Isotope-Labeled Compounds

Anthracene-9-carboxylic acid-d9 is a deuterium-labeled derivative of anthracene-9-carboxylic acid. This compound primarily functions as a stable isotope and is widely utilized in research to study calcium-activated chloride currents (CaCCs) across various cell types, including smooth muscle, epithelial, and salivary gland cells. Its deuterium labeling enhances analytical sensitivity in experiments, facilitating more accurate investigations into cellular signaling and ion channel activity.

Niflumic Acid-d5 is a deuterium-labeled derivative of Niflumic acid, which acts primarily as a calcium-activated chloride channel blocker. This compound exhibits significant analgesic and anti-inflammatory properties, making it useful in the management of conditions such as rheumatoid arthritis. Its stable isotope form is valuable for research applications in pharmacokinetics, metabolic studies, and mechanistic investigations of calcium channel modulation.

γ-Aminobutyric acid-d6 is a deuterium-labeled form of γ-Aminobutyric acid, a crucial inhibitory neurotransmitter in the mammalian central nervous system. This compound primarily targets ionotropic GABA receptors (GABAA) and metabotropic receptors (GABAB), playing a significant role in regulating neuronal excitability. It is useful in research applications focused on neurotransmitter dynamics, GABAergic signaling, and metabolic studies involving stable isotopes.

γ-Aminobutyric acid-d2 is a deuterium-labeled form of γ-Aminobutyric acid, a critical inhibitory neurotransmitter in the mammalian central nervous system. It functions by binding to both ionotropic GABA receptors (GABAA) and metabotropic GABA receptors (GABAB), playing a vital role in neuronal signaling and modulation. This stable isotope is particularly useful in research applications involving metabolic tracing, pharmacokinetics, and the study of neurochemical pathways.

Methionine-d3 is a deuterium-labeled form of Methionine, serving as a stable isotope useful in metabolic studies. This compound is known for its chemoprotective properties and its ability to inhibit neuronal activity via GABAA receptor activation. Methionine-d3 is valuable for researchers conducting studies in neurobiology and metabolic pathways, offering insights into the roles of methionine in cellular processes.

p-Hydroxybenzaldehyde-d4 is a deuterium-labeled variant of p-Hydroxybenzaldehyde. It primarily serves as a stable isotope for advanced analytical applications. This compound is known for its presence in Dendrocalamus asper bamboo shoots and exhibits antagonistic activity on the GABAA receptor α1β2γ2S subtype at elevated concentrations. It is useful in various research applications, including metabolic studies and receptor pharmacology.

Propofol-d18 is a deuterium-labeled derivative of Propofol, primarily utilized as a stable isotope in research. This compound effectively activates GABAA receptors, leading to enhanced inhibitory neurotransmission while simultaneously inhibiting excitatory synaptic transmission mediated by glutamate receptors. Propofol-d18 is valuable for studies investigating the neuropharmacology of anesthetics and the dynamics of synaptic transmission.

Tetrahydrodeoxycorticosterone-d3 is a deuterated form of Tetrahydrodeoxycorticosterone, a potent positive allosteric modulator of the GABAA receptor. This neurosteroid exhibits significant neuroinhibitory properties, making it a valuable tool in neuroscience research. Its stable isotope labeling allows for precise tracking and quantification in various biological assays and studies related to neuropharmacology and neurobiology.

Furosemide-d5 is a deuterium-labeled derivative of furosemide, primarily targeting the Na+/K+/2Cl- cotransporters, NKCC1 and NKCC2. This compound acts as a potent loop diuretic, exhibiting significant biological activity in the management of conditions such as congestive heart failure, hypertension, and edema. Additionally, furosemide-d5 can function as a GABAA receptor antagonist, demonstrating enhanced selectivity for α6-containing receptors. It serves as a valuable tool for biochemical research and pharmacokinetic studies involving furosemide.

17β-Estradiol sulfate-d4 sodium is a deuterium-labeled derivative of 17β-Estradiol sulfate, commonly referred to as β-Estradiol 3-sulfate sodium salt. This stable isotope is utilized in biochemical research to investigate the metabolism and pharmacokinetics of estrogenic compounds. Its applications extend to studies in neurobiology, endocrinology, and reproductive health, providing valuable insights into the hormonal modulation of various biological processes.

Riluzole-13C,15N2 is a stable isotope-labeled form of Riluzole, specifically incorporating 13C and 15N isotopes. Riluzole functions primarily as an anticonvulsant and is known to act as a use-dependent Na+ channel blocker. Additionally, it inhibits GABA uptake with an IC50 of 43 μM. This reagent is useful for tracer studies in metabolic research, pharmacokinetics, and drug mechanism investigations.

Propofol-d17 is a deuterium-labeled analog of Propofol, serving as a stable isotope for research applications. This compound acts primarily as a potent GABAA receptor agonist, effectively enhancing inhibitory synaptic transmission while simultaneously inhibiting glutamate receptor-mediated excitatory responses. Due to its significant antinociceptive properties, Propofol-d17 is valuable in studies focusing on pain modulation and anesthetic mechanisms.

Etiocholanolone-d5 is a deuterated form of Etiocholanolone, a metabolic product of testosterone. This compound serves as a neurosteroid with known positive allosteric modulation of the GABAA receptor, although it exhibits less potency compared to its enantiomer. Its unique isotopic labeling makes it valuable for tracing and quantification studies in metabolic research and pharmacokinetics, particularly in investigations related to anticonvulsant activity.

Acamprosate-d3 calcium is a deuterium-labeled form of Acamprosate calcium, a compound that acts as a GABA receptor agonist and modulates glutamatergic systems. This stable isotope is utilized in research to study the pharmacokinetics and dynamics of Acamprosate in various biological systems. Its unique labeling allows for precise tracking and analysis in metabolic studies and drug interaction investigations.

Baclofen-d4 is a deuterium-labeled variant of Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA). It acts as a selective agonist for metabotropic GABAB receptors, mimicking GABA's function to induce slow presynaptic inhibition. With its ability to effectively cross the blood-brain barrier, Baclofen-d4 is particularly valuable for research on muscle spasticity and related neurological conditions, providing insights into GABAB receptor dynamics and therapeutic applications.

Acamprosate-d6 calcium is a stable isotope-labeled form of Acamprosate calcium, functioning primarily as a GABA receptor agonist and modulating glutamatergic neurotransmission. This compound is crucial for research into alcohol dependence and withdrawal, as it helps investigate the biochemical pathways involved in these processes. The stable isotope labeling enhances the sensitivity and accuracy of analytical techniques, making it valuable for various pharmacological studies.

Alpidem-d14 is a stable isotope-labeled variant of Alpidem, a potent GABAA receptor ligand targeting the α1β2γ2 subunit with an IC50 of 17 nM. This compound is primarily investigated for its anxiolytic properties and influences various biological processes, including modulation of mitochondrial permeability and glutathione levels, leading to hepatocyte necrosis. Additionally, Alpidem-d14 is utilized in research focused on anxiety disorders, convulsive conditions, and the behavioral effects in stressed rodent models.

Baclofen-d5 hydrochloride is a deuterated analog of Baclofen, functioning as a selective agonist for the metabotropic GABAB receptor (GABABR). This compound closely mimics the action of γ-aminobutyric acid (GABA), facilitating slow presynaptic inhibition via GABAB signaling pathways. With its significant ability to penetrate the blood-brain barrier, Baclofen-d5 hydrochloride is valuable in studying muscle spasticity and related neurological conditions. Its stable isotope labeling further enhances its applications in metabolic and pharmacokinetic research.

Cipepofol-d6 is a deuterium-labeled derivative of Cipepofol, which acts as a gamma-aminobutyric acid (GABA) receptor potentiator. This stable isotope is utilized in research to investigate the pharmacokinetics and metabolic pathways of Cipepofol. Its biological activity as a psychomotor stabilizing agent makes it valuable for studies related to anesthetic effects and neuropharmacology.

p-Hydroxybenzaldehyde-d5 is a stable isotope-labeled derivative of p-Hydroxybenzaldehyde. This compound, primarily recognized for its role as a major component in vanilla aroma, exhibits antagonistic effects on the GABAA receptor, specifically the α1β2γ2S subtype, at elevated concentrations. It is widely utilized in chemical research for studies involving receptor activity and metabolic tracking.

Etbicyphat-13C3 is a stable isotope-labeled variant of Etbicyphat, a potent competitive antagonist of GABA(A) receptors. This compound has been shown to induce epileptiform activities in hippocampal CA1 neurons and effectively binds to GABA(A)-benzodiazepine receptors. Its isotopic labeling facilitates detailed studies of receptor interactions and the dynamics of GABAergic neurotransmission in various research applications.

Propofol-d14 is a deuterium-labeled form of Propofol (2,6-Diisopropylphenol-d14) designed for stable isotope applications. It acts as a potent and direct agonist of the GABAA receptor, inhibiting excitatory synaptic transmission mediated by glutamate receptors. This compound exhibits antinociceptive properties and is primarily utilized in research related to sedation and hypnotic mechanisms.

γ-Aminobutyric acid-4,4-d2 is a deuterated form of γ-aminobutyric acid (GABA), a principal inhibitory neurotransmitter in the mammalian brain. This compound selectively binds to ionotropic GABA receptors (GABAA) and metabotropic receptors (GABAB), modulating synaptic transmission and neuronal excitability. The stable isotope labeling allows for advanced metabolic studies and tracing applications in neuropharmacology and neuroscience research.

Isonipecotic acid-d9 is a deuterium-labeled analogue of Isonipecotic acid, which functions as a partial agonist at GABAA receptors. This stable isotope is valuable for pharmacokinetic studies and in vivo experimentation, providing insights into the metabolism and dynamics of GABAergic compounds. Researchers can employ Isonipecotic acid-d9 to explore mechanisms of action related to neurological disorders and the role of GABAA receptor modulation in various physiological processes.

3α,21-Dihydroxy-5α-pregnan-20-one-d3 is a deuterium-labeled derivative of the neurosteroid 3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), which acts as a positive modulator of GABAA receptors. This compound enhances the response of neurons to low concentrations of GABA, specifically at the α4β1δ subtype of GABAA receptors in vitro. It serves as a valuable stable isotope labeled reagent for research focusing on neurosteroid activity and GABAergic modulation.

P-Hydroxybenzaldehyde-13C6 is a stable isotope-labeled derivative of p-Hydroxybenzaldehyde. This compound serves as a key component in vanilla flavor profiles and exhibits antagonistic activity on the α1β2γ2S subtype of the GABAA receptor at elevated concentrations. It is useful in various research applications, particularly in studies involving flavor chemistry and neuropharmacology.

Cipepofol-d6-2 is a deuterium-labeled derivative of Cipepofol, a gamma-aminobutyric acid (GABA) receptor potentiator and psychomotor stabilizing agent. This stable isotope compound is essential for studies involving pharmacokinetics and metabolic pathways of Cipepofol, facilitating precise tracking and analysis in research applications. It provides a valuable tool for investigating the effects and mechanisms of GABA modulation in nervous system functioning.

Etiocholanolone-d2 is a deuterium-labeled derivative of Etiocholanolone (5β-Androsterone), which serves as a stable isotope for research applications. As a metabolite of testosterone, Etiocholanolone exhibits anticonvulsant properties and acts as a positive allosteric modulator of the GABAA receptor, albeit with lower potency compared to its enantiomer. This reagent is essential for studies focused on neurosteroids and their mechanisms in the central nervous system.

Rac-Vigabatrin-13C,d2 is a stable isotope-labeled derivative of Vigabatrin, a potent and irreversible inhibitor of GABA transaminase. By inhibiting the catabolism of GABA, it increases the levels of this inhibitory neurotransmitter in the brain, making it an effective antiepileptic agent. This compound is valuable for research applications that require stable isotope labeling, such as metabolic studies and drug mechanism investigations.

4-Hydroxy midazolam methanoate-d5 is a deuterated derivative of 4-hydroxymidazolam, a significant metabolite of the benzodiazepine midazolam, which exhibits potent anxiolytic effects. This stable isotope is primarily utilized in pharmacokinetic studies and drug metabolism research, enabling precise tracking of midazolam metabolism and its active metabolites in biological systems. Its incorporation in analytical assays aids in understanding the pharmacodynamics and pharmacokinetics of benzodiazepines, facilitating advancements in therapeutic interventions.

Baclofen-d4-1 is a deuterium-labeled derivative of Baclofen, an orally active selective agonist of metabotropic GABAB receptors. By mimicking GABA's actions, Baclofen induces slow presynaptic inhibition, contributing to its activity in the central nervous system. This compound is particularly relevant for research on muscle spasticity and neurological disorders, facilitating studies involving pharmacokinetics and metabolic pathways.

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.