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β-adrenergic Receptor Antagonist
Propranolol-d7 hydrochloride is a deuterium-labeled β-adrenergic receptor antagonist, exhibiting high affinity for both β1 and β2 adrenergic receptors with Ki values of 1.8 nM and 0.8 nM, respectively. It effectively inhibits [3H]-DHA binding in rat brain membrane preparations, with an IC50 of 12 nM. This compound is widely utilized in research focused on cardiovascular conditions such as hypertension, myocardial infarction, cardiac arrhythmias, and angina pectoris, as well as in studies on pheochromocytoma and hypertrophic cardiomyopathy. -
Adrenergic Blocker
Dibenamine hydrochloride is a competitive and irreversible adrenergic blocker that modulates the effects of epinephrine by binding to adrenergic receptors. This compound has been shown to significantly enhance the rate of degradation of I-epinephrine in murine models. It is widely utilized in research applications focusing on cardiovascular pharmacology and the study of adrenergic signaling pathways. -
β2 Adrenoreceptor Agonist
Procaterol hydrochloride hemihydrate is an orally active β2 adrenoreceptor agonist that primarily targets the β2 adrenergic receptors. It exhibits significant bronchodilatory activity, making it useful in studies related to asthma. This compound is valuable for researching therapeutic approaches to manage respiratory disorders and improving pulmonary function. -
Noradrenaline Antagonist
(±)-WB 4101 hydrochloride is a potent antagonist of noradrenaline, primarily targeting adrenergic receptors. This compound demonstrates significant efficacy in inhibiting noradrenaline's biological activity, influencing smooth muscle function. Its applications extend to pharmacological research in cardiovascular studies and investigations involving the modulation of adrenergic signaling pathways. -
Active Compound
Scopoline is an active compound that functions as an α1 adrenergic receptor agonist. It has been shown to exert significant biological activity in modulating cardiovascular responses and may play a role in various research applications related to hypertension and other adrenergic signaling pathways. This compound is valuable for studies investigating the therapeutic potential of adrenergic receptor modulation. -
Adrenergic Receptor Control
3-Hydroxy xylazine is a metabolite of the α2-adrenergic receptor agonist xylazine, primarily engaging with adrenergic receptors to exert its effects. This compound is significant in the study of adrenergic signaling pathways and can be utilized in research involving sedation and analgesia. Its role as a metabolite provides insight into the pharmacokinetics and mechanism of action of xylazine in various biological systems. -
β2-AR Agonist
3,4-Dihydro-6,7-isoquinolinediol acts as a selective β2-adrenergic receptor (β2-AR) agonist, exhibiting an EC50 of 106.9 μM in CH-K1/GA1S cells. In addition to its agonistic activity, it demonstrates anti-inflammatory properties by inhibiting nitric oxide production in lipopolysaccharide-stimulated mouse macrophage RAW 264.7 cells. This compound is suitable for research applications exploring β2-AR signaling and its implications in inflammation. -
β-block Agent
Timolol is a non-selective β-blocker that primarily acts on β-adrenergic receptors. It is widely utilized for its ability to lower intraocular pressure in conditions such as open-angle glaucoma and ocular hypertension. Additionally, Timolol serves as a valuable research tool for studying various cardiovascular and neurological conditions, including hypertension, myocardial infarction, migraine prophylaxis, and atrial fibrillation. Its cardioprotective properties further underscore its relevance in therapeutic investigations. -
Adrenergic Receptor Inhibitor
Todralazine hydrochloride is a selective β2 adrenergic receptor inhibitor primarily used in the treatment of hypertension. Its mechanism involves blocking β2 adrenergic receptors, contributing to its effectiveness as an antihypertensive agent. In addition to its receptor inhibition, Todralazine hydrochloride exhibits antioxidant properties, providing potential benefits in research focused on oxidative stress and cardiovascular health. -
Adrenergic Receptor Agonist
Amidephrine is a selective agonist of the alpha 1-adrenergic receptor, primarily involved in modulating smooth muscle contraction. It effectively inhibits monopulse field contraction in both the vas deferens epithelium and prostate gland, demonstrating its potential utility in studies of reproductive physiology and urology. This compound is valuable for research applications focused on adrenergic receptor signaling and its physiological implications. -
Stable Isotope
Clenbuterol-d9 is a deuterium-labeled derivative of Clenbuterol, a selective β2-adrenergic receptor agonist known for its potent biological activity, with an EC50 of 31.9 nM. This stable isotope serves as a valuable tool for pharmacokinetic studies and metabolic research, enabling precise tracking of drug interactions and bioavailability in various biological systems. Clenbuterol-d9 is instrumental in advancing research on β-adrenergic signaling and its implications in respiratory and metabolic disorders. -
β1/β2 Adrenergic Receptor Antagonist
4-Hydroxypropranolol hydrochloride is an active metabolite of Propranolol, functioning primarily as a β1 and β2 adrenergic receptor antagonist. This compound exhibits comparable potency to its parent drug, inhibiting β1-adrenergic receptors with a pA2 value of 8.24 and β2-adrenergic receptors with a pA2 value of 8.26. Additionally, 4-Hydroxypropranolol hydrochloride possesses intrinsic sympathomimetic activity, membrane stabilizing properties, and significant antioxidant effects, making it valuable in research related to cardiovascular diseases and stress response mechanisms. -
Adrenergic Receptor
Tilisolol hydrochloride is a non-selective β-adrenergic antagonist that acts primarily on adrenergic receptors, demonstrating significant vasodilatory and hypotensive effects. This compound promotes relaxation of smooth muscle in canine coronary arteries through the opening of ATP-sensitive K+ channels and exhibits concentration-dependent relaxation in KCl-precontracted rat thoracic aorta. Additionally, tilisolol hydrochloride has been shown to reduce diastolic blood pressure in a dose-dependent manner, with a mild increase in heart rate observed in spinal cord-stimulated rats. It is widely used in cardiovascular research to study adrenergic signaling and blood pressure regulation. -
α1A-AR Degrader
α1A-AR Degrader 9c is a selective, reversible degrader specifically targeting the α1A-adrenergic receptor (α1A-AR) through the proteasomal degradation pathway. It demonstrates significant biological activity, inhibiting the proliferation of PC-3 cells with an IC50 value of 6.12 μM. This compound is valuable for research applications in prostate cancer, providing insights into the therapeutic potential of α1A-AR degradation in oncology studies. -
Antiarrhythmic Agent
(+)-Sotalol is the S-isomer of Sotalol, functioning primarily as a non-selective β-adrenergic receptor blocker. This antiarrhythmic agent is effective in prolonging action potential duration in isolated cardiac muscle, making it valuable in the study of cardiac rhythm disorders. Its role in various research applications includes examining mechanisms underlying arrhythmias and evaluating therapeutic strategies for heart rate regulation. -
Adrenergic Receptor Agonist
Synephrine hydrochloride is an alkaloid that acts as an agonist for both α-adrenergic and β-adrenergic receptors. Derived from Citrus aurantium, this sympathomimetic compound exhibits stimulatory effects on the central nervous system and may promote weight loss through increased metabolic rate and thermogenesis. It is widely used in research applications investigating metabolic processes and the physiological effects of adrenergic stimulation. -
Lightening Agent
Undecylenoyl phenylalanine is a competitive antagonist of α-melanocyte-stimulating hormone (MSH) and β-adrenergic receptors (β-ADR), effectively inhibiting melanogenesis in melanocytes. This compound demonstrates significant potential as a skin lightening agent by reducing hyperpigmentation, thereby improving conditions such as melasma lesions and solar lentigines. Its mechanism of action makes it valuable for research in dermatological applications targeting skin pigmentation disorders. -
Beta-1 Receptor Full Agonist
T-0509 is a selective full agonist of the β1 adrenergic receptor. It activates the cAMP signaling pathway, significantly enhancing myocardial contractility. This compound is useful in research applications investigating cardiac function, β1 receptor signaling, and related pharmacological effects in cardiovascular studies. -
Adrenergic Receptor Agonist
Brombuterol hydrochloride is a selective β-adrenergic receptor agonist known for its ability to stimulate adenylate cyclase, leading to increased cyclic AMP levels. This compound exhibits significant bronchodilatory effects, making it useful in research related to respiratory disorders such as asthma and chronic obstructive pulmonary disease (COPD). Additionally, Brombuterol hydrochloride serves as a valuable tool in the study of adrenergic signaling pathways and their role in various physiological processes. -
α-adrenergic Receptor Antagonist
(S)-Terazosin is a selective α-adrenergic receptor antagonist, exhibiting high affinity for α1a, α1b, and α1d-adrenoceptors with Ki values of 3.91 nM, 0.79 nM, and 1.16 nM, respectively. Additionally, it interacts with α2a, α2B, and α2c-adrenoceptors, showing Ki values of 729 nM, 3.5 nM, and 46.4 nM. This compound is primarily utilized in research focused on cardiovascular conditions, benign prostatic hyperplasia, and as an innovative tool in understanding adrenergic signaling pathways. -
Adrenergic Receptor
Ethylnorepinephrine hydrochloride is a sympathomimetic compound that primarily targets adrenergic receptors. It exhibits bronchodilator activity, making it valuable in research focused on respiratory disorders and cardiovascular responses. This reagent is utilized in studies involving the modulation of sympathetic nervous system activity and the investigation of adrenergic signaling pathways. -
Stable Isotope
Isoxsuprine-d6 hydrochloride is a deuterium-labeled form of Isoxsuprine hydrochloride, a selective beta-adrenergic receptor agonist. It exhibits inhibitory constants (Kis) of 13.65 μM and 3.48 μM for myometrial and placental beta-adrenergic receptors, respectively, and also functions as an NMDA receptor antagonist. This stable isotope variant is valuable for pharmacokinetic studies and metabolic tracing in biological research, facilitating an understanding of drug interactions and mechanisms of action. -
Adrenergic Receptor Agonist
Prenalterol is a selective β1-adrenergic receptor agonist that primarily targets cardiovascular pathways. It facilitates increased cardiac contractility without affecting gastrointestinal smooth muscle activity. This compound is valuable for research applications focused on cardiovascular disease mechanisms and therapeutic interventions. -
Adrenergic Receptor
(-)-Dihydroalprenolol serves as a β-adrenergic receptor antagonist, effectively inhibiting β-adrenergic receptor activity. This compound is known to induce desensitization in approximately 60% of β-adrenergic receptor binding sites and decreases the binding affinity of specific β-adrenergic ligands. Additionally, (-)-Dihydroalprenolol may influence the stimulation of membrane-bound adenylate cyclase, making it a relevant tool in cardiovascular and pharmacological research applications. -
α2B/2C Adrenoceptor Antagonist
ARC 239 dihydrochloride is a selective antagonist of the α2B and α2C adrenoceptors, demonstrating pKd values of 5.95, 7.41, and 7.56 at the α2A, α2B, and α2C receptors, respectively. This compound effectively binds to CHO cell membranes expressing human recombinant α2A, α2B, and α2C adrenoceptor subtypes, showing pKi values of 5.6, 8.4, and 7.08. ARC 239 dihydrochloride is valuable for research applications in studying adrenergic signaling pathways and the physiological roles of α2 adrenergic receptors. -
Stable Isotope
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. -
α-2C Adrenergic Receptor Antagonist
ORM-10921 free base is a selective antagonist of the α-2C adrenergic receptor, exhibiting a Ki value of 1.4 nM. This compound demonstrates significant antidepressant and antipsychotic-like activities, making it a valuable tool for research in neuropharmacology and the exploration of mood disorders. Its specificity and potency position ORM-10921 free base as a potential candidate for studies related to the modulation of neurotransmitter systems. -
Stable Isotope
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. -
β3- Adrenergic Receptor Agonist
Mirabegron impurity-1 is a potent and selective β3-adrenergic receptor agonist. It has been shown to inhibit metabolism, contributing to its biological activity. This compound is valuable for research applications focused on bladder function and related disorders, facilitating studies into the pharmacological effects of β3-adrenergic modulation. -
Deuterated Brombuterol
Brombuterol-d9 is a deuterated form of Brombuterol, a selective β-adrenergic receptor agonist. This compound is utilized in pharmacological research to investigate β-adrenergic signaling pathways and assess the pharmacokinetics of Brombuterol in biological systems. Its deuterated nature enhances analytical sensitivity in mass spectrometry and other detection methods, making it a valuable tool for studying drug metabolism and receptor interactions. -
Adrenergic Receptor Antagonist
Nadolol-d9 is a deuterated derivative of Nadolol, functioning as a non-selective antagonist of β-adrenergic receptors. By inhibiting these receptors, Nadolol-d9 plays a significant role in cardiovascular research, particularly in studies related to hypertension and arrhythmias. Its stable isotope labeling enhances metabolite tracking and pharmacokinetic profiling in drug development. -
Stable Isotope
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. -
α2 Receptor Agonist
Guanoxabenz hydrochloride is a selective α2 adrenergic receptor agonist, demonstrating a Ki value of 4000 nM and a fully activated form with a potency of 40 nM at the α2A adrenoceptor. This compound plays a crucial role in modulating adrenergic signaling pathways and is commonly utilized in research investigating autonomic regulation, anxiety disorders, and analgesic effects. Its specificity for the α2 receptors supports studies aimed at exploring therapeutic targets for various neurological conditions. -
β-adrenoceptor Agonist
Arbutamine is a potent, nonselective β-adrenoceptor agonist that primarily targets β1-, β2-, and β3- adrenergic receptors. This short-acting compound enhances cardiac stress by increasing heart rate, contractility, and systolic blood pressure. Arbutamine is utilized in research applications related to cardiac function and stress testing, providing valuable insights into adrenergic receptor activity within cardiovascular studies. -
Stable Isotope
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. -
α1 Adrenoceptor Antagonist
Benoxathian hydrochloride is a potent α1 adrenoceptor antagonist primarily used in research to investigate the mechanisms of anorexia. Its action on α1 adrenergic receptors can provide insights into appetite control and related metabolic pathways, making it a valuable tool for studies in neuropharmacology and appetite regulation. -
βARK Substrate
RESA peptide is a substrate for β-adrenergic receptor kinase (βARK) that facilitates βARK-mediated phosphorylation. Its N-terminal acidic residues enhance both the efficiency of phosphorylation and the binding affinity to the kinase. This peptide is valuable for studies investigating βARK signaling pathways and the regulation of adrenergic receptors, contributing to the understanding of cardiac function and other physiological processes. -
β1 Adrenergic Receptor Antagonist
ICI 89406 is a selective β1 adrenergic receptor antagonist that can be labeled with positron emitters for positron emission tomography (PET) imaging. This compound is primarily utilized in cardiovascular research to study the effects of β1 adrenergic signaling, enabling insights into heart function and related disorders. Its ability to specifically target the β1 adrenergic receptor makes it a valuable tool for investigating therapeutic interventions in various cardiovascular conditions. -
Beta-adrenergic Receptor Agonist
Metaterol is a selective beta-adrenergic receptor agonist that modulates adrenergic signaling pathways. It primarily exhibits bronchodilatory effects, making it valuable in respiratory research, particularly for studying asthma and chronic obstructive pulmonary disease (COPD). This compound can aid in understanding receptor dynamics and developing targeted therapeutic interventions. -
β2 Adrenergic Receptor Agonist
Milveterol hydrochloride is a long-acting β2-adrenergic receptor agonist that primarily targets the β2 adrenergic receptor. It is utilized in research related to asthma and chronic obstructive pulmonary disease (COPD), facilitating studies on its therapeutic effects and mechanisms of action. This compound contributes to understanding bronchial relaxation and airway response in respiratory disorders. -
α1/β1-Adrenergic Receptor Inhibitor
Amosulalol is a dual inhibitor of the α1 and β1-adrenergic receptors, demonstrating significant antihypertensive activity. By selectively inhibiting the α1-adrenergic receptor, Amosulalol effectively reduces blood pressure, while its β1-adrenergic receptor blockade leads to decreased reflex-induced heart rate and plasma renin activity in spontaneously hypertensive rats. This compound is valuable for research applications focused on cardiovascular physiology and the pharmacological modulation of blood pressure. -
Stable Isotope
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. -
β1 Adrenergic Receptor Antagonist
Acebutolol is a selective β1 adrenergic receptor antagonist, primarily utilized in the study of cardiovascular conditions. It demonstrates significant antihypertensive and antiarrhythmic properties, making it suitable for research into hypertension, angina pectoris, and cardiac arrhythmias. This compound serves as an important tool in understanding the mechanisms underlying β1 adrenergic signaling in cardiac function. -
α1 AR Antagonist
Upidosin is an α-1 adrenergic receptor (α-1 AR) antagonist with moderate selectivity for the α-1A AR subtype. It demonstrates uroselectivity, exhibiting a Kb value of 2-3 nM in the urethra and prostate, compared to Kb values of 20-100 nM in the ear artery and aorta. Upidosin effectively inhibits [3H]prazosin binding to cloned human α-1A adrenergic receptors. This compound is a valuable tool for research focused on urethral obstruction and related conditions. -
Antiemetic
Benzquinamide hydrochloride targets the α2 adrenergic receptors (α2-AR), binding with Ki values of 1,365, 691, and 545 nM for the α2A, α2B, and α2C subtypes, respectively. As an antiemetic, it exhibits significant efficacy in preventing nausea and vomiting. Additionally, benzquinamide inhibits P-glycoprotein-mediated drug efflux, thereby enhancing the cytotoxic effects of anticancer agents in multidrug-resistant cell lines, making it a valuable tool in cancer research and therapeutic development. -
Adrenergic Receptor Modulator
Meranzin is an adrenergic receptor modulator derived from the Traditional Chinese Medicine Chaihu-Shugan-San (CSS), isolated from the leaves of Murraya exotica L. It primarily regulates the alpha 2-adrenoceptor and influences the AMPA-ERK1/2-BDNF signaling pathway. Meranzin exhibits potential beneficial effects in preventing the co-occurrence of atherosclerosis and depression, making it a valuable tool for research in neurovascular health and related disorders. -
Adrenergic receptor α2B Antagonist
BAY-6096 is a selective antagonist for the adrenergic receptor α2B, demonstrating a potent inhibitory effect with an IC50 of 14 nM. This compound is characterized by its high water solubility and has been shown to effectively reduce α2B receptor agonist-induced vascular contractions in rat models. BAY-6096 serves as a valuable tool for studying vascular physiology and the role of adrenergic receptors in cardiovascular research. -
β-adrenoceptor Antagonist
Carazolol hydrochloride is a potent β-adrenoceptor antagonist that primarily targets β1 and β2 adrenergic receptors. In addition to its antagonistic properties, it serves as a selective agonist for the β3-adrenoceptor. This compound is primarily utilized in research focused on hypertension and related cardiovascular studies, enabling investigations into β-adrenergic signaling pathways and therapeutic interventions. -
β1 Adrenergic Receptor Antagonist
(Rac)-Nebivolol is a racemic isomer of Nebivolol, a selective β1-adrenergic receptor antagonist with an IC50 value of 0.8 nM. This compound exhibits protective effects against ethanol-induced cardiac toxicity by inhibiting the up-regulation of Nox2/NADPH oxidase and reducing lipoperoxidation. Additionally, it demonstrates vasodilatory activity, making it valuable for research in cardiovascular pharmacology and related studies. -
β-adrenergic Blocker
Bunitrolol is an orally active β-adrenergic blocker with a strong affinity for β-adrenergic receptors. It exhibits significant β-receptor antagonist activity alongside weak α1-blocking effects. This compound is primarily utilized in research on cardiovascular disorders, including hypertension and angina pectoris, and has applications in studies related to placental transport mechanisms.

