Isotope-Labeled Compounds

Zafirlukast-d7 is a deuterated derivative of Zafirlukast, a selective antagonist of leukotriene D4 (LTD4) receptors. This stable isotope compound is utilized in biological research to trace and quantify Zafirlukast’s pharmacokinetics and metabolic processes in various systems. Its applications extend to studying therapeutic mechanisms in asthma, inflammation, and other related pathological conditions.

Zafirlukast-d6 is a deuterated labeled form of Zafirlukast, a potent orally active antagonist of the leukotriene D4 (LTD4) receptor. This compound exhibits significant anti-asthmatic, anti-inflammatory, and anti-bacterial properties, making it valuable in respiratory disease research. Zafirlukast-d6 is utilized as a stable isotope for advanced analytical studies, enabling the investigation of metabolic pathways and pharmacokinetics of leukotriene receptor antagonists in biological systems.

Sphingosine-1-phosphate-d7 is a deuterium-labeled analog of Sphingosine-1-phosphate (S1P), a well-established agonist for S1P1-5 receptors and a ligand for GPR3, GPR6, and GPR12. As a key intracellular second messenger, S1P plays a crucial role in mobilizing Ca2+ and mediating various physiological responses. This stable isotope is valuable for studying lipid signaling pathways, receptor interactions, and the metabolic fate of S1P in biochemical assays.

Sphingosylphosphorylcholine-d7 is a deuterium-labeled analog of Sphingosylphosphorylcholine, used as a stable isotope for analytical studies. This reagent is valuable for research applications involving lipid signaling and sphingolipid metabolism. Its stability and isotopic labeling facilitate advanced quantification and tracking of sphingolipid pathways in cellular processes.

Siponimod-d11 is a deuterium-labeled derivative of Siponimod, a selective modulator of sphingosine-1-phosphate (S1P) receptors. This compound exhibits preferential binding to the S1P1 and S1P5 receptors with EC50 values of 0.4 and 0.98 nM, respectively, while showing significantly lower affinity for S1P2, S1P3, and S1P4. Siponimod-d11 is a valuable tool in the research of multiple sclerosis, aiding in the understanding of S1P receptor signaling and its therapeutic implications.

2-Acetyl-4-tetrahydroxybutyl imidazole-13C6 is a stable isotope-labeled version of 2-Acetyl-4-tetrahydroxybutyl imidazole, serving as a potent inhibitor of sphingosine-1-phosphate (S1P) lyase in vivo. This compound is particularly useful for metabolic studies and tracing experiments in biological research. Researchers can utilize this isotope-labeled reagent to investigate the dynamics of sphingolipid metabolism and explore the roles of S1P in various physiological and pathological processes.

Fingolimod phosphate-d4 is a deuterium-labeled form of FTY720 phosphate, serving as a stable isotope label. This compound is utilized in pharmacokinetic studies and metabolic research to trace the biochemical pathways of Fingolimod, a sphingosine-1-phosphate receptor modulator. Its isotopic labeling enables precise measurement and analysis of drug metabolism and distribution in biological systems.

(Rac)-Atropine-d3 is a deuterium-labeled analog of atropine, serving as a stable isotope reagent. It primarily targets the muscarinic acetylcholine receptors, influencing various physiological processes. This compound is valuable for studies related to pharmacokinetics and metabolic labeling, enabling precise tracing and quantification in biological systems.

Tiotropium-d6 bromide is a deuterium-labeled analogue of Tiotropium, primarily targeting muscarinic acetylcholine receptors (mAChR). As a potent mAChR antagonist, it effectively inhibits the binding of acetylcholine, preventing the activation of ligand-gated ion channels. This reagent is valuable for studies involving receptor binding assays, pharmacokinetics, and metabolic pathway analysis.

Propantheline-d3 bromide is a deuterium-labeled version of Propantheline bromide, an antimuscarinic agent that primarily targets muscarinic acetylcholine receptors. It exhibits key biological activities in the inhibition of involuntary muscle contractions, making it effective for managing conditions such as hyperhidrosis, gastrointestinal cramps, bladder spasms, and enuresis. This stable isotope is useful in pharmacokinetic studies and tracer applications in research.

Xanomeline-d3 is a deuterated form of Xanomeline that selectively targets muscarinic type 1 and type 4 (M1/M4) receptors. As an effective agonist, it enhances neuronal excitability, making it a valuable tool in the study of neurological disorders, including schizophrenia. This stable isotope can be utilized in metabolic and pharmacokinetic research applications to trace and quantify Xanomeline metabolism in biological systems.

Tropicamide-d3 is a deuterium-labeled derivative of Tropicamide, which functions as a selective antagonist of the M4 muscarinic acetylcholine receptor. This compound is primarily utilized for its ability to induce short-acting mydriasis and cycloplegia when administered as eye drops. It serves as a valuable tool in neurological and pharmacological research, particularly in studies investigating cholinergic signaling and receptor pharmacodynamics.

Oxybutynin-d11 chloride is the deuterated form of Oxybutynin chloride, an anticholinergic agent primarily targeting vascular Kv channels. This compound exhibits concentration-dependent inhibition, with an IC50 of 11.51 μM. Oxybutynin-d11 chloride is useful for studies in pharmacokinetics, metabolic profiling, and isotopic tracing in chemical research.

(Rac)-5-Hydroxymethyl Tolterodine-d14 is a deuterium-labeled derivative of (Rac)-5-Hydroxymethyl Tolterodine, a potent muscarinic acetylcholine receptor (mAChR) antagonist. It exhibits high affinity with Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively. This stable isotope is instrumental in studies related to overactive bladder syndrome and facilitates pharmacokinetic research by enabling sensitive detection and quantification in biological samples.

Tiotropium-d3 bromide is a deuterium-labeled variant of Tiotropium bromide, a selective antagonist of muscarinic acetylcholine receptors (mAChRs). By inhibiting acetylcholine binding, it prevents the opening of ligand-gated ion channels, leading to bronchial dilation. This compound is primarily used in pharmacological studies related to respiratory disorders and can be utilized in isotopic labeling experiments to investigate drug metabolism and pharmacokinetics.

Darifenacin-d4 is a deuterium-labeled derivative of Darifenacin, which acts as a selective antagonist for the M3 muscarinic receptor, exhibiting a pKi value of 8.9. This stable isotope compound is valuable for pharmacokinetic studies and metabolic research, allowing for precise tracking of the parent compound and its metabolites in biological systems. Its use in isotope labeling enhances analytical techniques such as mass spectrometry in studying receptor interactions and drug metabolism.

Pirenzepine-d8 dihydrochloride is a deuterium-labeled derivative of Pirenzepine, a selective antagonist of the M1 muscarinic acetylcholine receptor (mAChR). This compound exhibits significant biological activity by inhibiting gastric acid secretion and alleviating muscle spasms, making it valuable for research in peptic ulcers. Additionally, Pirenzepine-d8 demonstrates anti-proliferative effects in cancer cell lines, contributing to its use in cancer research applications.

(Rac)-Tolterodine-d5 is a deuterium-labeled analogue of (rac)-Tolterodine, a muscarinic receptor antagonist. This stable isotope-labeled compound is primarily used in pharmacokinetic studies, allowing for the tracking of drug metabolism and bioavailability in biological systems. Its deuterium label enhances molecular stability, making it an essential tool in drug development and metabolic research.

Pilocarpine-d3 hydrochloride is a deuterium-labeled derivative of Pilocarpine hydrochloride, functioning as a selective agonist for the M3 muscarinic acetylcholine receptor. This stable isotope is employed in various biological research applications, including pharmacokinetic studies and metabolic tracking of cholinergic signaling pathways. Its ability to activate M3 muscarinic receptors makes it valuable for understanding aspects of neurotransmission and receptor pharmacology.

(Rac)-5-Hydroxymethyl tolterodine-d5 is a deuterated analog of (Rac)-5-Hydroxymethyl Tolterodine, functioning as a stable isotope for research applications. This compound serves as a useful tool in pharmacokinetic and metabolic studies, allowing for the tracking of drug disposition and dynamics in biological systems. Its isotopic labeling facilitates enhanced accuracy in quantitative analyses, making it valuable for studies in drug development and metabolism.

Pirenzepine-d8 is a deuterated form of Pirenzepine dihydrochloride, functioning as a selective antagonist of the M1 muscarinic receptor. This stable isotope labeling facilitates advanced biochemical analyses and studies of muscarinic receptor signaling pathways. It is particularly useful in pharmacokinetic studies, providing insights into drug interactions and receptor dynamics.

(±)-Darifenacin-d4 hydrobromide is a deuterium-labeled derivative of (±)-Darifenacin, which serves as a selective antagonist of the M3 muscarinic receptor. This stable isotope is useful in pharmacokinetic studies and can aid in elucidating the metabolic pathways of (±)-Darifenacin. Its unique labeling allows for precise tracking in biological assays and enhances the understanding of drug interactions and mechanisms of action.

Fesoterodine-d7 fumarate is a deuterium-labeled derivative of Fesoterodine fumarate, serving as a stable isotope for research applications. Fesoterodine fumarate acts as a competitive antagonist of muscarinic acetylcholine receptors (mAChRs), demonstrating non-subtype selectivity with pKi values of 8.0, 7.7, 7.4, 7.3, and 7.5 for M1, M2, M3, M4, and M5, respectively. It is primarily utilized in studies related to overactive bladder (OAB) and provides valuable insight into muscarinic receptor function and pharmacology.

(Rac)-Tolterodine-d14 tartrate is a stable isotope-labeled derivative of (Rac)-Tolterodine tartrate, featuring deuterium substitutions. This compound is utilized primarily in pharmacokinetic studies and can facilitate the investigation of drug metabolism and pharmacodynamics. Its isotopic labeling enables enhanced sensitivity and accuracy in analytical techniques such as mass spectrometry.

Fesoterodine-d3 is a deuterium-labeled derivative of Fesoterodine, functioning as a competitive antagonist of muscarinic acetylcholine receptors (mAChRs). It exhibits non-subtype selective activity, with pKi values of 8.0, 7.7, 7.4, 7.3, and 7.5 for M1, M2, M3, M4, and M5 receptors, respectively. This reagent is primarily utilized in research related to overactive bladder (OAB) and studies involving receptor pharmacology. Its stable isotope form aids in biochemical assays and metabolic studies.

Quifenadine-d10 is a stable isotope-labeled form of Quifenadine, a hydroxyl-(diphenyl)methyl quinuclidine derivative. As an M3 receptor antagonist, Quifenadine exhibits an IC50 value greater than 1000 nM. This compound is utilized in research related to neurological diseases, enabling insights into receptor interactions and mechanisms of action within the central nervous system.

(±)-Darifenacin-d4 is a deuterium-labeled derivative of (±)-Darifenacin, a selective M3 muscarinic receptor antagonist. This stable isotope is utilized in pharmacokinetic studies and metabolic research to track the absorption, distribution, metabolism, and excretion of the parent compound. Its application in isotopic labeling allows for enhanced sensitivity in analytical techniques such as mass spectrometry.

Arecoline-d5 hydrobromide is a deuterated form of the psychoactive alkaloid Arecoline, functioning as a partial agonist at nicotinic and muscarinic acetylcholine receptors. This reagent is useful for studying the compound's biological activity, including its stimulating, anxiolytic, and anti-parasitic effects. As a stable isotope, Arecoline-d5 hydrobromide can aid in tracing and quantifying metabolic pathways in pharmacological research, particularly in investigations of oxidative stress induction.

Tolterodine-d14 hydrochloride is a deuterium-labeled version of Tolterodine hydrochloride, a potent muscarinic acetylcholine receptor (mAChR) inhibitor. This compound competitively binds to acetylcholine, thereby reducing involuntary bladder muscle contractions and modulating sympathetic nervous activity. In addition to its role in managing overactive bladder and urinary tract infections, Tolterodine has been shown to restore the Nrf2/NF-κB signaling pathway, offering protective effects against inflammation and ferroptosis. Its applications extend to studies involving reactive oxygen species and lipid oxidation.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

(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.

Tricosanoic acid-d3 is a deuterium-labeled derivative of Tricosanoic acid, which acts as an endogenous agonist of long-chain saturated fatty acids and activates the free fatty acid receptor FFAR1. This compound has been shown to promote hair growth and enhance cognitive function by modulating neuronal membrane fluidity, inhibiting neuroinflammatory responses, and contributing to myelination and neuronal energy metabolism. In Alzheimer's disease models, Tricosanoic acid levels are significantly lower in the prefrontal cortex, while higher serum concentrations are associated with improved cognitive performance. As such, Tricosanoic acid serves as a valuable biomarker for conditions related to cognitive decline.

Deoxycholic acid-d4 is a deuterated form of deoxycholic acid, functioning as a stable isotope for research applications. It specifically activates the G protein-coupled bile acid receptor TGR5, which plays a crucial role in stimulating thermogenic activity in brown adipose tissue (BAT). This compound is valuable in studies focused on metabolic processes, energy expenditure, and the modulation of thermogenesis.

Deoxycholic acid-13C is a stable isotope-labeled form of Deoxycholic acid, known for its role in activating the G protein-coupled bile acid receptor TGR5. This activation enhances the thermogenic activity of brown adipose tissue (BAT), making it a valuable tool for research into metabolic processes and energy expenditure. The use of Deoxycholic acid-13C in studies can aid in understanding the mechanisms of energy regulation and the potential therapeutic roles of bile acids in metabolic disorders.