Catalog No.
Product Name
Application
Product Information
Citations
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α2-adrenergic Agonist
Detomidine carboxylic acid is a primary urinary metabolite of Detomidine, functioning as an α2-adrenergic agonist. This compound exhibits significant biological activity by influencing cardiovascular and respiratory systems, as well as displaying an antidiuretic effect. It is useful in research applications focused on pharmacology and the investigation of adrenergic receptor mechanisms. -
Adrenergic Receptor
L-654284 is a selective α2-adrenergic receptor antagonist that effectively competes with the binding of radiolabeled 3H-clonidine and 3H-rauwolscine, exhibiting Ki values of 0.8 nM and 1.1 nM, respectively. This compound demonstrates the ability to block the effects of clonidine in isolated rat vas deferens, with a pA2 value of 9.1. Additionally, L-654284 shows notable selectivity towards α2 and α1 adrenergic receptors, with a Ki of 110 nM against 3H-prazosin binding. In vivo studies reveal that L-654284 enhances norepinephrine turnover in the rat cerebral cortex, highlighting its potential applications in research related to central nervous system pharmacology. -
α1A Adrenergic Receptor Antagonist
SNAP5089 hydrochloride is a selective antagonist of the α1A adrenergic receptor. This compound exhibits significant biological activity in the modulation of adrenergic signaling pathways. It is primarily utilized in research related to hypertension and benign prostatic hyperplasia, providing valuable insights into these conditions and their underlying mechanisms. -
Dopamine receptor/α-adrenergic receptor antagonist/antiperoxidant
Bulbocapnine is an aporphine isoquinoline alkaloid that acts as an antagonist at dopamine and α-adrenergic receptors, alongside possessing anti-peroxidative properties. This compound has been shown to reduce intracellular dopamine levels and inhibit tyrosine hydroxylase activity with a Ki value of 0.20 mM. Additionally, Bulbocapnine decreases intracellular Ca2+ concentration and mitigates the dose-dependent inhibitory effects of dopamine on heart rate acceleration, making it a valuable tool for research in cardiovascular physiology and neurobiology. -
Stable Isotope
(Rac)-Talinolol-d5 is a stable isotope of Talinolol, a long-acting, cardioselective β1-adrenergic receptor blocker. This compound demonstrates significant cardioprotective and antihypertensive properties. Additionally, Talinolol serves as a valuable probe substrate for investigating P-glycoprotein (P-gp) activity in pharmacokinetic studies. -
Stable Isotope
Isoprenaline-d7 hydrochloride is a deuterated analog of Isoprenaline, serving as a stable isotope for research applications. As a non-selective β-adrenergic receptor agonist, Isoprenaline exhibits significant peripheral vasodilatory, bronchodilator, and cardiac stimulatory effects. This compound is valuable for studying conditions such as bradycardia and bronchial asthma, providing insights into β-adrenergic signaling pathways and related therapeutic interventions. -
D2 dopamine receptor and β2-adrenocepto agonist
Sibenadet hydrochloride is a dual agonist of the D2 dopamine receptor and the β2-adrenoceptor. It exhibits significant bronchodilator activity and has been shown to effectively inhibit sensory nerve activity in animal models of chronic obstructive pulmonary disease (COPD). Research indicates that Sibenadet hydrochloride reduces reflex cough, mucus production, and tachypnoea, making it a valuable tool for studying respiratory disorders and potential therapeutic interventions. -
β3-Adrenergic Receptor Agonist
LY-377604 hydrochloride is a potent agonist of the human β3-adrenergic receptor, with an EC50 value of 2.4 nM. In addition to its agonistic properties, it functions as an antagonist at the β1- and β2-adrenergic receptors. This compound is primarily utilized in research focused on metabolic disorders, obesity, and cardiovascular disease, providing insights into β-adrenergic signaling pathways. -
Stable Isotope
4-Hydroxypropranolol-d7 is a deuterium-labeled derivative of the active metabolite 4-Hydroxypropranolol hydrochloride, which targets β1- and β2-adrenergic receptors with high affinity, exhibiting pA2 values of 8.24 and 8.26, respectively. This compound maintains comparable potency to Propranolol and displays intrinsic sympathomimetic activity, membrane-stabilizing properties, and potent antioxidant effects. 4-Hydroxypropranolol-d7 is instrumental for pharmacokinetic studies, providing valuable insights into drug metabolism and receptor activity in various biological assays. -
Adrenergic Receptor Stimulator
Butopamine is a selective stimulant of β1-adrenergic and β2-adrenergic receptors, exerting its biological effects primarily in skeletal muscle and adipose tissue. This compound is notable for its role in enhancing muscle growth and altering fat metabolism, making it a valuable tool in research related to anabolic processes and energy expenditure. Its unique mechanism of action provides insights into adrenergic signaling pathways and their implications in metabolic disorders and muscle physiology. -
Adrenergic Receptor Agonist
DL-Methyldopa is a centrally acting α2-adrenergic receptor agonist, primarily involved in the modulation of neurotransmitter biosynthesis. It exhibits significant biological activity by influencing adrenergic signaling pathways, making it relevant for studies in neurological diseases. This compound serves as a valuable tool in research aimed at understanding and treating conditions related to adrenergic dysfunction. -
β1 Adrenergic Receptor Antagonist
Acebutolol-d7 is a deuterium-labeled form of Acebutolol, a selective β1 adrenergic receptor antagonist. This compound exhibits key biological activity by inhibiting β1 adrenergic receptors, leading to potential therapeutic effects in conditions such as hypertension, angina pectoris, and cardiac arrhythmias. Acebutolol-d7 is valuable for research applications involving pharmacokinetics and metabolic studies of β1 adrenergic signaling pathways. -
α1-Adrenergic Receptor Antagonist
Quinazosin dihydrochloride is an α1-adrenergic receptor antagonist primarily utilized in hypertension management. Its mechanism of action includes the inhibition of granulopoiesis, leading to effects such as neutropenia and leukopenia. Additionally, Quinazosin dihydrochloride demonstrates dose-dependent myelosuppression connected to the duration of exposure, making it valuable for research on hematologic effects and cardiovascular therapies. -
β2AR Negative Allosteric Modulator
AP-7-168 is a β-arrestin-biased negative allosteric modulator of the β2-adrenergic receptor (β2AR). It functions by promoting β2AR homodimerization and inhibiting GRK5-mediated phosphorylation, thereby sustaining bronchorelaxation in both cell and tissue models. This compound is particularly valuable for research in inflammation and immunology, including studies related to asthma and other respiratory conditions. -
α2-Adrenergic Receptor Agonist
Lidamidine is an α2-adrenergic receptor agonist known for its therapeutic potential as an antidiarrheal agent. By selectively activating α2-adrenergic receptors, it modulates neurotransmitter release, thereby impacting gastrointestinal motility. Lidamidine's biological activity makes it a valuable tool for research in neuromodulation and gastrointestinal disorders. -
Adrenergic Receptor Agonist
L-Mabuterol hydrochloride is a selective β2-adrenergic receptor agonist that displays significant bronchodilator activity. It is effective in enhancing respiratory function and alleviating symptoms associated with asthma. Additionally, L-Mabuterol hydrochloride demonstrates potential utility in the management of chronic obstructive pulmonary disease (COPD), making it valuable for research in respiratory disorders. -
β2-Adrenergic Receptor Agonist
Bedoradrine sulfate is a highly selective β2-adrenergic receptor agonist that effectively relieves airway spasms and dilates airway smooth muscle cells. By reducing airway inflammation, it enhances respiratory function, making it a valuable tool in respiratory research. Bedoradrine sulfate is particularly relevant for studies focused on asthma and related respiratory conditions. -
β3-Adrenergic Agonist
ZD-7114 is a potent and selective agonist of the β3-adrenergic receptor. This compound has been identified as a selective thermogenic agent, making it valuable for research in metabolic regulation. ZD-7114 is particularly useful in studies related to obesity and diabetes, providing insights into potential therapeutic approaches for these conditions. -
Adrenergic Receptor
S(-)-Bisoprolol fumarate is a selective β1-adrenergic receptor blocker, functioning primarily through antagonism of this target. This potent, orally active compound exhibits minimal β2-receptor activity, making it suitable for research applications related to hypertension, coronary artery disease, and stable ventricular dysfunction. Its unique pharmacological profile allows for in-depth exploration of β1-mediated cardiovascular effects in experimental studies. -
Adrenergic Receptor
O-Desmethyl Mebeverine alcohol is a metabolite of Mebeverine, primarily targeting the α1-adrenergic receptor. This compound exhibits significant biological activity by promoting the relaxation of the gastrointestinal tract, making it valuable in research related to gastrointestinal disorders and adrenergic signaling pathways. Its role as an inhibitor can support studies focused on gastrointestinal motility and related pharmacological effects. -
Dopamine Receptor Antagonist
Mafoprazine is a phenylpiperazine derivative that functions as a dopamine receptor antagonist, primarily targeting the D2 receptor. Its antipsychotic effects are thought to arise from its blockade of dopaminergic transmission, combined with α-adrenergic activity. Additionally, Mafoprazine may enhance the activity of dopamine metabolites, making it a valuable tool for research into the mechanisms underlying psychotic disorders and dopamine-related pathways. -
Stable Isotope
Ractopamine-d6 hydrochloride is a deuterium-labeled derivative of Ractopamine, a potent β-adrenergic receptor (βAR) agonist, exhibiting binding affinities of approximately 25 nM for both pig β1AR and β2AR. This stable isotope compound is primarily utilized in research focused on protein metabolism, particularly in enhancing lean tissue growth and improving production efficiency in swine. Its applications extend to studies investigating the physiological effects and benefits of βAR modulation in livestock management. -
β-Adrenergic Receptor Antagonist
Bucumolol hydrochloride is a β-adrenergic receptor antagonist that functions primarily by decreasing heart rate (negative chronotropic effect) and diminishing cardiac contractility (negative inotropic effect). This compound exhibits antiarrhythmic and local anesthetic properties, making it valuable in investigations of cardiovascular diseases and related pathophysiological conditions. -
Alpha-Adrenergic Agonist
Tetrahydrozoline nitrate, an α-adrenergic agonist, primarily targets adrenergic receptors to induce vasoconstriction. This compound is utilized extensively in research related to nasal and conjunctival congestion, providing insight into the mechanisms underlying these conditions. Its pharmacological profile makes it valuable for studies investigating vascular responses and the modulation of local blood flow. -
α1A Receptor Antagonist
KRG-3332 hydrochloride is a selective antagonist of the α1A adrenergic receptor. This compound demonstrates significant activity in modulating receptor signaling, making it a valuable tool for research into therapeutic interventions for glaucoma. Its specificity for the α1A receptor highlights its potential for studying mechanisms underlying ocular hypertension and related conditions. -
Adrenergic Receptor
SNAP5089 is a selective α1A-adrenoceptor antagonist, exhibiting over 1700-fold selectivity for the α1A subtype. This compound demonstrates significant receptor affinity, making it a valuable tool in research focused on hypertension and benign prostatic hypertrophy. The high selectivity of SNAP5089 positions it as a promising candidate for studies requiring precise modulation of the α1A receptor in various therapeutic contexts. -
Stable Isotope
Colterol hydrochloride-d9 is a deuterium-labeled derivative of Colterol hydrochloride, a selective agonist for adrenergic receptors. It demonstrates significant binding affinity for both the β1-adrenoreceptor, with an IC50 of 645 nM, and the β2-adrenoreceptor, with an IC50 of 147 nM. This compound is primarily utilized in research focusing on adrenergic signaling and has potential applications as a bronchodilator in respiratory studies. -
Nebivolol Metabolite
4-Hydroxy nebivolol hydrochloride is a hydroxylated metabolite of Nebivolol, primarily acting as a selective β-blocker. This compound exhibits significant vasodilatory properties and modulates cardiovascular function. It is utilized in research applications related to hypertension and heart failure, providing insight into β-adrenergic receptor signaling and its therapeutic implications. -
Adrenergic Receptor
S(-)-Bisoprolol is a selective β1-adrenergic receptor blocker, primarily inhibiting the activity of β1-receptors while exhibiting minimal effects on β2-receptors. This compound demonstrates significant efficacy in reducing heart rate and myocardial contractility, making it a valuable tool in studying cardiovascular conditions such as hypertension, coronary artery disease, and stable ventricular dysfunction. Its orally active nature allows for convenient administration in various research applications focused on cardiac health. -
Adrenergic Receptor Inhibitor
(+)-Amosulalol is an adrenergic receptor inhibitor that serves as an orally active dual blocker of α1 and β1-adrenergic receptors. This compound demonstrates significant antihypertensive activity by selectively inhibiting α1-adrenergic receptors, while also reducing reflex tachycardia and plasma renin activity in spontaneously hypertensive rats through β1-adrenergic receptor inhibition. As a valuable research tool, (+)-Amosulalol can be employed in studies related to cardiovascular physiology and pharmacology. -
Adrenergic Receptor
LY87130 free base is an inhibitor of octopamine-N-methyltransferase, targeting adrenergic receptors to modulate epinephrine levels. This compound exhibits significant reduction of basal epinephrine levels in the hypothalamus following administration, while not affecting the levels of norepinephrine, 3,4-dihydroxyphenylacetic acid (DOPAC), or 5-hydroxyindoleacetic acid (5-HIAA). LY87130 free base is valuable for research focused on adrenergic signaling and the neurochemical regulation of stress responses. -
Adrenergic Receptor Antagonist
Ronactolol is a selective adrenergic receptor antagonist primarily targeting β-adrenoceptors. It exhibits notable β-blocking activity, making it valuable for research focused on cardiovascular pharmacology and the modulation of sympathetic nervous system responses. This compound is suitable for studying the effects of β-adrenoceptor inhibition in various physiological and pathological conditions. -
β2-adrenergic Receptor Agonist
Rimiterol is a selective β2-adrenergic receptor agonist that activates adenylate cyclase, leading to an increase in intracellular cyclic AMP (cAMP) levels. This mechanism results in the relaxation of smooth muscle, making Rimiterol valuable for studying bronchial dilation. Its application is particularly relevant in research focused on asthma and other respiratory conditions. -
Adrenergic Receptor Agonist
(S)-Mabuterol is a selective β2 adrenergic receptor agonist that modulates cardiovascular responses by lowering blood pressure while enhancing heart rate and contractile force. This compound is of interest in research applications focused on studying adrenergic signaling pathways and cardiovascular function in preclinical models. Its unique properties make it a valuable tool for investigating the therapeutic potential in conditions related to heart function and blood pressure regulation. -
β2 Receptor Agonist
Procaterol is a selective β2 adrenergic receptor agonist that primarily enhances bronchodilation. It inhibits eosinophil migration and the release of eosinophil chemotactic factors from BEAS-2B cells via a cyclic AMP-dependent pathway. Due to its distinct dose-response relationship between bronchodilator and anabolic effects in animal models, Procaterol is valuable for research applications focused on asthma and exercise physiology. -
Adrenergic Receptor
Phendioxan is a selective adrenergic receptor ligand with a high binding affinity for the α(1)-adrenaline receptor subtype. Its facilitated membrane diffusion enhances its efficacy at the α(1d)-AR, supporting its potential in cardiovascular and neuropharmacological research. Docking simulations have elucidated the significant roles of polar, electrostatic, hydrophobic, and shape interactions of its phenoxy terminal substituents in ligand-receptor binding dynamics. -
β2AR/M3-Receptor Agonist
β2AR/M3-receptor agonist-1 is a potent agonist for both the β2 adrenergic receptor (β2AR) and the M3 muscarinic receptor. It exhibits high affinity for the M3 receptor, with a pIC50 value of 9.3. This compound is valuable for research focused on respiratory tract disorders, enabling studies on receptor interactions and their implications in respiratory physiology and pathology. -
Propranolol Metabolite
(±)-Desisopropylpropranolol serves as a metabolite of Propranolol, a nonselective β-adrenergic receptor antagonist that demonstrates high binding affinity for β1AR and β2AR with inhibition constants (Kis) of 1.8 nM and 0.8 nM, respectively. This compound effectively inhibits [3H]-DHA binding to rat brain membrane preparations with an IC50 of 12 nM. Research applications include investigations into cardiovascular conditions such as hypertension, myocardial infarction, cardiac arrhythmias, and angina pectoris, as well as studying mechanisms relevant to pheochromocytoma and hypertrophic cardiomyopathy. -
β-adrenergic Receptor Blocker
(S)-Bopindolol is a selective β-adrenergic receptor blocker that serves to mitigate muscle wasting, functional decline, and reduced bone density often associated with weight loss. This compound is particularly relevant in protecting myocardial integrity and cardiac function, as it aids in preventing excessive drops in blood pressure and increases in heart rate during periods of weight reduction. Its application spans various research areas, including cardiovascular health and metabolism. -
α₂B Adrenergic Receptor Antagonist
BRL-41992 is a selective antagonist of the α₂B-adrenergic receptor, demonstrating 94-fold greater selectivity for this subtype compared to the α₂A-receptor. It exhibits Kᵢ values of 1.1 nM in neonatal rat lung tissue, where the α₂B-receptor is expressed, and 103.3 nM in human platelet membranes, which express the α₂A-receptor. This compound is valuable for studying the functional differences between α₂ receptor subtypes in various biological contexts. -
β-AR Ligand
CGP 12177 is a selective β-Adrenergic receptor (β-AR) ligand that primarily acts as a β3-AR agonist (Ki = 88 nM) while displaying antagonist activity at β1 (Ki = 0.9 nM) and β2-AR (Ki = 4 nM). Additionally, it demonstrates partial agonist characteristics for α1-AR in rat pulmonary artery tissues. This compound is relevant for research investigating the regulation of metabolic pathways, particularly the expression of ucp and leptin genes in adipose tissues, and holds potential applications in cardiovascular and metabolic disease studies. -
Stable Isotope
Carazolol-d7 is a stable isotope form of Carazolol, a highly potent antagonist of β1 and β2 adrenoceptors. Additionally, Carazolol acts as a selective agonist for the β3-adrenoceptor, making it a valuable compound in studies of adrenergic receptor pharmacology. This reagent is particularly useful in hypertension research, enabling researchers to explore mechanisms of action and receptor interactions in cardiovascular studies. -
Adrenergic Receptor Antagonist
BE2254 is an adrenergic receptor antagonist that exhibits antipyretic and metabolic activity. It effectively modulates the febrile response and metabolism, as demonstrated by its ability to reduce lipopolysaccharide-induced metabolic and febrile activities in febrile rabbits. This compound may regulate body temperature through its action on the α1-adrenergic receptor, making it a valuable tool for research in fever regulation and metabolic processes. -
β-adrenergic Receptor Antagonist
(±)-Penbutolol is a racemic mixture functioning as a β-adrenergic receptor antagonist. It is known to mitigate exercise-induced tachycardia, reduce the exercise-related increase in peak expiratory flow rate (PEFR), and lower resting plasma renin activity (PRA). With a peak plasma concentration achieved one hour after oral administration and a half-life of 4.5 hours, (±)-Penbutolol also converts into an active metabolite. This compound is valuable for research in cardiovascular diseases and related physiological studies. -
β-adrenergic Receptor Antagonist
Esprolol hydrochloride is a selective β-adrenergic receptor antagonist that demonstrates oral bioactivity. It undergoes rapid metabolic conversion by blood and tissue esterases to yield the active metabolite amoxolol. This compound is of interest for studies related to exertional angina and cardiovascular function, making it a valuable tool for research in cardiac pharmacology. -
mAChR/Adrenergic Receptor Antagonist
Muscarinic toxin 3 (MT3) is a selective and non-competitive antagonist of muscarinic acetylcholine receptors (mAChRs) and adrenergic receptors. It exhibits high potency with pIC50 values of 6.71, 8.79, 8.86, 7.57, 8.13, and 8.49 against M1, M4, α1A, α1B, α1D, α2A, α2B, and α2C receptors, respectively, highlighting its prominent adrenoceptor activity. This compound is valuable in studying receptor signaling pathways and has potential applications in pharmacological research focused on nervous system disorders and cardiovascular diseases. -
Adrenergic Receptor Inhibitor
Besipirdine is an adrenergic receptor inhibitor that exhibits non-receptor-dependent cholinomimetic properties. This compound is known to inhibit voltage-dependent sodium and potassium channels, contributing to its pharmacological profile. Besipirdine's biological activity makes it relevant for research applications focused on neuropharmacology and the modulation of synaptic transmission. -
Adrenergic Receptor Antagonist
Dicentrine hydrochloride is an adrenergic receptor antagonist known for its anti-inflammatory and anti-cancer properties. It enhances TNF-α-induced apoptosis in A549 lung adenocarcinoma cells by increasing the activities of key apoptotic markers, including caspase-8, -9, -3, and poly(ADP-ribose) polymerase (PARP). Additionally, Dicentrine hydrochloride inhibits TNF-α-induced invasion and migration of A549 cells by downregulating the TAK1, p38, JNK, and Akt signaling pathways, as well as reducing NF-κB and AP-1 transcriptional activities. This compound is valuable for research in cancer biology and therapeutic development. -
Stable Isotope
Ractopamine-13C2 is a stable isotope-labeled version of Ractopamine, a potent β-adrenergic receptor agonist. With a Kd of approximately 25 nM for both pig β1 and β2 adrenergic receptors, Ractopamine is also an mTAAR1 agonist characterized by an EC50 of 16 μM. This compound enhances muscle mass development while minimizing fat deposition, resulting in improved growth rates and feed efficiency in swine. Ractopamine-13C2 is ideal for research focused on optimizing lean tissue growth and production efficiency in livestock. -
Adrenergic Receptor Antagonist
Naftopidil hydrochloride is a selective alpha-1 adrenergic receptor antagonist, exhibiting potent inhibition with Ki values of 3.7 nM, 20 nM, and 1.2 nM for the human α1a, α1b, and α1d adrenoceptor subtypes, respectively. It demonstrates antiproliferative effects, making it valuable in the study of conditions such as prostate hyperplasia. This compound is suitable for research applications involving adrenergic signaling and therapeutic strategies targeting prostate-related disorders.
