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β3 Adrenergic Receptor Agonist
L-770644 dihydrochloride is a potent and selective agonist of the human β3 adrenergic receptor, with an EC50 value of 13 nM. This compound is primarily utilized in research applications exploring metabolic regulation, adipocyte function, and energy expenditure. Its oral bioactivity makes it a valuable tool for studying β3 adrenergic receptor-mediated pathways in various biological contexts. -
β3-Adrenergic Agonist
Trecadrine is a potent β3-adrenergic agonist that selectively activates β3-adrenergic receptors. This compound is known for its role in promoting lipolysis and thermogenesis, making it a valuable tool in metabolic research. Trecadrine is commonly utilized in studies examining obesity, energy expenditure, and the physiological roles of β3-adrenergic signaling pathways. -
Adrenergic Receptor Agonist
β3-AR agonist 2 is a selective agonist of the β3-adrenergic receptor, exhibiting high potency with an EC50 of 8 nM. This compound is instrumental in various research applications, particularly in studies related to metabolic regulation, thermogenesis, and obesity. Its ability to selectively activate β3-AR makes it a valuable tool for exploring adipocyte function and potential therapeutic pathways for metabolic disorders. -
Adrenergic Receptor Modulator
α1 adrenoceptor-MO-1 is an S enantiomer that selectively targets the alpha-1 adrenergic receptor. This compound exhibits alpha-lytic activity and demonstrates analgesic properties, making it more effective than its R enantiomer counterpart. α1 adrenoceptor-MO-1 is suitable for research applications focused on adrenergic signaling and pain modulation. -
Adrenergic Receptor Modulator
D2343 is a β2-adrenoceptor agonist and α1-adrenoceptor inhibitor. This compound exhibits a dual mechanism of action, enhancing β2 receptor activation while simultaneously blocking α1 receptors. It is utilized in research applications that investigate adrenergic signaling pathways and the physiological effects mediated by these receptors. -
Adrenergic Receptor Agonist
Epanolol is a selective β-adrenoceptor partial agonist, demonstrating a higher affinity for β1-adrenoceptors compared to β2-adrenoceptors. This compound exhibits significant cardiovascular effects, making it useful in research focused on heart-related therapies and the modulation of adrenergic signaling pathways. Its specificity for β1-adrenergic receptors lends valuable insight into cardiac function and potential treatments for hypertension and other cardiovascular diseases. -
Adrenergic Receptor Antagonist
Fiduxosin is a potent α1-adrenoceptor antagonist, exhibiting Ki values of 0.160 nM, 24.9 nM, and 0.920 nM for the α1a, α1b, and α1d subtypes, respectively. This compound inhibits adrenergic signaling, making it a valuable tool in the study of cardiovascular and urological diseases. Its selective modulation of α1-adrenoceptors allows for targeted research applications in pharmacology and drug development. -
Adrenergic Receptor Antagonist
MG 1 is a selective α1 adrenergic receptor antagonist, primarily designed to inhibit the activity of these receptors. This compound demonstrates significant biological activity in modulating vascular smooth muscle contraction and has applications in studying cardiovascular function and related signal transduction pathways. MG 1 is valuable for researchers investigating the roles of adrenergic signaling in various physiological and pathological conditions. -
Adrenergic Receptor Inhibitor
Tropodifene is an α-adrenergic receptor inhibitor that modulates adrenergic signaling pathways. It is primarily utilized in research related to cardiovascular pharmacology and the study of sympathetic nervous system functions. Its unique mechanism of action makes it valuable for investigating the role of adrenergic receptors in various physiological and pathological conditions. -
Adrenergic Receptor Inhibitor
Benzquinamide is an adrenergic receptor inhibitor that selectively binds to the α2A, α2B, and α2C adrenergic receptors, exhibiting Ki values of 1,365, 691, and 545 nM, respectively. This compound demonstrates antiemetic properties and is utilized in research applications relating to nausea and vomiting. Its mechanism of action involves modulation of adrenergic signaling pathways, making it a valuable tool for studying the role of adrenergic receptors in various physiological and pathological conditions. -
Adrenergic Receptor
GP2-114 is a selective adrenergic receptor modulator that exhibits current-dependent cardiovascular effects. It is utilized in experimental models to study the physiological impacts on cardiovascular function and adrenergic signaling pathways. The compound offers valuable insights into the role of adrenergic receptors in cardiovascular responses, supporting various research applications in pharmacology and cardiovascular physiology. -
Adrenergic Receptor Agonist
ZK-90055 hydrochloride is a selective β2 adrenergic receptor agonist known for its ability to activate β2 receptors, influencing various physiological responses. This compound is primarily utilized in cardiovascular research and studies related to asthma and bronchial dilation. Its potent agonistic effects on β2 receptors make it a valuable tool for investigating adrenergic signaling pathways and developing therapeutic interventions for related disorders. -
Adrenergic Receptor Antagonist
Fenmetozole Tosylate is an adrenergic receptor antagonist primarily targeting the α2-adrenergic receptor. This compound has been shown to counteract the actions of ethanol and exhibits potential antidepressant properties. It is useful in research applications focused on understanding the mechanisms of alcohol-related effects and the modulation of mood disorders. -
Adrenergic Receptor Agonist
AR-08 is an agonist of the α2-adrenergic receptor, primarily involved in modulating neurotransmitter release and synaptic transmission. This compound exhibits key biological activity in the central nervous system, making it relevant for research into disorders such as attention deficit hyperactivity disorder (ADHD). AR-08 can be utilized to explore adrenergic signaling pathways and assess therapeutic potential in neuropsychiatric applications. -
Adrenergic Receptor Antagonist
Bometolol Hydrochloride is a selective beta-adrenergic receptor antagonist primarily targeting β1-adrenergic receptors. With its capacity to inhibit adrenergic signaling, it is employed in research focused on cardiovascular diseases, particularly in studies investigating heart rate regulation and blood pressure modulation. This compound provides valuable insights into the mechanisms underlying cardiac function and the therapeutic potential for hypertension and related disorders. -
Adrenergic Receptor Antagonist
Falintolol, (Z)- is a selective β-adrenergic receptor antagonist known for its unique oxime functionality. This compound exhibits key biological activity by blocking β-adrenergic signaling pathways, making it valuable for studies in cardiovascular research and the regulation of metabolic processes. Its ability to interact with adrenergic receptors provides insights into the pharmacological modulation of various physiological responses. -
Adrenergic Receptor Antagonist
Phentolamine Analogue 1 is a nonselective alpha-adrenergic receptor antagonist. This compound demonstrates significant inhibitory activity against adrenergic signaling pathways, making it a valuable tool for studying cardiovascular regulation and neuropharmacology. Its application in research may include investigations into blood pressure modulation, vasodilation mechanisms, and the effects of adrenergic receptor blockade in various biological systems. -
Antiarrhythmic Compounds
BW A256C is an antiarrhythmic compound that acts as both an angiotensin-converting enzyme inhibitor and a beta-adrenergic receptor blocker. This dual action contributes to its effectiveness in modulating cardiovascular responses and stabilizing cardiac rhythm. BW A256C serves as a valuable tool for research focused on cardiac arrhythmias and related cardiovascular conditions. -
Adenylate Cyclase Inhibitor
KUM 32 is a potent inhibitor of adenylate cyclase that functions by antagonizing epinephrine-induced platelet aggregation. By selectively binding to the alpha-2 adrenergic receptor on human platelets, KUM 32 modulates platelet activation and aggregation pathways. This compound is utilized in research focused on cardiovascular disease and hemostasis, providing insights into the mechanisms of platelet function. -
Adrenergic Receptor Agonist
Phenylephrine is a selective α1-adrenoceptor agonist that primarily functions as a decongestant. It exerts its biological activity by inducing vasoconstriction, leading to decreased nasal congestion. This compound is widely utilized in research applications related to cardiovascular studies, nasal physiology, and adrenergic receptor signaling pathways. -
Analgesic
α2AR agonist 2 is a selective agonist for the α2B adrenergic receptor, demonstrating an IC50 of 1.2 µM. This compound is primarily utilized in research focused on analgesic effects, particularly in the contexts of inflammatory and neuropathic pain. Its selective action makes it a valuable tool for studying pain modulation pathways and developing novel therapeutic strategies. -
β-Adrenoceptor Agonist
(-)-Isoproterenol hydrochloride is a potent β-adrenoceptor agonist. It primarily acts on β1 and β2 adrenergic receptors, resulting in increased heart rate and myocardial contractility. This compound is widely used in research related to cardiac function and ventricular remodeling, making it essential for studies exploring cardiovascular physiology and related therapeutic interventions. -
β3-AR Antagonist
SR59230A is a potent and selective antagonist of the β3-adrenergic receptor, demonstrating IC50 values of 40 nM, 408 nM, and 648 nM for β3, β1, and β2 receptors, respectively. Its ability to penetrate the blood-brain barrier makes it a valuable tool for exploring the physiological roles of β3-AR in the central nervous system. This compound is primarily utilized in research related to metabolic disorders, obesity, and cardiovascular diseases, providing insight into the therapeutic potential of β3-AR modulation. -
α1/β-adrenergic Receptors Antagonist
Labetalol is a competitive antagonist of α1-adrenergic and non-selective β-adrenergic receptors. This antihypertensive agent is orally bioavailable and effectively addresses hypertension by reducing peripheral vascular resistance with minimal impact on cardiac output. Labetalol is particularly relevant for research on cardiovascular diseases, including hypertension during pregnancy, and its ability to partially traverse the blood-brain barrier also makes it a candidate for neurological studies of vascular conditions. -
β3 Adrenergic Receptor Antagonist
L748337 is a selective β3-adrenergic receptor antagonist with a high affinity for the β3 receptor (Ki = 4.0 nM) compared to β1 (Ki = 390 nM) and β2 receptors (Ki = 204 nM). This compound predominantly couples to Gi proteins, leading to the activation of MAPK signaling pathways, which subsequently enhances the phosphorylation of Erk1/2 with a pEC50 value of 11.6. L748337 is applicable in research focused on cancer, nonalcoholic fatty liver disease (NAFLD), and various cardiovascular disorders. -
β2-Adrenergic Receptor Blocker
Butaxamine hydrochloride is a specific antagonist of the β2-adrenergic receptor. This compound effectively inhibits the reduction of urine volume in ethanol-anesthetized, water-diuretic rats, demonstrating its role in regulating diuresis. Butaxamine hydrochloride is valuable for studying β2-adrenergic receptor signaling and its implications in renal function and fluid regulation. -
β/α-1 Blocker
(S)-Carvedilol is a non-selective β/α-1 blocker that primarily targets adrenergic receptors. This compound demonstrates protective effects against the vascular and cardiac toxicity induced by Doxorubicin (DOX). It is utilized in research related to cardioprotection and the mitigation of chemotherapy-related side effects. -
α Blocker
(R)-Carvedilol primarily targets alpha (α) adrenergic receptors, acting as an α-blocker while exhibiting no β-receptor activity. This compound is noted for its ability to inhibit spontaneous Ca2+ waves, thereby contributing to its cardioprotective effects. Research applications for (R)-Carvedilol include the study of stress-induced ventricular tachycardia and the potential inhibition of UV-induced skin tumor development, suggesting its utility in cancer research and cardiovascular studies. -
α2A Agonist
Guanfacine functions as a selective α2A adrenergic receptor agonist, exhibiting potent noradrenergic activity. Its mechanism leads to reduced sympathetic outflow, resulting in hypotension and sedation. Guanfacine is utilized in research related to prefrontal cortex cognitive disorders, including Tourette’s syndrome and attention deficit hyperactivity disorder (ADHD), making it valuable for understanding the pharmacological modulation of these conditions. -
β1-AR Agonist
Dobutamine is a synthetic catecholamine that acts primarily as a selective agonist of the β1-adrenergic receptor (β1-AR). It is known to enhance cardiac output and improve conditions of hypoperfusion by elevating heart rate and contractility. Dobutamine is utilized in various research applications, including studies on cardiac function, mechanisms of heart failure, and other cardiovascular disorders. -
Adrenergic Receptor Agonist
Xamoterol hemifumarate is a selective and potent agonist of the beta-1 adrenergic receptor. It has significant potential for studying arrhythmogenesis and elucidating the relationship between β1-adrenergic stimulation and the potassium ion channel IKr. This compound is valuable for research applications focused on cardiac function and the mechanisms underlying arrhythmic conditions. -
β-adrenergic Antagonist
Pronethalol is a non-selective β-adrenergic antagonist that effectively inhibits β-adrenergic receptor activity. It has been shown to potently inhibit Sox2 expression and demonstrates protective effects against digitalis-induced ventricular arrhythmias. Additionally, Pronethalol limits the formation of cerebral arteriovenous malformations (AVMs), making it a valuable reagent for research into cardiovascular and neurological conditions. -
Adrenergic Receptor Agonist
A-61603 is a selective α1A-adrenergic receptor agonist that enhances adrenergic signaling. This compound increases the frequency of spontaneous calcium (Ca2+) transients in rat ventricular myocytes in vitro, indicating its potential role in cardiac research. A-61603 is valuable for studies investigating adrenergic receptor functions and cardiovascular physiology. -
β-AR Modulator
Lubabegron is a potent modulator of β-adrenergic receptors (β-AR). It exhibits antagonistic activity at the β1 and β2 receptor subtypes while acting as an agonist for the β3 receptor subtype in cattle. This compound is effective in reducing ammonia gas emissions from livestock and their waste, making it relevant for environmental and agricultural research applications. Lubabegron holds potential for studies focusing on animal physiology and sustainable farming practices. -
α-adrenoceptors Agonist
Levonordefrin is an α-adrenergic receptor agonist known for its role in blood pressure regulation. This compound exerts hypotensive effects through the stimulation of central α-adrenergic receptors in the nucleus tractus solitarius of the medulla oblongata, leading to centrally mediated hypotension and bradycardia. When administered intravenously, Levonordefrin demonstrates a dose-dependent increase in mean arterial blood pressure. This reagent is particularly useful for investigating the pathophysiology of hypertension and studying drug metabolism. -
Stable Isotope
Atenolol-d7 is a deuterium-labeled variant of Atenolol, a cardioselective β1-adrenergic receptor blocker that exhibits a Ki value of 697 nM at the β1-adrenoceptor in guinea pig left ventricle membranes. This stable isotope is instrumental in pharmacokinetic studies and metabolic research related to hypertension and angina pectoris. Its unique properties facilitate the investigation of drug metabolism and disposition in biological systems. -
Adrenergic Receptor Antagonist
Vatinoxan hydrochloride is a selective peripheral α2 adrenergic receptor antagonist. It demonstrates significant biological activity in modulating adrenergic signaling pathways and has been widely utilized in research exploring the effects of α2 receptor inhibition on cardiovascular function and neuropharmacology. This compound serves as a valuable tool for studies aimed at understanding the therapeutic potential of adrenergic modulation in various disease models. -
Gαi Inhibitor
0990CL is a selective inhibitor of the heterotrimeric Gαi subunit, functioning through direct interaction with Gαi. This compound effectively inhibits α2 adrenergic receptor-mediated regulation of cyclic AMP (cAMP), making it a valuable tool for studying Gαi signaling pathways. It is particularly useful in research related to neurotransmission and cardiovascular physiology, aiding in the exploration of GPCR-mediated processes. -
Alpha-Adrenergic Agonist
Norfenefrine hydrochloride is an orally active alpha-adrenergic agonist that primarily targets adrenergic receptors. It is utilized in research to investigate mechanisms underlying female stress incontinence and to explore therapeutic strategies for managing this condition. Its role as an endogenous compound also contributes to studies of adrenergic signaling pathways. -
β-adrenergic Receptor Antagonist
Metipranolol is a nonselective β-adrenergic receptor antagonist that exerts its effects primarily through the inhibition of β-receptor signaling. It has demonstrated efficacy in modulating cardiovascular function and intraocular pressure, making it valuable for research related to hypertension and glaucoma. This compound serves as a key tool for studying adrenergic pharmacology and its implications in various physiological and pathological conditions. -
β3-Adrenergic Receptor Agonist
BRL-37344 is a selective β3-adrenergic receptor agonist known for its role in modulating metabolic processes. It has been demonstrated to significantly reduce body weight in obese mouse models, highlighting its potential in obesity research and metabolic disorders. This compound serves as a valuable tool for investigating the therapeutic effects of β3-adrenergic activation in various preclinical studies. -
β-adrenoceptor Agonist
Isoprenaline is a non-selective β-adrenergic receptor agonist known for its potent peripheral vasodilator, bronchodilator, and cardiac stimulating effects. This compound is utilized extensively in research focused on conditions such as bradycardia and bronchial asthma, providing valuable insights into cardiovascular and respiratory therapeutic strategies. Isoprenaline’s diverse biological activity makes it a critical tool for understanding β-adrenoceptor modulation in various physiological and pathological contexts. -
Alkaloid
Aposcopolamine is an alkaloid isolated from Datura ferox, known for its ability to bind closely with acetylcholinesterase (ACHE), adrenergic receptor alpha-2A (ADRA2A), and muscarinic receptor subtype 2 (CHRM2). This compound is of significant interest in Alzheimer's disease research due to its potential effects on cholinergic signaling pathways. Aposcopolamine serves as a valuable tool in investigating neurodegenerative mechanisms and developing therapeutic strategies. -
β2 Agonist
Salmeterol-d3 is a deuterated form of Salmeterol, acting as a selective agonist for the human β2 adrenergic receptor. This compound effectively stimulates cyclic AMP (cAMP) accumulation in Chinese Hamster Ovary (CHO) cells expressing human β2 adrenergic receptors, demonstrating a pEC50 of 9.6, along with lower activity at β1 and β3 adrenergic receptors (pEC50 values of 6.1 and 5.9, respectively). Salmeterol-d3 is valuable for research applications focused on respiratory diseases, drug metabolism studies, and the pharmacological profiling of β2 agonists. -
Adrenergic Receptor
FFN270 hydrochloride is a fluorescent tracer that specifically targets adrenergic receptors, functioning as a substrate for norepinephrine and vesicular monoamine transporters. This compound displays distinct absorption and excitation maxima at either 320 nm or 365 nm depending on the solvent pH, with an emission wavelength of 475 nm. FFN270 hydrochloride is valuable in research applications that involve monitoring norepinephrine dynamics and can also serve as a ratiometric pH sensor for various biological studies. -
Adrenergic Receptor Agonist
Lofexidine hydrochloride is a selective α2-adrenergic receptor agonist, primarily utilized to mitigate the physical symptoms associated with opioid withdrawal, including heroin dependence. Its mechanism involves reducing norepinephrine release, thereby diminishing withdrawal-related discomfort. This compound is valuable in research focusing on addiction treatment and the physiological responses to opioid cessation. -
Adrenergic Receptor Agonist
Methyldopate is an ethyl ester proagent of α-Methyldopa, functioning primarily as an α-adrenergic receptor agonist with selectivity for α2-adrenergic receptors. This compound is of significant interest in the study of severe hypertension due to its potential to modulate adrenergic signaling pathways. Research applications include investigating the mechanisms of blood pressure regulation and the pharmacology of antihypertensive therapies. -
Adrenergic Receptor Antagonist
Medroxalol is an orally active adrenergic receptor antagonist that targets both α- and β-adrenergic receptors. This compound exhibits antihypertensive properties as well as vasodilatory effects, making it valuable in studies related to cardiovascular health. Its mechanism of action and biological activity are significant for researching hypertension and related cardiovascular conditions. -
Adrenergic Receptor Antagonist
(±)-N-Methylcoclaurine is a selective α2-adrenoceptor antagonist. This compound demonstrates potential to modulate adrenergic signaling pathways, making it a valuable tool in studies of cardiovascular function and neurobiology. Its ability to inhibit α2-adrenergic receptors positions it as a candidate for investigating therapeutic strategies in conditions related to adrenergic dysregulation. -
Adrenergic Receptor Agonist
Dopexamine hydrochloride is a selective β2 adrenergic receptor agonist. It exhibits positive inotropic and vasodilatory effects, making it valuable in the treatment of heart failure and shock. Additionally, its ability to enhance cardiac output and tissue perfusion underpins its application in cardiovascular research and studies investigating adrenergic signaling pathways.

