Isotope-Labeled Compounds

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  1. Stable Isotope

    Valproic acid β-D-glucuronide-d6 is a stable isotope-labeled derivative of Valproic acid β-D-glucuronide, which serves as a key urinary metabolite of Valproic acid. This compound is primarily utilized in pharmacokinetic studies and metabolic research, enabling precise tracking and quantification of Valproic acid metabolism in biological samples. Its deuterated form enhances sensitivity and accuracy in analytical applications, making it valuable for studies in drug metabolism and pharmacodynamics.
  2. Stable Isotope

    4-Phenylbutyric acid-d5 is a deuterium-labeled derivative of 4-Phenylbutyric acid, a known inhibitor of histone deacetylases (HDACs) and a modulator of endoplasmic reticulum (ER) stress. This compound demonstrates significant biological activity in reducing ER stress and has potential applications in cancer research and studies related to infectious diseases. Its stable isotope labeling makes it suitable for advanced biochemical analyses and metabolic tracing in various experimental settings.
  3. Stable Isotope

    Valproic acid-d4-1 is a deuterated form of Valproic acid, which functions as a histone deacetylase (HDAC) inhibitor. It exhibits biological activity by inhibiting HDAC1 and promoting the proteasomal degradation of HDAC2, contributing to its role in cancer research through the activation of Notch1 signaling and inhibition of proliferation in small cell lung cancer cells. This reagent is valuable for studies in neuropharmacology and cancer biology, particularly in assessing the effects of deuterated metabolites on therapeutic outcomes and drug metabolism.
  4. Stable Isotope

    4-Phenylbutyric acid-d2 is the deuterated form of 4-Phenylbutyric acid, a known inhibitor of histone deacetylases (HDAC) and a mitigator of endoplasmic reticulum (ER) stress. This compound is widely utilized in cancer research and studies of infectious diseases due to its ability to modulate cellular stress responses and influence gene expression. The stable isotope labeling allows for advanced analytical techniques in metabolic studies and pathway elucidation.
  5. Stable Isotope

    Valproic acid-d7 sodium is a deuterium-labeled form of valproic acid sodium salt, an established histone deacetylase (HDAC) inhibitor with an IC50 ranging from 0.5 to 2 mM. This compound selectively inhibits HDAC1 (IC50 of 400 μM) and promotes the proteasomal degradation of HDAC2. In addition to its role in modulating HDAC activity, Valproic acid-d7 sodium activates Notch1 signaling and demonstrates antiproliferative effects in small cell lung cancer (SCLC) cells. It is commonly utilized in research related to epilepsy, bipolar disorder, and migraine prevention.
  6. Stable Isotope

    Melitracen-d6 hydrochloride is a deuterium-labeled form of Melitracen hydrochloride, a biphasic antidepressant and anxiolytic. It primarily acts by inhibiting the reuptake of norepinephrine and serotonin at the presynaptic membrane, leading to increased levels of monoamine neurotransmitters in the synaptic cleft. This stable isotope form is useful in pharmacokinetic studies and metabolic tracing in biochemical research.
  7. Stable Isotope

    Zimeldine-d6 is a deuterium-labeled analog of Zimeldine, primarily used as a stable isotope in chemical research. This compound allows for enhanced tracking and analysis in metabolic studies and pharmacokinetic investigations. Its incorporation into experimental designs facilitates detailed studies of Zimeldine's biological activity and interactions, aiding in the understanding of its pharmacological properties.
  8. Stable Isotope

    Eletriptan-d3 is a deuterated form of Eletriptan hydrobromide, acting as a selective agonist for the 5-HT1B and 5-HT1D receptors, with Ki values of 0.92 nM and 3.14 nM, respectively. This stable isotope is valuable for pharmacokinetic studies, allowing researchers to investigate the distribution and metabolism of Eletriptan in biological systems. Its use in isotopic labeling enhances the sensitivity and specificity of analytical techniques in neurological research.
  9. Stable Isotope

    Setiptiline-d3 is a deuterium-labeled analog of Setiptiline, a tetracyclic antidepressant functioning primarily as a noradrenergic and specific serotonergic antidepressant. Its mechanism involves norepinephrine reuptake inhibition and antagonism of α2-adrenergic and various serotonin receptors, including 5-HT2A, 5-HT2C, and 5-HT3 subtypes, in addition to H1 receptor inverse agonism. This stable isotope variant is valuable for tracing studies in pharmacokinetics and elucidating the pharmacodynamics of Setiptiline in clinical research.
  10. Stable Isotope

    Cisapride-d6 is a deuterium-labeled analogue of Cisapride, primarily functioning as a stable isotope for analytical applications. As a 5-HT4 receptor agonist with an EC50 of 140 nM, Cisapride enhances gastrointestinal motility, making it a valuable gastroprokinetic agent. Additionally, it acts as a hERG blocker with an IC50 value of 9.4 nM, facilitating research into cardiac safety profiles. This reagent is ideal for studying pharmacokinetics and metabolic pathways in preclinical models.
  11. Stable Isotope

    Lumateperone-d4 is a deuterium-labeled analog of Lumateperone, primarily targeting the 5-HT2A receptor as an antagonist (Ki = 0.54 nM). It exhibits dual action as a partial agonist at presynaptic D2 receptors and an antagonist at postsynaptic D2 receptors (Ki = 32 nM), along with modulation of dopamine D1 receptors. This compound is valuable for investigating schizophrenia, bipolar depression, and has demonstrated anticancer properties, making it a versatile tool in chemical research.
  12. Stable Isotope

    Pindolol-d7 is a deuterated form of Pindolol, primarily targeting the 5-HT 1A (Ki=33 nM) and 5-HT 1B receptors, as well as β1/β2-adrenergic receptors. This stable isotope is utilized in research to investigate the pharmacokinetics and metabolic pathways of Pindolol. The compound demonstrates significant anti-anxiety and antidepressant activities, making it valuable for studies related to psychiatric disorders and neuropharmacology.
  13. Stable Isotope

    Dehydroaripiprazole-d8 is a deuterated form of Dehydroaripiprazole, a key active metabolite of the antipsychotic Aripiprazole. This stable isotope serves as a valuable analytical tool in pharmacokinetic studies and metabolic pathway investigations. Dehydroaripiprazole exhibits comparable antipsychotic activity to its parent compound, allowing researchers to explore its efficacy and safety profiles in various clinical settings. It is particularly useful for studies involving isotopic labeling techniques and drug metabolism enzyme interactions.
  14. Stable Isotope

    Trimipramine-d3 maleate is a deuterium-labeled analog of Trimipramine maleate, functioning primarily as a selective antagonist of 5-HT receptors. It exhibits pKis of 6.39 for 5-HT1C, 8.10 for 5-HT2, and 4.66 for 5-HT1A, highlighting its specificity towards serotonin signaling pathways. This stable isotope is valuable for pharmacokinetic studies and metabolic tracing in biological research, providing insights into the pharmacodynamics of serotonergic modulation.
  15. Stable Isotope

    Loxapine-d8 hydrochloride is a deuterated derivative of Loxapine, primarily acting as a D2 and D4 dopamine receptor inhibitor. This stable isotope is utilized in research to study pharmacokinetics and metabolic pathways of Loxapine. Its serotonergic receptor antagonism further facilitates investigations into the neuropharmacological effects associated with dibenzoxazepine anti-psychotic agents.
  16. Stable Isotope

    Granisetron-d3 is a deuterium-labeled derivative of Granisetron, which acts as a selective antagonist of the serotonin 5-HT3 receptor. This compound is primarily utilized in research related to antiemetic effects and mechanisms of nausea and vomiting, particularly in the context of chemotherapy treatments. Its stable isotope labeling enables advanced analytical studies and metabolism investigations in preclinical settings.
  17. Stable Isotope

    Bopindolol-d9 is the deuterium-labeled form of Bopindolol, a non-selective antagonist of β-adrenoceptors (ARs) with partial agonist activity. This compound exhibits low affinity for the β3-AR subtype and possesses intrinsic sympathomimetic properties, alongside membrane stabilizing actions. Bopindolol-d9 is useful for research on essential and renovascular hypertension, as well as for studying renin secretion and interactions with 5-HT receptors.
  18. Stable Isotope

    Quetiapine-d8 fumarate is a deuterated derivative of Quetiapine, primarily functioning as a stable isotope for enhanced analytical studies. This compound acts as a 5-HT receptor agonist, exhibiting a pEC50 of 4.77 for the human 5-HT1A receptor, while also serving as a dopamine receptor antagonist with a pIC50 of 6.33 for the human D2 receptor. Quetiapine-d8 fumarate demonstrates moderate to high affinity for multiple receptors, including human D2, 5-HT1A, 5-HT2A, and 5-HT2C, with respective pKis of 7.25, 5.74, 7.54, and 5.55, making it valuable for research into antidepressant and anxiolytic pharmacology.
  19. Stable Isotope

    Blonanserin-d5 is a deuterated analog of Blonanserin, serving as a stable isotope for research applications. As a dopamine D2 and 5-HT2 receptor antagonist, Blonanserin is classified as an atypical antipsychotic. This reagent is useful for pharmacokinetic studies and can facilitate investigations into the pharmacodynamics and metabolism of antipsychotic compounds.
  20. Stable Isotope

    Melperone-d4 hydrochloride is a deuterium-labeled derivative of Melperone hydrochloride, a butyrophenone with atypical antipsychotic properties. It acts as a multireceptor antagonist, exhibiting binding affinities (Kd values) of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Additionally, Melperone-d4 displays weak interactions with several other receptors and inhibits CYP2D6. This reagent is particularly valuable for investigating schizophrenia and managing agitation in geriatric populations.
  21. Stable Isotope

    GW-117 is a stable isotope characterized as a 5-HT2C receptor antagonist and a melatonin (MT1/MT2) receptor agonist. This compound exhibits significant antidepressant-like and anxiolytic-like effects, making it valuable for research in mood disorders and anxiety. It serves as a crucial tool for studies investigating the interplay between serotonin and melatonergic systems in neuropharmacology.
  22. Stable Isotope

    Clozapine-d3 is a deuterium-labeled derivative of Clozapine, primarily targeting neuroreceptors involved in psychiatric disorders. This compound exhibits high affinity as a dopamine D2 receptor antagonist with a Ki of 75 nM, while also inhibiting the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively. Additionally, Clozapine-d3 acts as a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM), making it valuable for investigations into schizophrenia and related neurochemical pathways.
  23. Stable Isotope

    Rizatriptan-d6 benzoate is a deuterium-labeled derivative of Rizatriptan benzoate, which acts as an agonist for the serotonin receptors 5-HT1B and 5-HT1D. This compound exhibits peripheral vasoconstrictive properties and effectively crosses the blood-brain barrier, thereby inhibiting pain neurotransmission within the central nervous system. It is commonly utilized in research applications focused on migraine pathophysiology, pharmacokinetics, and receptor signaling studies.
  24. Stable Isotope

    Urapidil-d4 is a deuterium-labeled derivative of Urapidil, which functions primarily as an α1 adrenoreceptor antagonist and a 5-HT1A receptor agonist. This stable isotope-labeled compound is valuable for tracing studies and in-depth biochemical research, allowing for precise pharmacokinetic assessments and potential insights into receptor interactions and mechanisms of action. Its unique isotopic labeling enhances the ability to study the metabolism and distribution of Urapidil in various biological contexts.
  25. Stable Isotope

    Metoclopramide-d3 is a deuterium-labeled derivative of Metoclopramide. This compound functions as a potent antagonist of the 5-HT3 and dopamine D2 receptors, exhibiting IC50 values of 308 nM and 483 nM, respectively. Metoclopramide-d3 is utilized in research focusing on nausea, vomiting, gastroesophageal reflux disease, and gastroparesis, providing a valuable tool for studying the pharmacokinetics and dynamics of this important therapeutic agent.
  26. Stable Isotope

    Cyclobenzaprine-d6 hydrochloride is a deuterium-labeled analogue of Cyclobenzaprine, serving as a stable isotope compound. This reagent is primarily utilized in pharmacokinetic studies and mass spectrometry applications for the quantification of Cyclobenzaprine and its metabolites. Its unique isotopic labeling allows for enhanced sensitivity and specificity in analytical assays, facilitating research in drug metabolism and pharmacodynamics.
  27. Stable Isotope

    Zolmitriptan-d6 is a deuterium-labeled derivative of Zolmitriptan, a selective partial agonist of the 5-HT1B and 5-HT1D receptors, exhibiting inhibitory constants (Kis) of 5.01 nM, 0.63 nM, and 63.09 nM for the 5-HT1B, 5-HT1D, and 5-HT1F receptors, respectively. This stable isotope is primarily utilized in analytical research for understanding the pharmacokinetics and metabolism of Zolmitriptan in migraine studies, facilitating more accurate mechanism-of-action investigations.
  28. Isotope-Labeled Compounds

    Cyclobenzaprine-d3-1 hydrochloride is a deuterium-labeled analog of Cyclobenzaprine hydrochloride, functioning primarily as a 5-HT2 receptor antagonist. This compound exhibits significant skeletal muscle relaxant properties, effectively alleviating muscle spasms and associated pain. Furthermore, it possesses antiprotozoal and antiparasitic activities, making it a valuable tool for research in acute musculoskeletal disorders as well as infectious diseases. Its isotope-labeled nature enables advanced studies in pharmacokinetics and mechanism of action.
  29. Stable Isotope

    Deulumateperone is a deuterated derivative of Lumateperone, serving as a stable isotope for research applications. Lumateperone acts as a selective antagonist of the 5-HT2A receptor (Ki = 0.54 nM) and modulates dopamine receptors, demonstrating significant antipsychotic and antineoplastic properties. This reagent is valuable for studies involving receptor interactions, pharmacokinetics, and metabolic profiling in various biological systems.
  30. Stable Isotope

    Paliperidone palmitate-d4 is a deuterium-labeled derivative of paliperidone palmitate, serving as a stable isotope for research applications. This compound functions as a competitive antagonist of dopamine D2 and 5-hydroxytryptamine 2A (5-HT2A) receptors, effectively modulating neurotransmitter systems and demonstrating antipsychotic activity. Its ability to cross the blood-brain barrier makes it particularly valuable for studies focused on schizophrenia and related psychiatric disorders.
  31. Stable Isotope

    Cisapride-13C,d3 is a stable isotope-labeled form of Cisapride, which primarily acts as a 5-HT4 receptor agonist, exhibiting an EC50 of 140 nM. Additionally, Cisapride functions as a hERG channel inhibitor with an IC50 of 9.4 nM. This compound serves as a gastroprokinetic agent, promoting gastrointestinal motility, making it valuable for research involving gastrointestinal disorders and pharmacokinetic studies.
  32. Stable Isotope

    Quetiapine-d4-1 fumarate is a deuterated analogue of Quetiapine, specifically designed to enhance analytical precision in research applications. As a serotonin (5-HT) receptor agonist, it exhibits a pEC50 of 4.77 at the human 5-HT1A receptor and acts as a dopamine receptor antagonist with a pIC50 of 6.33 for the human D2 receptor. Quetiapine-d4-1 fumarate demonstrates moderate to high affinity for several key receptors, including D2, 5-HT1A, 5-HT2A, and 5-HT2C, making it suitable for studies in neuropharmacology, particularly in exploring antidepressant and anxiolytic effects.
  33. Stable Isotope

    Ondansetron-13C,d3 is a stable isotope-labeled variant of Ondansetron, a selective 5-HT3 receptor antagonist with an IC50 of 103 pM. This compound inhibits nausea and vomiting by blocking 5-HT receptors in both peripheral and central nervous systems. It is particularly valuable in research applications involving the effects of chemotherapy and radiotherapy on antiemetic responses. Used in pharmacokinetic studies and metabolic research, Ondansetron-13C,d3 aids in understanding the drug's behavior and efficacy in clinical settings.
  34. Stable Isotope

    Sarpogrelate-d3 hydrochloride is a deuterium-labeled form of Sarpogrelate hydrochloride, serving as a selective antagonist for the 5-HT2 receptor family. With pKis of 8.52, 6.57, and 7.43 for the 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively, it demonstrates notable selectivity over 5-HT1, 5-HT3, 5-HT4, and various adrenergic and histamine receptors. This reagent is valuable for studying vascular diseases related to thrombosis, enabling researchers to investigate the pharmacodynamics and metabolism of Sarpogrelate in biological systems.
  35. Stable Isotope

    Azasetron Hydrochloride-13C,d3 is a deuterium and carbon-13 isotope-labeled form of Azasetron, a potent 5-HT3 receptor antagonist. This antiemetic agent is widely utilized in the research of postoperative nausea and vomiting, as well as nausea induced by chemotherapy. Importantly, Azasetron maintains neutrophil chemotaxis and phagocytosis without reacting with superoxide or hydrogen peroxide in cell-free systems, making it suitable for various biological studies.
  36. Stable Isotope

    Eletriptan-d5 is a deuterium-labeled analog of Eletriptan, a highly selective and orally active agonist for the serotonin 5-HT1B and 5-HT1D receptors, exhibiting pKi values of 8.0 and 8.9, respectively. This compound demonstrates inhibitory effects on neurogenic inflammation markers in preclinical models, particularly in rats. Eletriptan-d5 is valuable for research applications focused on migraine pathophysiology and the pharmacological profiling of serotonin receptor interactions.
  37. Stable Isotope

    Cyclobenzaprine-d6 is a deuterated analogue of Cyclobenzaprine, functioning primarily as a 5-HT2 receptor antagonist. This compound exhibits significant central nervous system activity, leading to skeletal muscle relaxation, alleviation of muscle spasms, and pain reduction. Additionally, Cyclobenzaprine demonstrates antiparasitic properties, making it a valuable tool for research in acute skeletal muscle disorders and the investigation of infectious diseases.
  38. Stable Isotope

    Arotinolol-d5 hydrochloride is a deuterated analog of Arotinolol, a nonselective α/β-adrenergic receptor blocker with vasodilatory properties. This compound exhibits notable activity in inhibiting the binding of the radioligand 125I-ICYP to 5HT1B serotonergic receptor sites. Arotinolol serves as an effective antihypertensive agent and is utilized in research related to various cardiovascular and non-cardiovascular diseases.
  39. Stable Isotope

    Cyclobenzaprine-13C,d3 hydrochloride is a stable isotope-labeled form of Cyclobenzaprine, incorporating both 13C and deuterium isotopes. This reagent is primarily utilized in isotopic labeling experiments, aiding in the study of pharmacokinetics and metabolic pathways. Its unique isotopic composition allows for precise tracking and analysis in biochemical research applications, making it a valuable tool for scientists investigating muscle relaxant dynamics and therapeutic efficacy.
  40. Stable Isotope

    Flibanserin-d4-1 is a deuterated form of Flibanserin, a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of the 5-HT2A receptor (Ki=49 nM). Additionally, Flibanserin demonstrates binding affinity for dopamine D4 receptors (4-24 nM) while exhibiting minimal interactions with various other neurotransmitter receptors and ion channels. This compound is primarily utilized in research applications focused on hypoactive sexual desire disorder (HSDD) and the underlying mechanisms of serotonergic and dopaminergic signaling.
  41. Stable Isotope

    Lurasidone-d8 is a deuterium-labeled derivative of Lurasidone, which acts as an antagonist of dopamine D2 and 5-HT7 receptors, exhibiting IC50 values of 1.68 nM and 0.495 nM, respectively. Additionally, Lurasidone functions as a partial agonist at the 5-HT1A receptor with an IC50 of 6.75 nM. This stable isotope is utilized in biological research for tracing studies, pharmacokinetic profiling, and investigating receptor interactions.
  42. Stable Isotope

    Palonosetron-d3 hydrochloride is a deuterium-labeled derivative of Palonosetron hydrochloride, functioning primarily as a 5-HT3 receptor antagonist. It is widely utilized in research to investigate mechanisms of chemotherapy-induced nausea and vomiting and is known for its ability to prevent both acute and delayed episodes. Additionally, Palonosetron hydrochloride demonstrates moderate activity against flavivirus and potent efficacy against Zika virus in mammalian cells, contributing to its relevance in virology studies. Its potential antidepressant properties also make it a compound of interest in neuropharmacology research.
  43. Stable Isotope

    Ondansetron-d6 hydrochloride is a deuterated form of Ondansetron hydrochloride, acting as a selective antagonist of the serotonin 5-HT3 receptor. This stable isotope is primarily utilized in pharmacokinetic studies and metabolism research, offering insights into the pharmacodynamics and efficacy of Ondansetron in managing nausea and vomiting, particularly in chemotherapy settings. The incorporation of deuterium enables enhanced tracking of the compound in biological systems.
  44. Stable Isotope

    Loxapine-d8 is a stable isotope-labeled analog of Loxapine that incorporates deuterium atoms in its structure. This compound is valuable for metabolic studies and pharmacokinetic research, allowing for precise tracking of drug behavior in biological systems. Loxapine-d8 is particularly useful in studies involving neuroleptics and their effects on neurotransmitter systems, providing insights into psychiatric treatments.
  45. Stable Isotope

    Vortioxetine-d3 is a stable isotope labeled derivative of Vortioxetine, which primarily acts as an antagonist of the 5-HT3A and 5-HT7 receptors, exhibiting high affinity with Ki values of 3.7 nM and 19 nM, respectively. Additionally, it serves as a potent inhibitor of the serotonin transporter (SERT) with a Ki of 1.6 nM, and functions as a 5-HT1A agonist and a partial agonist at the 5-HT1B receptor, showing Ki values of 15 nM and 33 nM. This compound is valuable for pharmacokinetic studies and research related to serotonin modulation in various neurological and psychiatric disorders.
  46. Stable Isotope

    Vortioxetine-d8 is a deuterated analog of Vortioxetine, acting primarily as an antagonist of the 5-HT3A and 5-HT7 receptors while inhibiting the 5-hydroxytryptamine transporter (SERT). This stable isotope marker is crucial for pharmacokinetic studies and metabolic profiling of Vortioxetine. Additionally, it functions as a 5-HT1A agonist and partial 5-HT1B agonist, facilitating research into serotonin receptor interactions and their implications in mood disorders.
  47. Stable Isotope

    Tandospirone-d8 is a deuterated derivative of Tandospirone, a selective partial agonist of the 5-HT1A receptor with a Ki of 27 nM. This compound exhibits significant anxiolytic and antidepressant effects, making it valuable for studying central nervous system disorders. Tandospirone-d8 serves as a stable isotope for research into the pharmacokinetics and mechanisms of action associated with serotonergic modulation in neurological studies.
  48. Stable Isotope

    Ondansetron-d3 is a deuterium-labeled analog of Ondansetron, a highly selective antagonist of the 5-HT3 receptor with an IC50 value of 103 pM. It effectively antagonizes serotonin receptors in both peripheral and central nervous systems, providing significant antiemetic activity. Ondansetron-d3 is utilized in pharmacokinetic studies to trace the metabolic pathways of Ondansetron and to explore its efficacy in preventing nausea and vomiting associated with chemotherapy and radiotherapy.
  49. Stable Isotope

    Cariprazine-d8 is a deuterated form of Cariprazine, a novel antipsychotic agent primarily targeting dopamine D3 and D2 receptors with high affinities of Ki = 0.085 nM and Ki = 0.49 nM, respectively. It also shows moderate affinity for the serotonin receptor 5-HT1A (Ki = 2.6 nM). This stable isotope-labeled compound enables enhanced pharmacokinetic studies and metabolic profiling in research applications, contributing valuable insights into therapeutic mechanisms and drug interactions.
  50. Stable Isotope

    (Rac)-Rotigotine-d3 hydrochloride is a deuterium-labeled analog of (Rac)-Rotigotine, primarily acting as a full agonist at dopamine receptors. It also serves as a partial agonist of the 5-HT1A receptor and acts as an antagonist at the α2B-adrenergic receptor, showcasing Ki values of 0.71 nM, 4-15 nM, and 83 nM for the respective targets. This stable isotope is vital for pharmacokinetic studies, isotope labeling experiments, and research related to neuropharmacology.

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