Catalog No.
Product Name
Application
Product Information
Citations
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Stable Isotope
Dronedarone-d6 is a deuterium-labeled derivative of the antiarrhythmic agent Dronedarone, primarily targeting various ion channels, including potassium, sodium, and L-type calcium channels. This compound is vital for investigating the mechanisms underlying atrial fibrillation (AF) and atrial flutter, as well as for studying its antiadrenergic properties through its noncompetitive binding to β-adrenergic receptors. In addition, Dronedarone-d6 serves as a substrate and moderate inhibitor of CYP3A4, making it relevant for pharmacokinetic studies in cardiovascular research. -
β1-adrenoceptor Antagonist
Landiolol is a highly selective, ultra-short-acting antagonist of β1-adrenergic receptors. By competitively inhibiting these receptors, Landiolol effectively reduces heart rate and myocardial oxygen demand while minimally affecting cardiac ion channels and exhibiting a weak negative inotropic effect. Its ability to inhibit TNF-α-induced mitochondrial hyperactivity and reactive oxygen species production makes it valuable in models of sepsis, where it can mitigate renal injury. Landiolol is applicable in research involving perioperative tachycardia management and investigations into sepsis-related acute kidney injury. -
Dopamine Receptors Blocker
Trifluoperazine is an antipsychotic agent primarily acting as a blocker of central dopamine receptors. It exhibits significant activity as a potent α1-adrenergic receptor antagonist and a NUPR1 inhibitor, demonstrating anticancer properties. Additionally, Trifluoperazine functions as a calmodulin inhibitor and inhibits P-glycoprotein, contributing to its diverse biological effects. This compound is utilized in research on schizophrenia and shows potential as a reversible inhibitor of influenza virus morphogenesis. -
β₂-adrenergic receptor Agonist/PDE4 Inhibitor
GS-5759 is a dual-action compound functioning as a β₂-adrenergic receptor agonist and a phosphodiesterase 4 (PDE4) inhibitor. By activating the β₂ receptor, GS-5759 elevates intracellular cAMP levels, resulting in bronchial dilation. Additionally, its inhibition of PDE4 activity decreases cAMP degradation, thereby enhancing anti-inflammatory responses. This compound is relevant for research into respiratory disorders, particularly chronic obstructive pulmonary disease (COPD), demonstrating significant bronchodilatory and anti-inflammatory effects in preclinical models. -
Cardiac
UK-1745 is a cardiotonic agent that targets phosphodiesterase III, leading to increased intracellular levels of cyclic adenosine monophosphate (cAMP) in cardiomyocytes. This elevation enhances myocardial contractility while also exhibiting β-adrenergic receptor antagonism, which decreases cardiac oxygen consumption and mitigates calcium overload. Due to these properties, UK-1745 is a valuable tool for research applications focused on congestive heart failure and cardiac function modulation. -
Fluorescent α1-Adrenergic Antagonist
BODIPY FL prazosin is a fluorescent α1-adrenergic antagonist, exhibiting Ki values of 14.5 nM and 43.3 nM for the α1a and α1b adrenergic receptors, respectively. This compound acts as a fluorescent ligand, with excitation and emission wavelengths at 485 nm and 535 nm. BODIPY FL prazosin is valuable for elucidating the subcellular localization and distribution of different α1-adrenoceptor subtypes in various biological contexts. -
Stable Isotope
(R)-Propranolol-d7 is a deuterated derivative of (R)-Propranolol, serving as a stable isotope-labeled compound. This reagent is invaluable for pharmacokinetic studies and metabolic pathway analysis, enabling the tracking of drug metabolism and distribution in biological systems. Researchers can utilize (R)-Propranolol-d7 in studies focused on cardiovascular research, anxiety treatments, and the mechanisms of action associated with beta-adrenergic receptors. -
β-Adrenoceptor Blocker
Propranolol is a non-selective β-adrenoceptor antagonist that effectively crosses the blood-brain barrier. It exhibits high affinity for both β1 and β2 adrenergic receptors, with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol has demonstrated inhibitory activity against [3H]-DHA binding in rat brain membrane preparations, with an IC50 of 12 nM. This compound is commonly employed in research related to hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy. -
α/β Adrenergic Receptor Blocker
Primidolol is an orally active α/β Adrenergic Receptor blocker that exhibits antihypertensive properties. This compound demonstrates significant antibacterial and antioxidant activities, making it relevant in studies focused on both cardiovascular diseases and infectious processes. Its dual mechanism of action positions Primidolol as a valuable tool for research aimed at understanding the interplay between adrenergic signaling and microbial resistance. -
β2-Drenergic Receptor Agonist
Terbutaline is an orally active β2-adrenergic receptor agonist that effectively stimulates the β2-adrenergic receptors. Its primary biological activity includes bronchodilation, making it relevant for research on asthma symptoms and respiratory disorders. Terbutaline is commonly used in studies investigating the therapeutic effects of β2-agonists in pulmonary conditions. -
β2-Drenergic Receptor Agonist
Terbutaline sulfate is an orally active β2-adrenergic receptor agonist, primarily utilized in the treatment of asthma and other bronchospastic conditions. As an active metabolite of bambuterol, it promotes bronchodilation by relaxing smooth muscle in the airways. This compound is essential for research applications focused on respiratory pharmacology and the therapeutic evaluation of β2-adrenergic systems in asthma symptom management. -
α/β-Adrenergic Receptor Blocker
Arotinolol is a nonselective α/β-adrenergic receptor blocker that also acts as a vasodilating β-blocker. It exhibits significant inhibitory activity against the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. Arotinolol is primarily utilized as an antihypertensive agent in the management of various cardiovascular conditions, as well as for certain non-cardiovascular diseases, facilitating research in cardiovascular pharmacology and receptor interaction studies. -
Antipsychotic Agent
Melperone is a butyrophenone class compound that functions primarily as an atypical antipsychotic agent. It acts as a multireceptor antagonist, with binding affinities (Kd values) of 102 nM, 180 nM, 180 nM, and 150 nM for the 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. With lower binding affinity for histamine H1 and various serotonin receptors, Melperone also exhibits inhibitory effects on CYP2D6. This compound is valuable for research into schizophrenia and behavioral disturbances in elderly populations. -
5-HT1α/ α2-adrenergic Antagonist
Spiroxatrine is a selective dual antagonist of the 5-HT1α and α2-adrenergic receptors, exhibiting Ki values of 3.94 nM for 5-HT1α, 224,000 nM for 5-HT1β, and 118.5 nM for 5-HT2. This compound demonstrates notable sedative effects, making it relevant for research into anxiety and depressive disorders. Spiroxatrine is valuable for studies exploring the modulation of serotonergic and adrenergic signaling pathways. -
Antidepressant Agent
Etoperidone is an antidepressant agent that functions as an orally active antagonist of serotonin and noradrenaline reuptake. It exhibits Kd values of 36 nM, 38 nM, 85 nM, and 570 nM for the 5-HT2 receptor, α1-adrenergic receptor, 5-HT1A receptor, and α2-adrenergic receptor, respectively. Due to its unique pharmacological profile, Etoperidone is utilized in research focused on the mechanisms of mood regulation and the treatment of depressive disorders. -
5-HT2A Receptor Ligand
Iloperidone carboxylic acid is a ligand targeting the 5-HT2A receptor. This metabolite of Iloperidone demonstrates a strong affinity for the 5-HT2A receptor, with a pKi value of 8.15, while also showing moderate binding affinity to adrenergic receptors α1, α2B, and α2C. It serves as a valuable reagent for research exploring neuropharmacology and the modulation of serotonergic signaling in various biological contexts. -
α2-adrenoceptor Antagonist/5-HT Receptor re-uptake Inhibitor
Napamezole (hydrochloride) functions as an α2-adrenoceptor antagonist and a serotonin (5-HT) reuptake inhibitor, exhibiting Ki values of 28 nM and 93 nM for rat α2 and α1 adrenergic receptors, respectively. This compound is particularly relevant for research into depression and related neuropsychiatric disorders, facilitating studies on serotonin modulation and adrenergic signaling pathways. Its dual action can provide insights into the mechanisms underlying mood regulation and therapeutic interventions. -
α2B/C-Adrenergic Receptor Antagonist
ARC 239 is a selective antagonist of the α2B and α2C adrenergic receptors, exhibiting a pKi of 7.06 for rat kidney α2B and 6.95 for human α2C. In addition, ARC 239 inhibits the 5-HT1A receptor with a Ki value of 63.1 nM. This compound is valuable in research involving adrenergic signaling pathways and the modulation of neurotransmitter systems, making it suitable for studies on cardiovascular function and psychiatric disorders. -
PKC Inhibitor
NA 0345 is a potent protein kinase C (PKC) inhibitor, exhibiting IC50 values of 70 nM in the presence of 12-O-tetradecanoyl-13-acetate and 110 nM in its absence. This compound selectively inhibits PKC activity, effectively reducing the positive inotropic effects associated with α1-adrenergic receptors. NA 0345 is useful in research applications aimed at elucidating the role of PKC in cardiovascular function and signal transduction pathways. -
Anti-tumor Agent
Scoulerine hydrochloride is a multi-target inhibitor primarily acting as an anti-tumor agent. It disrupts the PI3K/Akt/mTOR signaling pathway and α1D-adrenergic receptors, leading to microtubule destabilization, cell cycle arrest, and apoptosis in cancer cells. This compound also inhibits mitochondrial dehydrogenase activity and demonstrates effects on GABA receptors and BACE1, suppressing tumor cell proliferation, migration, invasion, and stem cell-like properties. Additionally, Scoulerine hydrochloride exhibits pharmacological activities against Plasmodium falciparum, as well as antibacterial, antiemetic, and antitussive properties, while also influencing endoplasmic reticulum stress and mitochondrial function. It is particularly relevant in studies focused on leukemia, ovarian cancer, and colorectal cancer. -
Stable Isotope
Gramine-d2 is a deuterium-labeled derivative of Gramine, a natural alkaloid derived from giant reed. This compound functions as an adiponectin receptor agonist, exhibiting IC50 values of 3.2 μM for AdipoR2 and 4.2 μM for AdipoR1. Additionally, Gramine acts as an agonist for human and mouse β2-Adrenergic receptors, demonstrating anti-tumor, anti-viral, and anti-inflammatory activities. Gramine-d2 is valuable for research applications that require stable isotopic labeling in biological studies. -
NMDA Receptor Antagonist
Ifenprodil is a noncompetitive antagonist of the NMDA receptor, with a strong affinity for the NR1A/NR2B subunit (IC50 = 0.34 μM) compared to NR1A/NR2A (IC50 = 146 μM). This compound also acts as an α1 adrenergic receptor antagonist and inhibits GIRK channels, reducing basal inward currents. Additionally, Ifenprodil demonstrates antiviral activity against A/H1N1 strains (EC50 = 6.6 µM) and possesses neuroprotective, anticonvulsant, and antinociceptive properties. It is suitable for research in cerebrovascular diseases and peripheral arterial obliterative disease. -
α1-adrenergic Receptor Antagonist
Butanserin is a selective antagonist of the α1-adrenergic receptor, primarily utilized in cardiovascular research. This compound modulates adrenergic signaling pathways, making it valuable for investigating the role of α1-adrenoceptors in various cardiovascular conditions. Its potency and specificity support its application in studies aimed at understanding hypertension and heart failure mechanisms. -
α2 Receptor Antagonist
Napitane mesylate is a selective antagonist of presynaptic α2 adrenergic receptors, impacting norepinephrine reuptake inhibition. This compound demonstrates significant antidepressant activity, making it relevant for research in mood disorders and neuropharmacology. It is utilized to explore the modulation of noradrenergic neurotransmission and its effects on depressive states. -
α2-adrenergic Agonist
Detomidine is a potent α2-adrenergic agonist characterized by its imidazole structure. Its primary mechanism involves the activation of α2-adrenergic receptors, leading to significant analgesic effects in a dose-dependent manner. This compound is commonly utilized in veterinary medicine for sedation and analgesia, as well as in research applications focused on examining α2-adrenergic signaling pathways. -
ADRB2 Agonist
Indacaterol xinafoate is a potent β2-adrenergic receptor agonist known for its long-acting bronchodilatory effects. By inhibiting NF-κB activity in a β-arrestin2-dependent manner, it not only improves lung function but also mitigates further lung damage, making it relevant in the context of chronic obstructive pulmonary disease (COPD). This compound serves as a valuable tool for research into asthma and related respiratory disorders. -
Stable Isotope
Tetrahydrozoline-d4 hydrochloride is a deuterium-labeled form of Tetrahydrozoline hydrochloride, an α-adrenergic agonist that targets α-adrenergic receptors to induce vasoconstriction. This stable isotope is utilized in research applications focusing on nasal and conjunctival congestion. Its unique isotopic labeling allows for enhanced tracking and quantification in various biochemical studies. -
β-adrenergic Blocker
Bunitrolol hydrochloride is a β-adrenergic blocker known for its high affinity for β-adrenergic receptors and its significant antagonist activity. It also exhibits weak α1-blocking effects. This compound is primarily utilized in research related to cardiovascular diseases, including hypertension and angina pectoris, and is applicable in studies of placental transport. -
Silodosin Racemate
(Rac)-Silodosin is a racemic mixture that targets the α1A-adrenergic receptor (α1A-AR) as a potent and selective antagonist. This compound is primarily utilized in research related to urology and the treatment of benign prostatic hyperplasia (BPH), contributing to the understanding of adrenergic signaling pathways. Its oral bioavailability makes it a significant candidate for pharmacological studies focusing on α1-adrenergic receptor modulation. -
Adrenergic Receptor
2-(4-(2-Hydroxy-3-(isopropyl(nitroso)amino)propoxy)phenyl)acetamide targets adrenergic receptors and is recognized as a genotoxic derivative of Atenolol. This compound has been shown to induce DNA fragmentation in rat hepatocytes at concentrations between 0.1 and 1 mM, making it a valuable tool for studying genotoxic mechanisms and the effects of adrenergic signaling in cellular contexts. Its applications extend to research involving DNA damage and repair pathways. -
Adrenergic Receptor Agonist
Octopamine is a biogenic monoamine that functions as an adrenergic receptor agonist, primarily targeting alpha2-adrenoceptors. It serves as a neurohormone, neuromodulator, and neurotransmitter in invertebrates. In vitro studies demonstrate that Octopamine enhances glycogenolysis, glycolysis, oxygen uptake, and gluconeogenesis, along with increasing portal perfusion pressure. This compound is valuable for research in neurobiology, metabolism, and cardiovascular studies. -
Adrenergic Receptor Inhibitor
Cetamolol hydrochloride acts as a potent β1-adrenergic receptor inhibitor, exhibiting intrinsic sympathomimetic activity and cardioselectivity. It demonstrates a prolonged inhibitory effect on heart rate and myocardial contractility at low to moderate doses, making it a valuable reagent for cardiovascular research. Its unique profile allows for exploration in studies evaluating hypertension, arrhythmias, and other cardiac conditions. -
α2 Agonist
Apraclonidine dihydrochloride is a selective α2 adrenergic receptor agonist with weak activity at α1 receptors. This compound is primarily used to reduce intraocular pressure (IOP) in various ophthalmic conditions. Its effectiveness in lowering IOP makes it a valuable tool in the study of glaucoma and other eye disorders. -
β2-adrenergic Receptor Agonist
Trantinterol hydrochloride is a potent agonist of the β2-adrenergic receptor, demonstrating significant efficacy in bronchial relaxation. It serves as a valuable tool in the investigation of asthma and other respiratory conditions. This compound may aid in understanding the mechanisms of bronchial hyperreactivity and support the development of therapeutic strategies targeting β2-adrenergic pathways. -
Adrenergic Receptor Agonist
BFE-55 is a derivative of befunolol that acts as a β-adrenergic receptor partial agonist. This compound exhibits significant biological activity by modulating adrenergic signaling pathways. BFE-55 can be utilized in research focused on cardiovascular dynamics and therapeutic interventions targeting adrenergic receptors. -
Adrenoreceptor Agonist
Colterol hydrochloride is an agonist of the adrenergic receptors, demonstrating significant affinity for the β1-adrenoreceptor and β2-adrenoreceptor, with respective IC50 values of 645 nM and 147 nM. It exhibits potent bronchodilator activity, making it valuable for research applications related to respiratory conditions. This compound can be utilized in studies investigating cardiovascular responses and airway reactivity, contributing to the understanding of adrenergic signaling pathways. -
Adrenergic Receptor Agonist
Amibegron is a selective β3-adrenergic receptor agonist, demonstrating an EC50 of 3.5 nM for activation of β-adrenoceptors in rat colon tissues. This compound exhibits notable anxiolytic and antidepressant properties, making it a valuable tool for research in neuropharmacology and the study of mood disorders. Its specificity for β3-adrenergic receptors lends it potential applications in exploring metabolic and cardiovascular responses. -
β3-adrenergic Receptor Agonist
SB251023 is a selective β3-adrenergic receptor agonist, exhibiting pEC50 values of 7.14 for the β3a and 6.91 for the β3b receptor subtypes. This compound effectively modulates intracellular cyclic AMP levels and influences extracellular acidification rates (EAR) in cellular systems. SB251023 is relevant for research into cardiovascular diseases and metabolic disorders, providing insights into the therapeutic potential of β3-adrenergic signaling in related pathologies. -
Drug Metabolite
Deacetylmoxisylyte is an orally active drug metabolite derived from the prodrug Moxisylyte, primarily targeting alpha-1 and alpha-2 adrenoceptors. It demonstrates significant affinity and selectivity in rabbit corpus cavernosum and urethra tissues, with IC50 values of 400 nM and 1200 nM, respectively. This compound is valuable in pharmacological research focused on understanding adrenergic receptor interactions and their physiological effects. -
Adrenergic Receptor Antagonist
Phenoprolamine hydrochloride is an adrenergic α1 receptor antagonist known for its potent antihypertensive properties. In addition to lowering blood pressure, it exhibits neuroprotective and cardioprotective activities. This compound also inhibits the enzymatic activity of CYP2D and CYP3A, resulting in the down-regulation of their mRNA transcription, which may have implications in drug metabolism studies and cardiovascular research. -
Metabolite
4-Hydroxy xylazine O-glucuronide lithium is a metabolite derived from the α2-adrenergic receptor agonist xylazine. This compound serves as an important biochemical marker, aiding in the study of xylazine metabolism and its physiological effects. It can be synthesized from xylazine through the intermediate metabolite 4-hydroxy xylazine and is valuable in pharmacokinetic and toxicological research applications. -
β1/β2 Adrenergic Receptor Antagonist
4-Hydroxypropranolol-d7 hydrochloride is a deuterated derivative of 4-Hydroxypropranolol, functioning as a potent β1/β2 adrenergic receptor antagonist. It exhibits equivalent potency to its parent compound Propranolol, with pA2 values of 8.24 and 8.26 for β1 and β2 receptors, respectively. This compound is characterized by its intrinsic sympathomimetic activity, membrane stabilizing effects, and significant antioxidant properties, making it valuable for various biochemical and pharmacological research applications. -
α-Adrenoreceptor Antagonist
Taprizosin is an α-adrenoreceptor antagonist that selectively inhibits the activity of α1-adrenergic receptors. It has demonstrated efficacy in modulating vascular smooth muscle contraction and influencing blood pressure regulation. This compound is primarily utilized in cardiovascular research, particularly in studies focused on hypertension and related disorders. -
α-2B adrenergic receptor Agonist
AGN-201781 is an orally active agonist of the α-2B adrenergic receptor. This compound exhibits significant biological activity in modulating adrenergic signaling pathways, making it a valuable tool for research into neuropathic pain mechanisms and potential therapeutic interventions. Its specificity for the α-2B receptor supports investigations into pain management and related neurological studies. -
α1-Adrenoceptor Ligand
CHIR-2279 is a high-affinity ligand for the α1-adrenergic receptor, exhibiting a binding affinity characterized by a Ki value of 5 nM. This compound serves as a valuable tool for investigating the α1-adrenoceptor signaling pathways and has potential applications in drug development aimed at cardiovascular and other relevant disorders. -
β-Adrenergic Receptor Agonist
Hexoprenaline sulfate is a selective β-adrenergic receptor agonist that promotes bronchodilation. This compound enhances adenylate cyclase activity, leading to an increased uptake of 14C-Aminopyrine. Additionally, Hexoprenaline sulfate exhibits anti-inflammatory and anti-infective properties, while also demonstrating effects on placental weight and blood flow. It is applicable in research areas including inflammation, immunology, infection, endocrinology, and the study of neurological diseases, such as asthma, chronic bronchitis, sepsis, and organophosphorus compound intoxication. -
Adrenergic Receptor Antagonist
RU 52583 is an oral bioactive antagonist of the alpha-2 adrenergic receptor. This compound has been shown to enhance cognitive function in rodent models with septohippocampal system damage, indicating its potential utility in studying cognitive disorders. Its pharmacological profile may provide insights into the modulation of adrenergic signaling in various neurological research applications. -
Stable Isotope
Solabegron-d8 is a deuterium-labeled derivative of Solabegron, a selective β3-adrenergic receptor agonist. It effectively stimulates cAMP accumulation in Chinese hamster ovary cells expressing human β3-adrenergic receptors, exhibiting an EC50 value of 22 nM. This compound is primarily utilized in research focused on the treatment of overactive bladder and irritable bowel syndrome, allowing for the investigation of β3-adrenergic signaling pathways in various biological contexts. -
Stable Isotope
Lofexidine-d4 is a deuterium-labeled derivative of Lofexidine (hydrochloride), a selective α2-adrenergic receptor agonist. This compound is primarily employed in research related to opioid withdrawal by mimicking the activity of Lofexidine in biological assays. The stable isotope labeling enables precise tracking in pharmacokinetic studies and helps in elucidating the pharmacological properties of opioid withdrawal treatments. -
β3-adrenergic Receptor Agonist
N-5984 hydrochloride is a potent and selective agonist of the β3-adrenergic receptor. This compound exhibits significant biological activity in promoting lipolysis and thermogenesis, making it a valuable tool for research on obesity and diabetes mellitus. Its specificity for the β3-adrenergic receptor allows for targeted investigations into metabolic regulation and potential therapeutic applications in metabolic disorders.
