This compound enhances prolactin levels and dopaminergic turnover, leading to sedative effects in animal models. It is utilized in research focusing on psychosis and the modulation of amphetamine-induced stereotypic behaviors in rats, making it a valuable tool for studying neuropharmacological mechanisms.
  2. Stable Isotope

    Itopride-d6 hydrochloride is a deuterium-labeled derivative of Itopride hydrochloride that serves as a stable isotope. Itopride functions as a gastroprokinetic agent by inhibiting acetylcholinesterase (AChE) and antagonizing dopamine D2 receptors. This compound is valuable for studies investigating gastrointestinal motility and neurotransmitter interactions, as well as for tracing and quantifying its metabolic pathways in biological research.
  3. Stable Isotope

    Desmethyl cariprazine-d8 is a deuterium-labeled analog of desmethyl cariprazine, a prominent active metabolite of cariprazine. This compound demonstrates significant affinity for human dopamine D2 and D3 receptors, with pEC50 values of 8.90 and 8.09, respectively, as well as a pEC50 of 6.28 at serotonin 5-HT1A receptors. Desmethyl cariprazine-d8 effectively inhibits forskolin-induced cAMP production and suppresses serotonin-induced Ca2+ release at the 5-HT2B receptor. Its utility is particularly relevant in research focused on mental health disorders such as schizophrenia and bipolar disorder type I.
  4. Stable Isotope

    Dexpramipexole-d3 dihydrochloride is a deuterium-labeled derivative of Dexpramipexole, which acts as a neuroprotective agent and a weak non-ergoline dopamine agonist. This stable isotope is useful in tracing studies and pharmacokinetic investigations, allowing researchers to monitor drug metabolism and distribution. Its applications extend to studies focusing on neurodegenerative diseases and the modulation of dopaminergic pathways in various biological contexts.
  5. Stable Isotope

    Ropinirole-d4 hydrochloride is a deuterium-labeled derivative of Ropinirole hydrochloride, functioning primarily as a selective D2/D3 receptor agonist. It exhibits a Kiof of 29 nM for the D2 receptor and demonstrates pEC50 values of 7.4, 8.4, and 6.8 for human D2, D3, and D4 receptors, respectively. With its specific action and lack of affinity for D1 receptors, Ropinirole-d4 is particularly valuable in investigations related to Parkinson's disease and receptor pharmacology.
  6. Stable Isotope

    Didesmethyl cariprazine-d8 is a deuterium-labeled derivative of didesmethyl cariprazine, a metabolite of the antipsychotic drug Cariprazine. This compound acts as a partial agonist at dopamine D2 and D3 receptors, a full agonist at the serotonin 5-HT1A receptor, and an antagonist at the 5-HT2B receptor. Its activity has been shown to dose-dependently inhibit the spontaneous firing of rat midbrain dopaminergic neurons, making it valuable for research in psychiatric disorders and neuropharmacology.
  7. Stable Isotope

    Molindone-d8 is a deuterated form of the antipsychotic agent molindone, primarily used as a stable isotope in scientific research. Its primary mechanism involves dopamine receptor antagonism, reducing the effects of dopamine and helping to mitigate symptoms of schizophrenia. This labeled compound is particularly valuable in pharmacokinetic studies and metabolic research, allowing for precise tracking and analysis of drug behavior in biological systems.
  8. Stable Isotope

    Ropinirole-d14 hydrochloride is a deuterated analog of Ropinirole hydrochloride, functioning primarily as a D3/D2 receptor agonist. It exhibits a Ki value of 29 nM for the D2 receptor and pEC50 values of 7.4, 8.4, and 6.8 for human D2, D3, and D4 receptors, respectively. This compound is instrumental in studying Parkinson's disease due to its targeted pharmacological activity and lack of affinity for D1 receptors, making it a valuable tool in neuropharmacological research.
  9. Stable Isotope

    Ropinirole-d3 is a deuterated analog of Ropinirole, primarily targeting D3 and D2 dopamine receptors. As a potent agonist, Ropinirole exhibits a Ki value of 29 nM for the D2 receptor, alongside pEC50 values of 7.4, 8.4, and 6.8 for human D2, D3, and D4 receptors, respectively. This stable isotope is useful in pharmacokinetic studies and can provide insights into the mechanism of action related to dopaminergic therapies, particularly in the context of Parkinson's disease research.
  10. Stable Isotope

    Domperidone-d6 is a deuterium-labeled derivative of Domperidone, a selective antagonist of dopamine D2 receptors. It exerts antiemetic and prokinetic effects by modulating the chemoreceptor trigger zone and enhancing gastrointestinal motility. This stable isotope serves as a valuable tool for research applications, including pharmacokinetic studies and metabolic pathway investigations.
  11. Stable Isotope

    Metopimazine-d6 is a deuterium-labeled derivative of Metopimazine, a phenothiazine compound that functions primarily as a selective antagonist of dopamine D2 receptors. It is characterized by its inability to penetrate the blood-brain barrier, making it effective in inhibiting dopamine activity in peripheral regions and the chemoreceptor trigger zone, thus reducing nausea and vomiting. Metopimazine is commonly utilized in the management of chemotherapy-induced nausea and vomiting, with minimal central nervous system effects owing to its limited brain access. This stable isotope compound is valuable for research applications involving pharmacokinetics and metabolic studies.
  12. Stable Isotope

    Haloperidol-d4 N-Oxide is a deuterium-labeled derivative of Haloperidol, functioning primarily as a stable isotope. This compound serves as a potent antagonist of the dopamine D2 receptor and is extensively utilized in antipsychotic research. Its isotopic labeling facilitates advanced pharmacokinetic studies, enabling researchers to investigate the metabolism and dynamics of Haloperidol in biological systems.
  13. Stable Isotope

    Promazine-d6 hydrochloride is a deuterium-labeled derivative of the antipsychotic agent promazine, which targets the dopamine D2 receptor. This stable isotope compound is utilized in pharmacokinetic studies and isotopic labeling applications. By inhibiting dopaminergic neurotransmission, it plays a critical role in understanding the mechanisms underlying neuropsychiatric disorders and the metabolic pathways of antipsychotic drugs.
  14. Stable Isotope

    Ropinirole-d3 hydrochloride is a deuterium-labeled derivative of Ropinirole hydrochloride, functioning as a potent agonist for D2 and D3 dopamine receptors, with a Ki value of 29 nM for the D2 receptor. It exhibits pEC50 values of 7.4, 8.4, and 6.8 for human D2, D3, and D4 receptors, respectively, while showing no affinity for D1 receptors. This compound is primarily utilized in research related to dopamine receptor signaling and has potential implications for therapies targeting Parkinson's disease.
  15. Stable Isotope

    Raclopride-d5 hydrochloride is a deuterium-labeled derivative of Raclopride, a selective antagonist for dopamine D2 and D3 receptors. It exhibits high affinity, with dissociation constants (Kis) of 1.8 nM for D2 and 3.5 nM for D3 receptors, while demonstrating minimal interaction with D1 and D4 receptors (Kis of 18000 nM and 2400 nM, respectively). This compound is valuable in neuropharmacology research for studying dopamine signaling pathways and receptor mechanisms in various models.
  16. Stable Isotope

    7α,25-Dihydroxycholesterol-d6 is a deuterated form of 7α,25-Dihydroxycholesterol, functioning as a selective agonist and endogenous ligand for the orphan G protein-coupled receptor EBI2 (GPR183). This stable isotope is crucial for studies involving lipid metabolism and immune response, particularly in relation to the modulation of B cell trafficking. Researchers utilize 7α,25-Dihydroxycholesterol-d6 in various biochemical assays to elucidate signaling pathways mediated by EBI2.
  17. Stable Isotope

    Bosentan-d4 is a deuterium-labeled form of Bosentan, which acts as a competitive dual antagonist of endothelin-1 (ET) at both the ETA and ETB receptors, exhibiting Ki values of 4.7 nM and 95 nM in human smooth muscle cells, respectively. This reagent is primarily utilized in pharmacokinetic and metabolic studies, providing insights into the biological processes modulated by endothelin signaling. Its stable isotope labeling enhances the accuracy of quantification in analytical applications and research focused on cardiovascular disease mechanisms.
  18. Stable Isotope

    (Rac)-Ambrisentan-d3 is a deuterated form of (Rac)-Ambrisentan, a selective endothelin receptor antagonist. This stable isotope is utilized in pharmacokinetic studies and metabolic research, allowing for precise tracking of drug metabolism and distribution in biological systems. Its application is essential for understanding the pharmacological properties and efficacy of endothelin receptor-targeted therapies.
  19. Stable Isotope

    Nicorandil-d4 is the deuterium-labeled analog of Nicorandil, a potent activator of potassium channels, specifically targeting vascular nucleoside diphosphate-dependent K+ channels and cardiac ATP-sensitive K+ channels (KATP). This compound exhibits significant vasodilatory and cardioprotective effects, making it relevant for research in angina and ischemic heart diseases. Nicorandil-d4 serves as a valuable stable isotope for metabolism studies and pharmacokinetic investigations in cardiovascular research.
  20. Stable Isotope

    Glipizide-d11 is a deuterium-labeled derivative of Glipizide, a sulfonylurea-class anti-diabetic agent. It demonstrates potent activity in the management of type 2 diabetes mellitus by partially inhibiting ATP-sensitive potassium (KATP) channels in the β cells of the pancreatic islets of Langerhans. This stable isotope form is utilized in pharmacokinetic studies and metabolic research, helping to better elucidate the drug's pharmacodynamics and biological interactions.
  21. Stable Isotope

    Gliclazide-d4 is a deuterated analog of Gliclazide, a recognized inhibitor of ATP-sensitive potassium channels in pancreatic beta cells. It exhibits biological activity as an antidiabetic agent with an IC50 of 184 nM, effectively regulating insulin secretion. Gliclazide-d4 is suitable for pharmacokinetic studies, metabolic research, and tracer studies in glucose homeostasis investigations.
  22. Stable Isotope

    Vernakalant-d6 hydrochloride is a deuterium-labeled analogue of Vernakalant, primarily used as a stable isotope in research applications. This compound facilitates investigations into the pharmacokinetics and metabolic pathways of Vernakalant by enabling the tracking of molecular interactions and dynamics in biological systems. Researchers can utilize Vernakalant-d6 hydrochloride in studies related to cardiac arrhythmias and antiarrhythmic drug mechanisms.
  23. Stable Isotope

    (Rac)-Ropivacaine-d7 is a deuterium-labeled analogue of (Rac)-Ropivacaine, a local anesthetic that primarily acts by blocking voltage-gated sodium channels. This stable isotope is valuable in pharmacokinetic studies and metabolic research, enabling researchers to investigate the drug's distribution, metabolism, and elimination in biological systems. The incorporation of deuterium enhances the sensitivity and specificity of analytical methods such as mass spectrometry.
  24. Stable Isotope

    Amifampridine-d3 (3,4-Diaminopyridine-d3) is a deuterium-labeled analog of Amifampridine, a potent and cell-permeable blocker of voltage-gated potassium (Kv) channels. This compound enhances neurotransmitter release at neuromuscular junctions, making it effective in the reversal of botulinum toxin A (BoNT/A) intoxication. Amifampridine-d3 is also valuable for research into Lambert-Eaton myasthenic syndrome (LEMS), providing insights into neuromuscular transmission and associated pathophysiology.
  25. Stable Isotope

    Dehydroindapamide-d3 is a deuterium-labeled derivative of Dehydroindapamide, targeting cytochrome P450 enzyme CYP3A4. This stable isotope standard is designed for the quantitative assessment of Indapamide turnover rates, demonstrating a turnover rate roughly 10-fold greater than Indoline and showing enhanced affinity for CYP3A4. It is a valuable tool in pharmacokinetic studies and can aid in drug metabolism research.
  26. Stable Isotope

    Acetohexamide-d11 is a deuterium-labeled derivative of Acetohexamide, a first-generation sulfonylurea compound. This reagent primarily targets ATP-sensitive potassium channels in pancreatic β cells, promoting insulin secretion vital for studies on type 2 diabetes. Researchers can utilize Acetohexamide-d11 to trace metabolic pathways and evaluate pharmacokinetics in diabetes research applications.
  27. Stable Isotope

    Mesoridazine-d3 is a deuterium-labeled derivative of Mesoridazine, a phenothiazine antipsychotic that primarily targets human ether-a-go-go related gene (hERG) channels. This compound functions as a rapid open-channel blocker of hERG currents, exhibiting an IC50 value of 550 nM in human embryonic kidney 293 cells. Mesoridazine-d3 is useful in pharmacological studies related to schizophrenia and other psychiatric disorders, facilitating research into the mechanisms underlying these conditions.
  28. Stable Isotope

    Ropivacaine-d7 hydrochloride is a deuterium-labeled derivative of Ropivacaine, primarily functioning as a potent sodium channel blocker. It inhibits sodium ion influx in nerve fibers, leading to reversible blockade of impulse conduction. Additionally, Ropivacaine acts as an inhibitor of the TREK-1 potassium channel, demonstrating an IC50 of 402.7 μM in COS-7 cell membranes. This reagent is valuable for research in neuropathic pain management and the study of ion channel dynamics.
  29. Stable Isotope

    L-Palmitoylcarnitine-d3-1 hydrochloride is a deuterated form of L-Palmitoylcarnitine, a long-chain acylcarnitine known for its role in fatty acid metabolism. This reagent contributes to the understanding of membrane lipid dynamics during ischaemic conditions, where it accumulates in the sarcolemma and disrupts lipid environments. Additionally, L-Palmitoylcarnitine-d3-1 hydrochloride inhibits KATP channel activity through interaction with the Kir6.2 subunit, making it a valuable tool for investigating metabolic pathways and channel function in various research applications.
  30. Stable Isotope

    Indapamide-13C,d3 is a stable isotope-labeled form of the sulphonamide diuretic, Indapamide. This compound primarily acts by lowering blood pressure through the reduction of vascular reactivity and peripheral vascular resistance. Additionally, Indapamide is known to decrease left ventricular hypertrophy, making it useful for cardiovascular research applications, including studies on hypertension and cardiac remodeling.
  31. Stable Isotope

    (rac)-Indapamide-d3 is a stable isotope-labeled derivative of the racemic compound Indapamide. As a sulphonamide diuretic, Indapamide functions primarily by reducing vascular reactivity and peripheral vascular resistance, leading to decreased blood pressure. Additionally, it has been shown to mitigate left ventricular hypertrophy. This isotope-labeled reagent is suitable for pharmacokinetic studies, metabolic analysis, and tracing applications in biological research.
  32. Stable Isotope

    L-Palmitoylcarnitine-d9 is a deuterium-labeled derivative of L-Palmitoylcarnitine, functioning as a stable isotope for biological studies. L-Palmitoylcarnitine plays a critical role in fatty acid metabolism and is known to accumulate in the sarcolemma, where it influences the lipid environment during ischemic conditions. This compound inhibits KATP channel activity by interacting with the Kir6.2 subunit, while not altering single-channel conductance. Its unique properties make it suitable for research in metabolic diseases and cardiac physiology.
  33. Stable Isotope

    Flecainide-d3 is a deuterium-labeled form of Flecainide, a clinically utilized antiarrhythmic agent. Its primary mechanism involves blocking sodium channels while also inhibiting calcium ion release through the cardiac ryanodine receptor (RyR2). This reagent is valuable in research focused on cardiac arrhythmias, particularly in the study of catecholaminergic polymorphic ventricular tachycardia (CPVT) and related cardiac conditions. Its stable isotope labeling facilitates advanced pharmacokinetic and metabolic studies.
  34. Stable Isotope

    Abscisic acid-d6 is a deuterium-labeled derivative of abscisic acid, functioning as a stable isotope. This compound is known for its ability to inhibit the proton pump (H+-ATPase), making it a valuable tool for investigating physiological processes regulated by abscisic acid. Its applications extend to studying plant stress responses, signal transduction pathways, and metabolic regulation in various biological systems.
  35. Stable Isotope

    Esomeprazole-d6 sodium is a deuterium-labeled derivative of Esomeprazole. This compound functions primarily as a proton pump inhibitor, effectively reducing gastric acid secretion by inhibiting the H+, K+-ATPase enzyme in gastric parietal cells. Esomeprazole-d6 sodium is valuable for research applications focused on gastroesophageal reflux disease, enabling the study of metabolic pathways and pharmacokinetics in related therapeutic investigations.
  36. Stable Isotope

    Pantoprazole sulfide-d8 is a deuterated form of Pantoprazole sulfide, acting as a stable isotope analogue. This compound serves as a metabolite of Pantoprazole, a well-known proton-pump inhibitor. Pantoprazole sulfide-d8 is primarily utilized in pharmacokinetic studies to investigate the metabolic pathways and mechanisms of action of proton-pump inhibitors in various biological systems.
  37. Stable Isotope

    Lansoprazole sulfone-d4 is a deuterium-labeled derivative of Lansoprazole sulfone, which functions as a selective inhibitor of H+, K+-ATPase. This compound is significant in the study of various gastrointestinal disorders, including duodenal ulcer, gastric ulcer, gastroesophageal reflux disease, and Zollinger-Ellison syndrome. As a stable isotope, Lansoprazole sulfone-d4 is valuable for metabolic studies and tracing applications in pharmacokinetic research.
  38. Stable Isotope

    Lansoprazole sulfone-13C6 is a stable isotope-labeled form of Lansoprazole sulfone, a known inhibitor of the H+, K+-ATPase enzyme. This compound serves as a valuable metabolic marker for studying the pharmacokinetics and biological effects of Lansoprazole in various conditions, including duodenal and gastric ulcers, gastroesophageal reflux disease, and Zollinger-Ellison syndrome. Its stable isotope labeling allows for precise tracking in metabolic studies and applications in drug formulation research.
  39. Stable Isotope

    Empagliflozin-d4 is a deuterium-labeled derivative of Empagliflozin, a selective sodium-glucose cotransporter-2 (SGLT-2) inhibitor. With an IC50 of 3.1 nM for human SGLT-2, this stable isotope is utilized primarily in pharmacokinetic studies and metabolic research. Its labeling facilitates the investigation of drug metabolism and the tracking of pharmacological effects in biological systems.
  40. Stable Isotope

    Dapagliflozin-d5 is a deuterated form of Dapagliflozin, a selective inhibitor of the sodium-glucose cotransporter 2 (SGLT2). This stable isotope is utilized in metabolic studies and pharmacokinetic research to trace the absorption and distribution of Dapagliflozin in biological systems. Its application in advanced research provides insights into the drug's mechanism and efficacy in managing diabetes.
  41. Stable Isotope

    Canagliflozin-d4 is a deuterium-labeled derivative of Canagliflozin, a selective inhibitor of the sodium-glucose cotransporter 2 (SGLT2). This stable isotope is primarily utilized in pharmacokinetic studies and metabolic research to trace and quantify the pharmacological fate of Canagliflozin in biological systems. The presence of deuterium allows for enhanced detection and analysis, facilitating investigations into glucose homeostasis and associated therapeutic applications in diabetes management.
  42. Stable Isotope

    Empagliflozin-d8 is a deuterium-labeled derivative of Empagliflozin, a selective sodium-glucose cotransporter-2 (SGLT-2) inhibitor. With an IC50 of 3.1 nM for human SGLT-2, this compound exhibits significant biological activity in glucose regulation and is utilized in diabetes research. Its stable isotope labeling enables enhanced analytical sensitivity and specificity in pharmacokinetic studies and metabolic profiling.
  43. Stable Isotope

    Pragliflozin-13C6 is a stable isotope-labeled form of Ipragliflozin, a selective sodium-glucose cotransporter 2 (SGLT2) inhibitor. This compound demonstrates inhibitory activity with IC50 values of 7.38 nM for human SGLT2 and significantly higher values for SGLT1, making it a potent antidiabetic agent. Pragliflozin-13C6 is primarily utilized in pharmacokinetic studies and metabolic experiments to trace the pathways and mechanisms of Ipragliflozin in biological systems.
  44. Stable Isotope

    Ertugliflozin-d5 is a deuterium-labeled form of Ertugliflozin, a selective and potent inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2). With an IC50 of 0.877 nM against human SGLT2, it effectively reduces glucose reabsorption in the kidneys, making it relevant in research aimed at understanding type 2 diabetes mellitus treatment mechanisms. This stable isotope-labeled reagent is valuable for pharmacokinetic studies and metabolic tracing in biological systems.
  45. Stable Isotope

    Remogliflozin etabonate-d7 is the deuterium-labeled variant of Remogliflozin etabonate, a selective sodium glucose cotransporter 2 (SGLT2) inhibitor. With Ki values of 1.95 μM for hSGLT2 and 2.14 μM for rSGLT2, it demonstrates notable inhibition of glucose reabsorption in renal tissues. Remogliflozin etabonate is metabolized to its active form within the body, contributing to its antidiabetic effects observed in rodent models. This stable isotope-labeled compound is valuable for pharmacokinetic studies and metabolic research involving SGLT2 inhibition.
  46. Stable Isotope

    Dapagliflozin-d4 is a stable isotope-labeled form of Dapagliflozin, an SGLT2 inhibitor that effectively targets sodium/glucose cotransport in the treatment of diabetes mellitus (DM). This compound promotes glucose excretion via urine, contributing to improved glycemic control. Additionally, Dapagliflozin has been shown to induce HIF1 expression and mitigate renal ischemia-reperfusion injury, making it a valuable tool for research in diabetic complications and renal protection mechanisms.
  47. Stable Isotope

    Triamterene-d5 is a deuterium-labeled derivative of Triamterene, functioning primarily as a stable isotope for analytical purposes. It acts as a blocker of the epithelial Na+ channel (ENaC) in a voltage-dependent manner, serving as a mild diuretic. Additionally, Triamterene demonstrates inhibitory activity at the TGR5 receptor, making it valuable for research into renal function and metabolic processes.
  48. Stable Isotope

    Benzocaine-(ethyl-d5) is a deuterated form of benzocaine, targeting voltage-gated Na+ channels. This stable isotope serves as a valuable tool in pharmacokinetic studies and mechanistic research, enabling precise tracking of benzocaine metabolism and dynamics in biological systems. Its inhibitory concentration (IC50) is reported at 0.8 mM when assessed at a membrane potential of +30 mV, making it relevant for investigations into local anesthetic mechanisms and interactions.
  49. Stable Isotope

    Butibufen-d5 is a deuterated analog of Butibufen, a non-steroidal compound known for its analgesic and antipyretic effects. This stable isotope can be utilized in pharmacokinetic studies and metabolic research to trace the compound's behavior in biological systems. It is particularly valuable in inflammation research, providing insights into the mechanisms of action and efficacy of non-steroidal anti-inflammatory drugs.
  50. WNK Kinase Inhibitor

    WNK-IN-11-d3 is a selective and potent inhibitor of WNK kinases, designed for oral administration. This compound plays a crucial role in modulating cardiovascular homeostasis and serves as a valuable tool in studying cardiovascular signaling pathways and related conditions. Its unique mechanism of action makes it a significant reagent for research applications targeting WNK kinase-related processes.

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