Isotope-Labeled Compounds

Flupirtine-d4 hydrochloride is a deuterium-labeled variant of Flupirtine hydrochloride, a non-opioid analgesic that crosses the blood-brain barrier. This compound functions primarily as a neuronal potassium channel opener (Kv7 activator) and exhibits properties as an NMDA receptor antagonist and GABA receptor activator. It is utilized in research focused on pain management, neuroprotection, and conditions such as Alzheimer’s disease and multiple sclerosis, offering insights into pathways of ischemic neuron death, oxidative stress modulation, and the maintenance of blood-brain barrier integrity. Flupirtine-d4 hydrochloride serves as a valuable tool for studying the underlying mechanisms and therapeutic approaches for neurological disorders.

p-Hydroxybenzaldehyde-13C is a stable carbon isotope-labeled variant of p-Hydroxybenzaldehyde. This compound is primarily utilized in metabolic studies and isotopic tracing due to its involvement in the biosynthesis pathways found in Dendrocalamus asper bamboo shoots. It exhibits an antagonistic effect on the GABAA receptor of the α1β2γ2S subtype at elevated concentrations, making it a valuable tool for research into neurological functions and receptor signaling.

Tiagabine-d5 hydrochloride is a deuterium-labeled derivative of Tiagabine hydrochloride, primarily functioning as a selective GABA reuptake inhibitor. It exhibits potent anticonvulsant properties, with IC50 values of 67 nM, 446 nM, and 182 nM for [3H]GABA uptake in synaptosomes, neurons, and glial cells, respectively. This stable isotope form is valuable for pharmacokinetic studies and metabolic profiling in research applications focused on GABAergic neurotransmission and seizure disorders.

Valnoctamide-d5 is a stable isotope-labeled form of Valnoctamide, a derivative of valproate known for its efficacy in suppressing benzodiazepine-refractory status epilepticus. This compound primarily targets GABAA receptors, modulating their activity to exert its therapeutic effects. Valnoctamide-d5 is suitable for use in biochemical research and drug development studies focused on epilepsy and related neurological disorders.

Etifoxine-d5 is a deuterium-labeled analog of Etifoxine, a non-benzodiazepine compound that acts as a positive allosteric modulator of GABAA receptors containing α1β2γ2 and α1β3γ2 subunits. This reagent is essential for studies focusing on the anxiolytic and anticonvulsant properties of GABAergic compounds. Its stable isotope labeling allows for enhanced tracing and quantification in various research applications, including pharmacokinetic and metabolic studies.

Tiagabine-d6 is a deuterium-labeled derivative of the potent GABA reuptake inhibitor, Tiagabine. This compound selectively inhibits GABA reuptake, exhibiting IC50 values of 67 nM, 446 nM, and 182 nM in synaptosomes, neurons, and glial cells, respectively. Tiagabine-d6 is primarily utilized in research applications requiring stable isotope labeling, facilitating studies in pharmacokinetics and metabolism of GABAergic drugs.

THIP-d4, a deuterium-labeled derivative of THIP (Gaboxadol), selectively targets extrasynaptic GABAA receptors (eGABARs) with a reported EC50 of 13 μM for δ-GABAAR. This compound demonstrates strong potentiation of GABAA-mediated currents in layer 2/3 neurons while having no effect on miniature inhibitory postsynaptic currents (IPSCs). THIP-d4 is valuable for research into sleep disorders and other neurological conditions related to GABAergic signaling.

Sarcosine-d3 is a deuterated form of sarcosine, which acts as a competitive inhibitor of the glycine transporter type I (GlyT1) and serves as a co-agonist for the N-methyl-D-aspartate (NMDA) receptor. By increasing glycine levels, sarcosine-d3 indirectly enhances NMDA receptor activity. This reagent is primarily utilized in the investigation of schizophrenia and related neurological disorders, facilitating studies on neurotransmission and metabolic pathways.

Stearoyl-L-carnitine-d3 chloride is a stable isotope-labeled derivative of Stearoyl-L-carnitine chloride, which serves as an endogenous long-chain acylcarnitine. This compound exhibits a moderate inhibitory effect on GlyT2, reducing glycine responses by approximately 16.8% at concentrations up to 3 μM. It is mainly utilized in biochemical research to trace metabolic pathways and study acylcarnitine-related biological processes.

N-Arachidonylglycine-d8 is a deuterated analog of N-Arachidonylglycine, primarily functioning as a stable isotope. It acts as a selective agonist for the GPR18 receptor, with an EC50 of 44.5 nM, while showing no activity at CB1 or CB2 receptors. Additionally, N-Arachidonylglycine-d8 inhibits the glycine transporter GLYT2 with an IC50 of 5.1 μM and effectively promotes endometrial cell migration. This reagent is valuable in research exploring endocannabinoid signaling and transporter interactions.

Sarcosine-13C3 is a stable isotope-labeled derivative of N-Methylglycine that serves as a valuable tool in biological research. As a competitive inhibitor of the glycine transporter type I (GlyT1) and a co-agonist at the N-methyl-D-aspartate (NMDA) receptor, Sarcosine-13C3 enhances glycine levels, thereby potentiating NMDA receptor activity. This compound is particularly useful in studies related to schizophrenia and neuropharmacology, facilitating the investigation of glycine modulation in neurotransmission.

Ivabradine-d6 hydrochloride is a deuterium-labeled derivative of ivabradine hydrochloride, which serves as an inhibitor of the If current in sinoatrial node cells. This compound exhibits an IC50 value of 2.9 μM, making it a potent heart rate-lowering agent. Ivabradine-d6 hydrochloride is primarily utilized in pharmacokinetic studies and metabolic research, enabling the investigation of ivabradine's mechanisms and effects in cardiovascular studies.

Ivabradine-d3 hydrochloride is the deuterated form of Ivabradine hydrochloride, a potent inhibitor of the If channel. With an IC50 of 2.9 μM, it functions primarily as a heart rate-lowering agent. This stable isotope-labeled reagent is ideal for pharmacokinetic studies and metabolic research, facilitating the investigation of Ivabradine's mechanisms of action and its therapeutic effects in cardiovascular diseases.

Glycine-d5 is a deuterium-labeled form of Glycine, an important inhibitory neurotransmitter in the central nervous system (CNS). It also serves as a co-agonist with glutamate, enhancing excitatory signaling at the glutamatergic N-methyl-D-aspartic acid (NMDA) receptors. This stable isotope is useful in metabolic studies, tracer experiments, and research involving neurotransmitter dynamics.

Glycine-13C2 is a stable isotope-labeled form of glycine, which serves as an inhibitory neurotransmitter in the central nervous system (CNS). It also functions as a co-agonist with glutamate, enhancing excitatory signaling at glutamatergic N-methyl-D-aspartic acid (NMDA) receptors. This reagent is invaluable for applications in metabolic studies, tracer studies, and research on neurotransmitter dynamics.

Decanoic acid-d19 is a deuterium-labeled derivative of decanoic acid, serving as a stable isotope in research applications. This compound acts as a non-competitive inhibitor of AMPA receptors and demonstrates brain-penetrant properties, contributing to its antiseizure effects. Decanoic acid-d19 is valuable for studies investigating ionotropic glutamate receptors and exploring potential therapeutic avenues for epilepsy and related neurological disorders.

Glycine-d2 is a deuterium-labeled form of glycine, a significant inhibitory neurotransmitter in the central nervous system. It functions as a co-agonist with glutamate, enhancing excitatory signaling through NMDA receptors. Glycine-d2 is valuable for studies involving neurotransmission, metabolic tracing, and isotopic labeling in biological research.

Glycine-2-13C is a stable isotope-labeled form of glycine, a vital inhibitory neurotransmitter in the central nervous system (CNS). It functions as a co-agonist with glutamate, enhancing excitatory transmission at the N-methyl-D-aspartic acid (NMDA) receptors. This reagent is useful for metabolic labeling studies, tracing pathways in bioenergetics, and investigating neurotransmission dynamics in various research applications.

N,N-Dimethylglycine-d6 hydrochloride is a deuterium-labeled derivative of N,N-Dimethylglycine hydrochloride, functioning as a stable isotope. This compound serves as a methyl donor and exhibits potential biological activity by acting as a partial agonist at the glycine site of the N-methyl-D-aspartate receptor (NMDAR). It is utilized in research studying its effects on immunity, antioxidant properties, and its antidepressant-like activity, making it valuable for investigations into oxidative stress and related diseases. Additionally, its surfactant properties are of interest for various biochemical applications.

Glycine-1-13C is a stable isotope-labeled form of glycine, functioning primarily as an inhibitory neurotransmitter in the central nervous system (CNS). It serves as a co-agonist with glutamate, enhancing excitatory signaling at the glutamatergic N-methyl-D-aspartic acid (NMDA) receptors. This reagent is valuable in metabolic studies, neurotransmission research, and isotopic tracing experiments.

Glycine-15N is a stable isotope-labeled form of glycine, a crucial inhibitory neurotransmitter in the central nervous system. It plays a significant role as a co-agonist with glutamate, enhancing excitatory signaling at NMDA receptors. This compound is widely utilized in research applications such as metabolic studies, neuropharmacology, and isotope tracing in biological systems.

D-Serine-d3 is a deuterium-labeled form of D-Serine, functioning primarily as a stable isotope in biochemical research. D-Serine, an endogenous amino acid, serves as a co-agonist at NMDA glutamate receptors, influencing various neurological processes. Its involvement in NMDA receptor-mediated neurotransmission, synaptic plasticity, and cell migration makes it a valuable tool for studies related to neuropharmacology and neurodevelopmental disorders. This labeled compound facilitates advanced research into the dynamics of neurotransmitter interactions and their implications in brain function.

Glycine-13C2,15N is a stable isotope-labeled form of glycine, incorporating both carbon-13 and nitrogen-15 isotopes. As an important inhibitory neurotransmitter in the central nervous system, glycine also functions as a co-agonist with glutamate, enhancing excitatory signaling at the NMDA receptors. This labeled reagent is valuable for applications in metabolic studies, isotope tracing, and investigating neurotransmitter dynamics in various biological systems.

Decanoic acid-d5 is a deuterium-labeled derivative of decanoic acid, which serves as a stable isotope in research applications. The compound functions as a non-competitive inhibitor of AMPA receptors and exhibits brain-penetrant properties, contributing to its antiseizure effects. This reagent is valuable for studies involving neurotransmission, epilepsy, and the metabolic pathways of medium-chain triglycerides.

S-Benzyl-DL-cysteine-2,3,3-d3 is a deuterium-labeled derivative of Benzylcysteine, functioning as an inhibitor of the ASCT2 transporter. It demonstrates an apparent Ki of 780 μM, acting through a competitive inhibition mechanism by binding to the substrate-binding site of ASCT2. This compound is valuable for studying amino acid transport and cellular uptake mechanisms in various biological systems.

Elacridar-d4(Major) is a deuterium-labeled variant of Elacridar, a potent inhibitor of P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP). This stable isotope labeled compound is instrumental in studying the role of efflux transporters in drug distribution, particularly within the brain, and is valuable for cancer research. Its unique deuterated structure allows for detailed metabolic and pharmacokinetic investigations.

L-Phenylalanine-d5 is a stable deuterated form of the essential amino acid L-Phenylalanine, which serves as a competitive antagonist of the glycine and glutamate-binding sites on N-methyl-D-aspartate receptors (NMDARs). It exhibits an affinity for the α2δ subunit of voltage-dependent calcium channels with a Ki of 980 nM, making it valuable in studies of neurotransmission and synaptic function. This reagent is widely utilized in biochemical research, including metabolic studies and the synthesis of pharmaceuticals and food flavors.

L-Phenylalanine-13C6 is a stable isotope-labeled variant of the essential amino acid L-Phenylalanine. As a competitive antagonist of the glycine- and glutamate-binding sites on N-methyl-D-aspartate receptors (NMDARs), it exhibits a binding affinity (KB) of 573 μM. Additionally, it targets the α2δ subunit of voltage-dependent calcium channels with a Ki of 980 nM. This reagent is valuable in biochemical research, particularly in metabolic studies and the synthesis of pharmaceuticals and food flavorings.

Acetylcholine-d4 chloride is a deuterium-labeled form of the neurotransmitter acetylcholine. It functions as a potent cholinergic agonist and effectively crosses the blood-brain barrier (BBB). This reagent modulates dopaminergic neuronal activity by stimulating nicotinic acetylcholine receptors (nAChRs) and has also been shown to inhibit the aggregation of p53 mutant peptides in vitro. Its unique isotopic labeling makes it a valuable tool for chemical and biological research applications.

L-Phenylalanine-d8 is the deuterated form of the essential amino acid L-Phenylalanine, which is recognized for its role as an antagonist of the α2δ subunit of voltage-dependent calcium channels with an inhibition constant (Ki) of 980 nM. Additionally, it competes for glycine- and glutamate-binding sites at N-methyl-D-aspartate receptors (NMDARs) with a binding affinity (KB) of 573 μM. This stable isotope is essential for applications in metabolic studies, tracer experiments, and the synthesis of pharmaceuticals and food flavoring compounds.

Acetylcholine-d9 chloride is a deuterium-labeled form of acetylcholine chloride, a potent cholinergic agonist that effectively crosses the blood-brain barrier. This compound modulates dopaminergic neuronal activity by stimulating nicotinic acetylcholine receptors (nAChRs). Additionally, it has been shown to inhibit p53 mutant peptide aggregation in vitro, making it valuable for research focused on neurobiology, receptor pharmacology, and protein aggregation studies.

L-Phenylalanine-13C9 is a stable isotope labeled form of the essential amino acid L-Phenylalanine, also known as (S)-2-Amino-3-phenylpropionic acid. This compound serves as an antagonist of the α2δ subunit of voltage-dependent calcium channels, exhibiting a Ki of 980 nM. Additionally, L-Phenylalanine acts as a competitive antagonist at the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) with a KB of 573 μM. It is employed in various research applications, including metabolic studies and tracer experiments in biochemical pathways.

L-Phenylalanine-15N is a stable isotope-labeled form of the essential amino acid L-Phenylalanine, recognized chemically as (S)-2-Amino-3-phenylpropionic acid. It serves as an antagonist of the α2δ subunit of voltage-dependent calcium channels, exhibiting a Ki value of 980 nM. Furthermore, it acts as a competitive antagonist at the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) with a KB value of 573 μM. This compound finds broad applications in biochemical research, particularly in studies related to amino acid metabolism and receptor function.

Acetylcholine-d4 bromide is a stable isotope-labeled form of acetylcholine bromide, featuring deuterium substitution. It serves as a valuable internal standard in quantitative mass spectrometry applications, enabling precise detection and quantification of acetylcholine in biological samples. This reagent is essential for studies involving neurotransmitter dynamics, pharmacokinetics, and metabolic analysis, providing enhanced accuracy in research focused on cholinergic signaling pathways.

DL-Phenylalanine-d5 is a deuterium-labeled derivative of DL-Phenylalanine, a naturally occurring amino acid. This stable isotope is utilized in various biochemical and metabolic research applications, particularly in studies involving protein synthesis and pathways involving phenylalanine metabolism. Its labeling enables precise tracking and quantitative analysis in mass spectrometry and NMR experiments, facilitating advanced studies in metabolic flux and neurochemistry.

Acetylcholine-d9 bromide is a deuterium-labeled derivative of acetylcholine that serves as a stable isotope. This reagent is primarily used in biochemical and pharmacological research to study acetylcholine receptor interactions and metabolic pathways. Its unique isotopic labeling enables precise tracking in mass spectrometry and other analytical techniques, facilitating advancements in neurobiology and drug development.

L-Phenylalanine-d2 is a deuterium-labeled form of the essential amino acid L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid). It serves as a stable isotope and acts as an antagonist of the α2δ subunit of voltage-dependent calcium channels, with a Ki of 980 nM. Additionally, L-Phenylalanine-d2 competitively inhibits glycine- and glutamate-binding sites on both N-methyl-D-aspartate receptors (NMDARs) and non-NMDARs, demonstrating a Ki of 573 μM. This reagent is valuable for applications in biochemical research, including metabolic studies and tracer experiments.

Verapamil-d3 hydrochloride is a deuterium-labeled derivative of the calcium channel blocker, verapamil hydrochloride. It serves as a potent inhibitor of P-glycoprotein (P-gp) and CYP3A4, facilitating detailed pharmacological studies. This stable isotope is primarily utilized in research related to hypertension, cardiac arrhythmias, and angina, providing insight into drug metabolism and transport mechanisms in various biological systems.

L-Phenylalanine-13C9,15N is a stable isotope-labeled version of the essential amino acid L-Phenylalanine, featuring carbon-13 and nitrogen-15 isotopes. This compound serves as an α2δ subunit antagonist for voltage-dependent Ca²⁺ channels, exhibiting a Ki of 980 nM. Additionally, L-Phenylalanine acts as a competitive antagonist at the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs), with a KB of 573 μM. Its applications extend to the fields of metabolic studies, tracer studies in amino acid metabolism, and the development of food flavors and pharmaceuticals.

L-Phenylalanine-3-13C is a stable isotope-labeled analog of the essential amino acid L-Phenylalanine, known to inhibit the α2δ subunit of voltage-dependent calcium channels with a Ki of 980 nM. This compound also competitively antagonizes glycine- and glutamate-binding sites on N-methyl-D-aspartate receptors (NMDARs), exhibiting a KB of 573 μM. L-Phenylalanine-3-13C is utilized in metabolic studies and tracer applications, facilitating insights into amino acid metabolism and neurotransmitter signaling.

Gabapentin-d4 is a deuterium-labeled derivative of Gabapentin, a GABA analog. This stable isotope is primarily utilized in research applications to study the pharmacokinetics and metabolism of Gabapentin. Its use facilitates the investigation of neurological disorders, epilepsy, and neuropathic pain mechanisms.

L-Phenylalanine-13C is a stable isotope-labeled form of L-Phenylalanine, an essential amino acid known for its role in protein synthesis. This compound serves as an antagonist of the α2δ subunit of voltage-dependent Ca2+ channels, showing a Ki of 980 nM, and competes for glycine and glutamate-binding sites on N-methyl-D-aspartate receptors (NMDARs) with a KB of 573 μM. L-Phenylalanine-13C is utilized in various research applications, including metabolic studies, food flavoring production, and pharmaceutical development.

1-Octanol-d17 is a deuterated derivative of 1-Octanol, serving as a stable isotope for various analytical applications. This saturated fatty alcohol acts as an inhibitor of T-type calcium channels, demonstrating an IC50 value of 4 μM for native T-currents. In addition to its role in calcium signaling research, 1-Octanol is also recognized for its potential as a biofuel due to its diesel-like properties.

Diltiazem-d3 hydrochloride is a deuterated form of Diltiazem hydrochloride, acting as a calcium channel blocker. This stable isotope serves as a valuable tool in pharmacokinetic studies and metabolic research, enabling the investigation of Diltiazem's mechanisms of action and its effects on calcium influx regulation. Its use in isotopic labeling facilitates precise tracking in biological systems, contributing to enhanced understanding in drug metabolism and efficacy studies.

Nifedipine-d6 is a deuterium-labeled derivative of nifedipine, a potent calcium channel blocker. This stable isotope is primarily utilized in pharmacokinetic studies and metabolic research to trace the metabolism and distribution of nifedipine in biological systems. Its incorporation of deuterium enhances analytical precision in spectroscopic and mass spectrometric techniques, facilitating advanced research in drug development and therapeutic monitoring.

Acetylcholine-d16 bromide is a deuterium-labeled analog of acetylcholine, functioning as a stable isotope. It serves as a valuable standard in analytical studies, particularly in the quantification of acetylcholine dynamics and metabolism. This reagent is instrumental for researchers investigating cholinergic signaling pathways and exploring cholinergic receptor interactions.

Taurolithocholic acid-d4 is a deuterated form of Taurolithocholic acid, serving as a stable isotope internal standard in chemical research. Its primary mechanism involves the conjugation and regulation of bile acids within hepatic pathways. This reagent is essential for accurately quantifying Taurolithocholic acid levels in biological samples, enabling researchers to explore metabolic pathways and bile acid homeostasis. Its isotopic labeling enhances analytical precision in mass spectrometry and other analytical techniques.

Amlodipine-d4 is a deuterium-labeled derivative of Amlodipine, a dihydropyridine calcium channel blocker and antianginal agent. This compound selectively inhibits voltage-dependent L-type calcium channels, leading to reduced calcium influx. Amlodipine-d4 is primarily utilized in pharmacokinetics studies and metabolic research to investigate the pharmacological effects of Amlodipine in conditions such as hypertension and cancer.

Ethosuximide-d3 is a deuterium-labeled derivative of Ethosuximide, which primarily targets low-voltage activated T-type calcium channels. This reagent exhibits significant anti-epileptic properties and has been shown to enhance phenotypic outcomes in various neurodegenerative disease models. Ethosuximide-d3 is valuable for tracing studies and metabolic research, aiding in the understanding of drug disposition and action in biological systems.

Amlodipine-d4 maleate is a deuterium-labeled derivative of Amlodipine maleate, a dihydropyridine calcium channel blocker. This compound selectively inhibits voltage-dependent L-type calcium channels, thereby reducing calcium influx and exerting pharmacological effects as an antianginal agent. Amlodipine-d4 maleate is particularly useful in research applications focused on hypertension and cancer, providing a stable isotopic reference for metabolic studies and pharmacokinetic assessments.