Isotope-Labeled Compounds

Bisoprolol-d5 is a deuterium-labeled derivative of Bisoprolol, a selective and potent β1-adrenergic receptor blocker. This compound predominantly inhibits β1-receptors with minimal β2-receptor activity, making it relevant for research in hypertension, coronary artery disease, and stable ventricular dysfunction. Bisoprolol-d5 serves as a valuable tool in pharmacokinetic studies and metabolic profiling.

Brimonidine-d4 D-tartrate is a stable isotope-labeled form of Brimonidine D-tartrate, featuring deuterium substitution. This compound serves as an important tool for pharmacokinetic studies, enabling precise tracking of drug metabolism and distribution in biological systems. Its incorporation in research applications can enhance the understanding of Brimonidine's mechanisms of action, particularly in the context of its use in the treatment of ocular conditions such as glaucoma.

Acebutolol-d5 is a deuterated form of Acebutolol, specifically designed for use as a stable isotope. This compound is valuable in pharmacokinetic studies and metabolic research, enabling precise tracing of drug metabolism and distribution in biological systems. Its unique labeling makes it an essential tool for researchers investigating the pharmacological effects and metabolism of beta-blockers.

Celiprolol-d9 hydrochloride is a deuterium-labeled derivative of Celiprolol, primarily utilized as a stable isotope. This compound serves as a valuable tool in pharmacokinetic studies, enabling the investigation of metabolic pathways and drug interactions. Researchers can leverage its unique isotopic properties for precise quantification in various biological matrices, making it essential for studies in cardiovascular pharmacology and drug development.

Prazosin-d8 is a deuterium-labeled form of Prazosin, an alpha-adrenergic blocker that exhibits sympatholytic properties. This stable isotope is utilized in pharmacokinetic studies, providing enhanced sensitivity and specificity in metabolic profiling and drug interaction assessments. It plays a crucial role in research applications related to hypertension, anxiety disorders, PTSD, and panic disorder, aiding in the understanding of adrenergic signaling and therapeutic efficacy.

Oxprenolol-d7 hydrochloride is a deuterium-labeled derivative of the β-adrenergic receptor antagonist, Oxprenolol. It exhibits a Ki of 7.10 nM in radioligand binding assays, demonstrating effective inhibition of β-AR activity. This stable isotope is primarily used in pharmacokinetic studies and metabolic research, facilitating investigations into the metabolism and distribution of β-adrenergic antagonists in biological systems.

Sotalol-d6 hydrochloride is a deuterium-labeled derivative of Sotalol hydrochloride, a potent non-selective competitive β-adrenergic receptor blocker. This compound exhibits significant antiarrhythmic activity and is primarily utilized in research focused on pediatric arrhythmias. In addition to blocking β-receptors, Sotalol-d6 also inhibits potassium KCNH2 channels, providing valuable insights into cardiac electrophysiology and potential therapeutic applications.

Brimonidine-d4 is a deuterium-labeled derivative of Brimonidine, a potent agonist of the α2-adrenergic receptor (α2-AR). This stable isotope is primarily utilized in pharmacokinetic studies and metabolic profiling to trace and quantify Brimonidine in biological systems. Its applications extend to research involving ocular therapies and the modulation of neurotransmitter release through α2-AR pathways.

Formoterol-d6 is a deuterium-labeled derivative of Formoterol, a highly selective and long-acting β2-adrenoceptor agonist. This stable isotope is primarily utilized in pharmacokinetic studies and metabolic research to trace the behavior of Formoterol in biological systems. Its incorporation into experimental designs aids in understanding drug metabolism and the pharmacological effects associated with β2-adrenoceptor activation.

Octopamine-d4 hydrochloride is a deuterium-labeled derivative of octopamine, a biogenic monoamine related to noradrenaline. It primarily functions as a neurohormone, neuromodulator, and neurotransmitter in invertebrates. This compound has been shown to stimulate alpha2-adrenoceptors in Chinese hamster ovary cells expressing human alpha2-ARs, leading to enhanced glycogenolysis, glycolysis, oxygen uptake, and gluconeogenesis. Octopamine-d4 hydrochloride is utilized in research applications involving metabolic regulation and neurotransmitter signaling pathways.

Phenylephrine-2,4,6-d3 hydrochloride is a stable isotope-labeled form of phenylephrine hydrochloride. It acts as a selective α1-adrenoceptor agonist, exhibiting pKis of 5.86, 4.87, and 4.70 for the α1D, α1B, and α1A receptors, respectively. This compound is utilized in pharmacological research to trace the metabolism and pharmacokinetics of phenylephrine in biological systems, enhancing the understanding of adrenergic signaling pathways.

Yohimbine-13C,d3 is a deuterium and carbon-13 labeled version of Yohimbine, a potent and nonselective antagonist of alpha-2 adrenergic receptors. With an IC50 value of 0.6 μM, Yohimbine exhibits significant biological activity in modulating adrenergic signaling pathways. This stable isotope compound is valuable for research applications in pharmacokinetics, metabolic studies, and tracing within biological systems.

Prazosin-d8 hydrochloride is a deuterium-labeled derivative of Prazosin hydrochloride, an alpha-adrenergic blocker. This stable isotope is utilized in pharmacokinetic studies and metabolic research, enabling precise tracking of drug metabolism and distribution. Its labeling with deuterium enhances the accuracy of analytical methods, facilitating investigations into the physiological effects of alpha-adrenergic antagonism.

Bambuterol-d9 hydrochloride is a deuterated form of Bambuterol, a long-acting beta-adrenoceptor agonist (LABA) primarily utilized in asthma management. As a prodrug of terbutaline, it demonstrates significant bronchodilatory effects. This stable isotope compound is valuable for pharmacokinetic studies, enabling researchers to trace metabolic pathways and characterize drug behavior in biological systems.

Terazosin-d8 is a deuterated form of Terazosin, functioning as a competitive and orally active antagonist of the α1-adrenoceptor. This compound plays a crucial role in biological research involving the modulation of vascular tone and bladder relaxation. Terazosin-d8 is particularly valuable for studies related to benign prostatic hyperplasia (BPH) and hypertension, facilitating deeper insights into mechanisms of action and pharmacokinetics through stable isotope labeling.

Tulobuterol-d9 hydrochloride is a deuterated derivative of Tulobuterol, a long-acting β2-adrenoceptor agonist. This compound is primarily utilized as a stable isotope in pharmacokinetic studies, providing insights into the metabolic pathways and kinetics of Tulobuterol. It has demonstrated efficacy in reducing the frequency of exacerbations in chronic obstructive pulmonary disease and bronchial asthma while also enhancing diaphragm muscle strength as a sympathomimetic agent. Researchers can leverage Tulobuterol-d9 for elucidating the pharmacological properties and physiological effects of β2-adrenoceptor activation.

Alfuzosin-d3 is a deuterium-labeled analog of Alfuzosin, primarily used as a stable isotope. This compound is significant in pharmacokinetic studies, aiding in the analysis of drug metabolism and pharmacodynamics. Its incorporation in research allows for precise tracking of Alfuzosin's biological pathways and interactions in various biological systems.

Formoterol-d3 is a deuterium-labeled form of Arformoterol, which is the (R,R)-enantiomer of Formoterol, acting as a long-acting β2-adrenergic receptor (β2-AR) agonist with a Kd of 2.9 nM. This stable isotope allows for enhanced tracking and analysis in pharmacokinetic studies. Formoterol-d3 is primarily utilized in research relating to chronic obstructive pulmonary disease (COPD) and can aid in understanding the pharmacodynamics and metabolism of β2-AR agonists.

Metoprolol-d7 is a deuterium-labeled form of Metoprolol, a selective β1 adrenergic receptor antagonist. It primarily targets β1 receptors to effectively manage conditions such as hypertension and heart failure. This stable isotope is useful in pharmacokinetic studies and metabolic research to trace the metabolic pathways and behavior of Metoprolol in biological systems.

Doxazosin-d8 hydrochloride is a deuterium-labeled derivative of Doxazosin hydrochloride, primarily utilized as a stable isotope in biochemical research. This compound retains the pharmacological activity of the parent molecule, targeting alpha-1 adrenergic receptors and providing insights into receptor dynamics and drug metabolism. Its application is particularly relevant in studies involving pharmacokinetics, enabling more accurate tracking and quantification in biological systems.

Lofexidine-d4 hydrochloride is a deuterium-labeled analog of Lofexidine hydrochloride, which selectively targets the α2-adrenergic receptor. This compound is primarily utilized in research to investigate the mechanisms underlying opioid withdrawal and the pharmacological properties of α2-agonists. Its stable isotope labeling allows for enhanced sensitivity in analytical techniques, facilitating studies in drug metabolism and receptor dynamics.

Fenoterol-d6 hydrobromide is a deuterium-labeled analog of Fenoterol hydrobromide, a selective β2-adrenoceptor agonist. As a stable isotope, it serves as a valuable tool in pharmacokinetic studies and metabolic research. Fenoterol hydrobromide is known for its bronchodilator activity, making it relevant in investigations related to asthma, bronchitis, and other obstructive airway diseases. This isotopically labeled compound can enhance the understanding of β2-adrenergic signaling and drug metabolism in various biological assays.

(Rac)-Timolol-d5 maleate is a labeled stable isotope of racemic (S)-Timolol maleate, a non-cardioselective β-adrenoceptor antagonist. This compound effectively reduces intraocular pressure and is commonly employed in the management of glaucoma by inhibiting aqueous humor production. Additionally, it finds applications in the treatment of hypertension, angina pectoris, and myocardial infarction, making it a valuable tool for cardiovascular research and ophthalmic studies.

Bufuralol-d9 hydrochloride is a deuterated form of Bufuralol hydrochloride, serving as a stable isotope. Its primary mechanism involves selective beta-adrenergic receptor antagonism, which is crucial for research involving pharmacokinetics and metabolic studies. This reagent is particularly useful in tracing and quantifying drug metabolism and interactions in biological systems, facilitating advanced studies in cardiovascular and pharmacological research.

(S)-Metoprolol-d7 is a deuterated form of Metoprolol, a selective β1-adrenergic receptor antagonist. This stable isotope-labeled compound is primarily utilized in pharmacokinetic studies and drug metabolism research, providing insights into the pharmacological properties of Metoprolol in cardiovascular applications, particularly in hypertension treatment. Its incorporation of deuterium allows for enhanced tracking and analysis in various analytical techniques.

(S)-Atenolol-d7 is a deuterium-labeled analog of (S)-Atenolol, primarily utilized as a stable isotope. This compound serves as a valuable tool in pharmacokinetic studies and metabolic profiling, allowing for precise tracking of drug metabolism and distribution in biological systems. (S)-Atenolol-d7 is particularly advantageous for researchers investigating cardiovascular pharmacology and drug interactions involving beta-adrenergic blockers.

Phenoxybenzamine-d5 hydrochloride is the deuterated analog of Phenoxybenzamine hydrochloride, a nonselective, irreversible α-adrenoceptor antagonist. This reagent is primarily utilized in research related to hypertension, particularly in cases caused by pheochromocytoma. Additionally, Phenoxybenzamine hydrochloride exhibits antitumor activity, making it relevant for studies in cancer biology and therapeutic development.

Atomoxetine-d3 hydrochloride is a deuterium-labeled derivative of Atomoxetine hydrochloride, a potent and selective norepinephrine reuptake inhibitor. It exhibits binding affinities with Ki values of 5 nM for the human norepinephrine transporter, 77 nM for the serotonin transporter, and 1451 nM for the dopamine transporter. This stable isotope is invaluable for pharmacokinetic studies, tracer experiments, and understanding the metabolic pathways of noradrenergic agents in chemical research.

Alfuzosin-d3 hydrochloride is a deuterated form of Alfuzosin hydrochloride, targeting α1 adrenergic receptors. This stable isotope is utilized primarily in pharmacokinetic studies and drug metabolism research, enabling precise tracking of drug behavior in biological systems. It is particularly relevant in studies involving benign prostatic hyperplasia (BPH) therapies.

(R)-Metoprolol-d7 is a deuterium-labeled analog of Metoprolol, a selective β1 adrenergic receptor antagonist. This stable isotope is essential for pharmacokinetic studies and metabolic research, allowing for precise tracking and quantification of Metoprolol in biological systems. It is particularly valuable in investigations related to cardiovascular diseases, including hypertension and heart failure.

Nomifensine-d3 maleate is a deuterium-labeled derivative of Nomifensine maleate, a potent inhibitor of norepinephrine (NE) and dopamine (DA) reuptake. It effectively blocks the reuptake of NE, DA, and serotonin (5-HT) in rat brain synaptosomes, with IC50 values of 6.6 nM, 48 nM, and 830 nM, respectively. This compound displays antidepressant and analgesic properties, and is applicable in research related to neurodegenerative diseases, substance addiction, and pain mechanisms.

Prazobind-d8 is a deuterium-labeled analog of Prazobind, functioning as an irreversible antagonist of the α1-adrenoceptor. With an IC50 value of 1 nM, Prazobind-d8 exhibits potent competitive binding to α1-adrenoceptor subtypes, specifically in the hippocampus and liver. This compound partially inhibits contractions in smooth, circular, and longitudinal muscle tissues, making it a valuable tool for investigating mechanisms related to blood pressure regulation and related cardiovascular research.

Clonidine-d4 hydrochloride is a deuterium-labeled analog of Clonidine, an alpha-2 adrenergic agonist. This stable isotope is valuable for pharmacokinetic studies and metabolic research, providing enhanced sensitivity and specificity in mass spectrometry analyses. Its applications include elucidating drug metabolism, developing analytical methods, and studying adrenergic signaling pathways.

Medetomidine-d3 hydrochloride is a deuterated form of Medetomidine hydrochloride, targeting adrenergic alpha-2 receptors as an agonist. This stable isotope is useful for pharmacokinetic studies, enabling researchers to trace metabolic pathways and evaluate the efficacy of alpha-2 adrenergic receptor modulation in various biological systems. Its application is particularly valuable in drug discovery and development involving sedative and analgesic compounds.

(Rac)-Tamsulosin-d3 hydrochloride is a deuterium-labeled variant of (Rac)-Tamsulosin hydrochloride, functioning as a stable isotope. This compound is designed for use in pharmacokinetic studies, allowing researchers to trace and quantify the metabolism and distribution of Tamsulosin in biological systems. Its stable isotope labeling facilitates accurate detection and analysis in various biological assays, making it an essential tool for drug metabolism research.

Terbutaline-d9 is a deuterium-labeled analog of Terbutaline, a selective beta-2 adrenergic agonist. This stable isotope is primarily utilized in pharmacokinetic studies to trace drug metabolism and pharmacodynamics in biological systems. Its application in research enhances the understanding of beta-adrenergic signaling pathways and contributes to the development of therapeutic strategies targeting respiratory disorders.

Carteolol-d9 hydrochloride is a deuterated isotope of Carteolol hydrochloride, a non-selective beta-adrenergic antagonist. This compound is primarily utilized in research applications that require stable isotopes for tracing and pharmacokinetic studies. Carteolol hydrochloride is recognized for its efficacy in managing intraocular pressure in glaucoma patients, making the deuterated form suitable for studies in drug metabolism and pharmacology.

Indacaterol-d3 is a deuterium-labeled form of Indacaterol, an inhaled beta-2 adrenergic receptor agonist. This stable isotope is utilized in pharmacokinetic studies and drug metabolism research, enabling precise tracking of drug behavior in biological systems. Its unique labeling allows for enhanced analytical sensitivity in studies involving respiratory conditions and therapeutic applications in chronic obstructive pulmonary disease (COPD) and asthma.

Naftopidil-d5 is a deuterium-labeled form of Naftopidil, a selective alpha-1 adrenoceptor antagonist. With inhibition constants (Kis) of 3.7 nM, 20 nM, and 1.2 nM for the human α1a, α1b, and α1d adrenoceptor subtypes respectively, Naftopidil exhibits significant antiproliferative effects. This reagent is particularly useful for research studies focused on benign prostatic hyperplasia and related conditions.

Acepromazine-d6 hydrochloride is a deuterium-labeled derivative of Acepromazine hydrochloride. As a phenothiazine tranquilizer and alpha-adrenoceptor antagonist, it serves as a valuable tool in pharmacological research to study drug metabolism and behavioral responses. This stable isotope enables precise tracing of biological processes involving Acepromazine, facilitating investigations into its therapeutic effects and mechanisms of action.

Phenoxybenzamine (benzyl-2,3,4,5,6-d5) hydrochloride is a deuterium-labeled form of Phenoxybenzamine hydrochloride, a nonselective and irreversible antagonist of α-adrenoceptors. This compound is employed in research to investigate hypertension, particularly when associated with pheochromocytoma. Additionally, it has demonstrated antitumor properties, making it a valuable tool for studies in cancer biology and pharmacology.

Carazolol-d7 hydrochloride is a deuterium-labeled derivative of Carazolol hydrochloride, primarily targeting β1 and β2 adrenoceptors as a potent antagonist. Additionally, it acts as a selective agonist for the β3-adrenoceptor, making it a versatile tool in cardiovascular research. This reagent is valuable for studying mechanisms in hypertension and related conditions, allowing for enhanced clarity in the investigation of adrenergic signaling pathways.

Alfuzosin-d7 hydrochloride is a deuterium-labeled derivative of Alfuzosin hydrochloride, which functions as an α1 adrenergic receptor antagonist. This compound is primarily used in research applications related to benign prostatic hyperplasia (BPH) and pharmacokinetic studies. The stable isotope label allows for enhanced tracking and analysis of drug metabolism and distribution in various biological systems.

Harman-13C2,15N is a stable isotope-labeled derivative of Harmane, a known benzodiazepine receptor antagonist (IC50 = 7 μM). This compound exhibits notable affinity for various biological targets, including mACh (IC50 = 24 μM), Opioid Receptor (IC50 = 2.8 μM), MAO-A/B (IC50 = 0.5 μM), and the α2-adrenergic receptor (IC50 = 5 μM). Harmane is recognized for its diverse pharmacological activities, such as reducing blood pressure via I1 imidazoline receptor inhibition (IC50 = 30 nM), as well as demonstrating antidepressant, anti-anxiety, anticonvulsant, and analgesic properties. Additionally, it has been shown to affect dopamine biosynthesis and enhance mutagenic effects in specific cellular assays.

Carazolol-d6 hydrochloride is a deuterium-labeled derivative of Carazolol hydrochloride, functioning primarily as a highly potent antagonist of β1 and β2 adrenoceptors. This compound is also recognized for its selective agonistic activity at the β3-adrenoceptor. Carazolol-d6 hydrochloride is valuable in research investigating hypertension and related cardiovascular conditions, providing insights into adrenoceptor pharmacology and the physiological effects of adrenergic signaling.

(S)-Carvedilol-d4 is a deuterium-labeled variant of (S)-Carvedilol, a non-selective β-adrenergic and α-1 adrenergic receptor blocker. This compound is utilized in studies investigating the cardioprotective effects against the vascular and cardiac toxicity induced by Doxorubicin (DOX). Its stable isotope labeling enables precise tracking in metabolic studies and pharmacokinetic research applications.

Guanfacine-d2 hydrochloride is a deuterated form of guanfacine hydrochloride, which primarily targets the α2A-adrenoceptor. This selective agonist exhibits a Kd of 31 nM, demonstrating significant selectivity with a 60-fold preference for the α2A subtype over the α2B receptor. This stable isotope-labeled compound is valuable for pharmacological studies and tracing applications in research related to hypertension and neuropharmacology.

Vilanterol-d4 trifenatate is a deuterium-labeled analog of Vilanterol, a long-acting β2-adrenergic receptor agonist. It selectively binds to β2 adrenergic receptors, leading to increased intracellular cAMP levels and subsequent relaxation of bronchial smooth muscle. This reagent is valuable for research into asthma and related airway diseases, providing a stable isotope for pharmacokinetic and metabolic studies.

Oxprenolol-d7 is a deuterated form of Oxprenolol, a selective β-adrenergic receptor antagonist exhibiting a Ki of 7.10 nM as determined by radioligand binding assays in rat heart muscle. This stable isotope-labeled compound is primarily used in pharmacokinetic studies and metabolic research to trace β-AR activity in various biological systems. Its application in isotope labeling enables enhanced detection and quantification in advanced analytical techniques.

Ractopamine-13C6 is a stable isotope-labeled derivative of Ractopamine, a potent β-adrenergic receptor (βAR) agonist known for its high affinity with a Kd of approximately 25 nM for pig β1AR and β2AR. Additionally, Ractopamine acts as a mTAAR1 agonist with an EC50 of 16 μM. This compound plays a crucial role in promoting muscle mass development, reducing fat deposition, and enhancing feed efficiency in swine. Ractopamine-13C6 is ideal for research focused on increasing lean tissue growth and improving production efficiency in livestock.