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α1-Adrenergic Receptor Antagonist
Piperoxan is an α1-adrenergic receptor antagonist that effectively inhibits 3H-prazosin binding to rat brain α1-adrenoceptors with a Ki value of 360 nM. This compound serves as a useful tool for studying the adrenergic system and can aid in the exploration of adrenergic system-related diseases. Its application extends to various research fields investigating the physiological and pharmacological effects mediated by α1-adrenergic receptors. -
Adrenergic Receptor antagonist
Abanoquil methylsulfate is an alpha-1 adrenergic receptor antagonist. It exhibits significant biological activity in inhibiting adrenergic signaling pathways, making it a valuable tool in research related to cardiovascular diseases, including arrhythmias and erectile dysfunction. Its use can enhance understanding of the physiological roles of adrenergic receptors in these conditions. -
Adrenergic Receptor
Moxisylyte is an alpha-1 adrenergic receptor antagonist that enhances bladder emptying. It is primarily utilized to alleviate urinary complications in patients with multiple system atrophy by reducing residual urine following urination. Additionally, Moxisylyte is effective in addressing erectile dysfunction and temporarily improving blood flow in conditions such as Raynaud's syndrome. Furthermore, this compound can be topically applied to the eye to counteract mydriasis induced by phenylephrine and other sympathetic agonists. -
α1b-AR Antagonist
α1B-AR antagonist 1 is a selective antagonist of the alpha-1B adrenergic receptor (α1B-AR). This compound exhibits significant inhibitory effects on α1B-AR signaling, making it valuable for studying cardiovascular and central nervous system disorders. Its specificity allows for detailed investigation into the role of α1B-AR in various physiological and pathological processes. -
Adrenergic Receptor
Ambenoxan hydrochloride targets adrenergic receptors as a central nervous system-acting skeletal muscle relaxant. It effectively reduces decerebrate rigidity in animal models such as rabbits, while preserving righting reflex without peripheral neuromuscular blocking effects. The compound has been shown to prolong sleep duration in conjunction with hexobarbitone and can lower blood pressure and diminish epinephrine-induced pressor responses in anesthetized cats. It is not associated with local anesthetic effects or antagonism of strychnine, leptazol, or tremorine. -
β-Adrenergic Antagonist
Levobunolol is a potent, nonselective β-adrenergic receptor antagonist. It is primarily utilized as an ocular hypotensive agent, effectively lowering mean intraocular pressure (IOP). This compound is of interest in research focused on glaucoma and superior oblique myokymia (SOM), providing valuable insights into their mechanisms and potential therapeutic strategies. -
Adrenergic Receptor
(-)-Domesticine is an anti-α-1D-adrenoceptor compound with demonstrated cytotoxic activity. It exhibits significant activity in MTS cytotoxicity assays against human colon cancer cell lines, specifically HCT-116 and Caco-2, with IC50 values ranging from 23 to 38 μM, comparable to the cytotoxic agent etoposide. This compound is also amenable to structural modifications, allowing the inclusion of alkoxy substituents and benzoate functional groups at the C1 position, which may enhance its biological activity in various cancer research applications. -
β2 Agonist
Mabuterol-d9 is a deuterated form of Mabuterol, a selective agonist of the β2-adrenergic receptor. It is primarily utilized in research related to respiratory conditions and is crucial for studying receptor interactions and pharmacokinetics. The deuterium labeling enhances its stability and allows for advanced analytical applications, making it a valuable tool in pharmacological research. -
β1-adrenergic Receptor Blocker
Pafenolol is a selective β1-adrenergic receptor blocker that effectively reduces blood pressure. Studies have demonstrated that its bioavailability can be affected by gastrointestinal factors, with the presence of food leading to decreased absorption in animal models. This compound is valuable for research applications in cardiovascular diseases and respiratory conditions such as asthma. -
Adrenergic Receptor Antagonist
Terazosin dimer impurity dihydrochloride serves as an impurity derived from Terazosin, a well-known quinazoline compound functioning as a competitive and orally active α1-adrenoceptor antagonist. This impurity may provide insights into the stability and metabolism of Terazosin during pharmacological studies. It is relevant for research applications focused on adrenergic signaling and the characterization of drug formulations. -
Stable Isotope
Ractopamine-d5 hydrochloride is a stable isotope-labeled form of the potent β-adrenergic receptor (βAR) agonist, Ractopamine hydrochloride. It exhibits strong binding affinity to pig β1AR and β2AR, with Kd values approximately 25 nM. This reagent is primarily utilized in research focused on protein metabolism, specifically for studying the enhancement of lean tissue growth and production efficiency in swine. -
Adrenergic Receptor Antagonist
Butidrine is an adrenergic receptor antagonist known for its intraocular pressure-lowering activity. While it demonstrates efficacy in reducing intraocular pressure, it is relatively less potent compared to certain other beta-adrenergic receptor blockers in rabbit models. This compound is primarily utilized in ocular pharmacology research to explore its potential applications in treating conditions such as glaucoma and ocular hypertension. -
β3-Adrenergic Receptor Agonist
CP-331684 is an orally active agonist of the β3-Adrenergic receptor, which plays a significant role in metabolic regulation. This compound has demonstrated potential in promoting lipolysis and improving insulin sensitivity, making it valuable for research applications focused on obesity and metabolic disorders. Its ability to selectively activate β3-adrenergic signaling pathways positions CP-331684 as a useful tool for investigating therapeutic strategies in weight management and related metabolic conditions. -
Adrenergic Receptor
Levomoprolol, the (S)-enantiomer of moprolol, functions as a beta-adrenergic receptor antagonist. It exhibits key biological activity by inhibiting beta-1 and beta-2 adrenergic receptors, making it relevant for studies related to cardiovascular physiology and pharmacology. This compound is utilized in research applications focused on heart rate regulation, hypertension, and other adrenergic receptor-mediated processes. -
Adrenergic Receptor
DSP 4 free base is a selective neurotoxin that targets the adrenergic receptors in noradrenergic neurons, particularly within the locus coeruleus. This compound is notable for its capacity to cross the blood-brain barrier and cyclizes to generate a reactive aziridinium derivative, which accumulates within noradrenergic neurons. It serves as a valuable tool for research into neurotoxicity and the pharmacological mechanisms of adrenergic signaling. -
Adrenergic Receptor Blocker
N-1518 is an adrenergic receptor blocker that exhibits competitive antagonism at both α1 and β1 receptors, with approximately 20-fold selectivity for α1. This compound demonstrates vasodilatory effects, making it a valuable tool for investigating hypertension treatment and related cardiovascular research applications. N-1518 offers insights into the differential roles of adrenergic receptors in physiological processes and therapeutic interventions. -
D1 Dopamine Agonist
Agroclavine is a natural ergot alkaloid that acts as a D1 dopamine receptor and α1-adrenoceptor agonist. This compound exhibits notable biological activities, including anticancer and antimicrobial properties. Agroclavine is of interest in research applications related to dopamine signaling pathways, cancer therapeutics, and antimicrobial studies. -
β2AR Agonist
β2AR Agonist 5 is a selective agonist of the β2-adrenergic receptor (β2AR), exhibiting an EC50 value of 0.19 nM. This compound effectively induces Bioluminescence Resonance Energy Transfer (BRET), demonstrating its potential in receptor signaling studies. β2AR Agonist 5 is particularly useful for research related to asthma and chronic obstructive pulmonary disease (COPD), aiding in the understanding of therapeutic mechanisms and drug development in respiratory conditions. -
α2A/α2B AR Inhibitor
BRL-44408 is a selective antagonist of the α2A and α2B adrenergic receptors. It effectively inhibits the actions of norepinephrine and the agonist Clonidine on the release of [3H]norepinephrine and [3H]5-hydroxytryptamine in K+-stimulated conditions. With a higher affinity for α2A-adrenoceptors in human platelet membranes compared to other antagonists, BRL-44408 may play a significant role in modulating neurotransmitter release, making it a valuable tool for research in adrenergic signaling and related pharmacological studies. -
Bucindolol Isomer
(S)-Bucindolol is the (S)-isomer of Bucindolol, functioning as a selective β1-adrenergic receptor blocker. This compound is primarily utilized in research focusing on cardiac failure and related cardiovascular conditions, providing insights into heart function and pharmacological interventions. Its specificity for the β1-adrenergic receptors makes it valuable for studying therapeutic effects and mechanisms in cardiac health. -
Anesthetic Agent
Jingsongling is an anesthetic agent that acts primarily on α2-adrenoceptors. Its mechanism of action results in bradycardia and hypertension, highlighting its impact on cardiovascular function. Additionally, Jingsongling inhibits gastric motility in canines through the modulation of both α1 and α2 adrenergic receptors, making it valuable for research in anesthetic effects and gastrointestinal regulation. -
NET Inhibitor
XEN-2174 is a selective noradrenaline transporter (NET) inhibitor that functions through non-competitive inhibition of noradrenaline reuptake. By increasing the synaptic concentration of noradrenaline, it activates α2-adrenergic receptors at the spinal level, leading to pronounced analgesic effects. This compound demonstrates sustained analgesia in various models of neuropathic and postoperative pain in rats, making it a valuable tool for pain research applications. -
β-adrenergic Receptor Antagonist
Ridazolol hydrochloride is a selective β-adrenergic receptor antagonist, predominantly targeting the β-1 adrenergic receptor. It exhibits moderate intrinsic sympathomimetic activity, allowing it to competitively inhibit the relaxation effects of isoproterenol. This compound is utilized in research focused on cardiovascular diseases, providing insights into adrenergic signaling and potential therapeutic interventions. -
β-blocker
(S)-Alprenolol is a potent nonselective β-blocker that exerts its effects by antagonizing β-adrenergic receptors. This compound is primarily utilized in cardiovascular research to investigate mechanisms of heart rate regulation and blood pressure control. Its unique properties make it suitable for studying various physiological responses mediated by adrenergic signaling. -
Stable Isotope
(R)-Carvedilol-d4 is a deuterium-labeled derivative of (R)-Carvedilol, primarily targeting α-adrenergic receptors. This compound exhibits significant biological activity by inhibiting spontaneous Ca2+ waves and effectively mitigating stress-induced ventricular tachycardia. Furthermore, (R)-Carvedilol-d4 demonstrates potential in research applications related to cardiovascular health and oncology, notably delaying the progression of UV-induced skin tumors and reducing their malignancy. -
Stable Isotope
DL-Phenylephrine-d3 hydrochloride is a deuterium-labeled derivative of DL-Phenylephrine hydrochloride, primarily targeting the alpha1-adrenergic receptor. This compound demonstrates significant vasoconstrictive activity, making it useful in the study of adrenergic signaling pathways. Its stable isotope labeling facilitates precise quantitative analyses in pharmacokinetic studies and metabolic research applications. -
Adrenergic Receptor Inhibitor
(-)-Amosulalol is a selective inhibitor of α1/β1-adrenergic receptors, demonstrating dual action in pharmacological studies. It exhibits antihypertensive properties primarily through the blockade of α1-adrenergic receptors, effectively reducing peripheral vascular resistance. Additionally, (-)-Amosulalol decreases reflex tachycardia and plasma renin activity in models of hypertension, making it valuable for research in cardiovascular diseases and hypertension management. -
β-blocking Agent
Timolol hemimaleate is a β-blocking agent that exerts its effects primarily by antagonizing β-adrenergic receptors. It is widely utilized in the management of intraocular pressure associated with open-angle glaucoma and ocular hypertension through topical application. Additionally, Timolol hemimaleate has applications in the research of conditions such as infantile hemangiomas, hypertension, myocardial infarction, migraine prophylaxis, and atrial fibrillation, demonstrating its cardioprotective properties. -
α1-Adrenoceptor Antagonist
Neldazosin is a selective α1-adrenoceptor antagonist that exhibits significant pharmacological activity by blocking the action of norepinephrine on α1-adrenergic receptors. This compound has been widely studied for its potential in managing hypertension and benign prostatic hyperplasia. Its ability to induce vasodilation and relax smooth muscle makes it valuable in cardiovascular and urological research applications. -
α1-adrenergic Receptor Antagonist
Terazosin-md is an orally active α1-adrenergic receptor antagonist that enhances mitochondrial metabolism and degrades pathological protein accumulations. This compound also improves vascular endothelial cell function, demonstrating efficacy in a mouse model of Alzheimer's disease. Terazosin-md is valuable for research focusing on Alzheimer's disease, related complications, and conditions arising from protein accumulation and metabolic dysregulation. -
Beta1 Adrenergic Receptor Blocker
Pacrinolol is a selective and orally active beta1 adrenergic receptor blocker. It effectively inhibits the positive inotropic effects and increased heart rate induced by Isoprenaline. Pacrinolol is valuable for research applications focused on cardiovascular diseases, offering insights into heart function modulation and potential therapeutic strategies. -
α1 Adrenoceptor Antagonist
GG-818 is a selective antagonist of the α1 adrenoceptor, exhibiting potent inhibition with pKi values of 9.7 for α1a, 7.8 for α1b, and 7.6 for α1d. This compound is valuable in the study of benign prostatic hyperplasia and contributes to understanding α1 adrenoceptor-mediated signaling pathways and their implications in urological health. Its specificity may facilitate research into potential therapeutic interventions targeting α1 adrenergic receptors. -
Adrenergic Receptor
Garomefrine hydrochloride is an α1A-adrenergic receptor agonist known for its potential to inhibit urinary incontinence. This compound demonstrates significant contractile activity in porcine nasal mucosal vessels, suggesting its effectiveness in modulating vascular responses. Due to its high potency and biological efficacy, Garomefrine hydrochloride serves as a valuable tool for research focused on adrenergic signaling and related therapeutic applications. -
Adrenergic Receptor
KUL-7211 racemate is a selective β-adrenoceptor agonist with significant affinity for adrenergic receptors. This compound demonstrates enhanced cardiovascular effects and has potential applications in research focused on cardiovascular physiology and pharmacology. It serves as a valuable tool for studying the mechanisms of β-adrenergic signaling and its implications in disease models. -
Adrenergic Receptor Agonist
Naminterol is a phenethanolamine derivative that functions as a β2 adrenergic receptor agonist, demonstrating significant bronchodilatory activity. This compound is primarily utilized in research related to respiratory conditions, particularly for exploring therapeutic options in asthma management. By activating β2 receptors, Naminterol helps to relax bronchial smooth muscle, making it a valuable tool in understanding airway responsiveness and the pharmacological modulation of asthma symptoms. -
Adrenergic Receptor
(S)-Dabelotine is a selective adrenergic receptor agonist that has been primarily investigated for its potential role in dementia research. As the S-isomer of Dabelotine, it exhibits enhanced biological activity at adrenergic receptors, making it a valuable tool for studying neurodegenerative diseases and related neurological pathways. Its unique mechanism of action offers insights into adrenergic signaling and its implications in cognitive function disorders. -
β1-Adrenergic Receptor Blocker
Atenolol hydrochloride is a cardioselective β1-adrenergic receptor blocker, exhibiting a Ki of 697 nM at the β1-adrenoceptor in guinea pig left ventricle membranes. This compound is primarily used in the investigation of cardiovascular conditions such as hypertension and angina pectoris, providing insights into heart rate modulation and blood pressure regulation. Its selective mechanism makes it a valuable tool for researchers studying adrenergic signaling pathways and therapeutic approaches for cardiac disorders. -
β-adrenergic Receptor Agonist
BRL-26830A is a selective β-adrenergic receptor agonist that enhances metabolic activity and promotes weight loss in obese mouse models. In ICR mouse models, BRL-26830A significantly stimulates insulin secretion and lowers blood glucose levels. This compound is valuable for investigating the mechanisms underlying endocrine and metabolic disorders, such as obesity and diabetes. -
β-adrenergic Agonist
Phenylethanolamine A is a β-adrenergic agonist that engages the β-adrenergic receptor, leading to physiological responses such as increased heart rate and bronchodilation. This compound serves as a valuable research tool for studying the signaling pathways associated with adrenergic receptor activation and its implications in various physiological processes and conditions. Its utility extends to investigations in cardiovascular and respiratory pharmacology. -
Adrenergic Receptor Agonist
Methyldopate hydrochloride is an ethyl ester hydrochloride prodrug of α-Methyldopa, functioning primarily as an α-adrenergic receptor agonist, with a selectivity for α2-adrenergic receptors. This compound plays a crucial role in research related to severe hypertension, facilitating studies into adrenergic receptor modulation and its implications in cardiovascular health. Its efficacy as a proagent makes it a valuable tool for exploring the pharmacodynamics of α-adrenergic receptor activity. -
Postsynaptic Alpha-Receptor Antagonist
IP-66 is a potent postsynaptic alpha-receptor antagonist that inhibits α-adrenergic receptor signaling. This compound is valuable for studying cardiovascular diseases, particularly hypertension, by offering insights into receptor-mediated pathways and their role in vascular function. Researchers may utilize IP-66 to explore therapeutic interventions targeting α-receptors in cardiovascular research. -
β3 Agonist
BMS-201620 is a selective β3 adrenergic receptor agonist, exhibiting a Ki of 93 nM. This compound demonstrates potential in promoting lipolysis and improving metabolic parameters, making it valuable for research in obesity and non-insulin-dependent diabetes. Its specificity for the β3 receptor facilitates studies investigating the role of β3 signaling in energy expenditure and glucose metabolism. -
Adrenergic Receptor Inhibitor
IMTPPE is an adrenergic receptor inhibitor that selectively targets the androgen receptor (AR) in prostate cancer cells. It effectively inhibits AR transcriptional activity and reduces protein levels, leading to decreased proliferation of AR-positive prostate cancer cells, while showing no effect on AR-negative cells. Additionally, IMTPPE demonstrates significant anti-tumor activity against enzalutamide-resistant 22Rv1 xenograft tumors, making it a valuable tool for studying AR signaling pathways and developing therapeutic strategies for resistant prostate cancer. -
Adrenaline Receptor Antagonists
AH 11110A is a selective antagonist of the α1B-adrenoceptor. It exhibits potent activity in modulating adrenergic signaling pathways, though it may not effectively differentiate between the various α1 adrenoceptor subtypes (A, B, and D) or distinguish between α1 and α2 adrenoceptors. This compound is primarily utilized in research focused on cardiovascular and neurological studies involving adrenergic receptor modulation. -
Stable Isotope
Bisoprolol-d7 is a deuterium-labeled analog of Bisoprolol, a selective and orally active β1-adrenergic receptor blocker with minimal β2-receptor activity. This stable isotope is primarily used in pharmacokinetic studies to investigate the metabolism and distribution of Bisoprolol in biological systems. Its applications extend to research involving hypertension, coronary artery disease, and stable ventricular dysfunction. -
Adrenergic Receptor Agonist
Dilevalol, a selective β2-adrenergic receptor agonist, exhibits significant antihypertensive properties, making it useful in managing hypertension, particularly during pregnancy. This compound facilitates vasodilation and reduces peripheral resistance, thus improving blood flow. Its applications in clinical research include studying adrenergic signaling pathways and exploring potential therapeutic strategies for managing pregnancy-induced hypertension. -
Stable Isotope
Salmeterol-d5 is a deuterated analog of Salmeterol, serving as a stable isotope. Salmeterol is a highly selective agonist of the human β2 adrenergic receptor, demonstrating significant stimulation of cAMP accumulation in Chinese Hamster Ovary (CHO) cells expressing β2, β1, and β3 adrenoceptors with pEC50 values of 9.6, 6.1, and 5.9, respectively. This compound is valuable in pharmacological research, particularly in studies investigating β2 adrenergic signaling pathways and respiratory system pharmacotherapy. -
Adrenergic Receptor Agonist
Prenalterol hydrochloride is a selective partial agonist of the β1-adrenergic receptor, known for its positive inotropic effects. This compound has demonstrated significant efficacy in the management of acute heart failure, low output syndrome following myocardial infarction, and shock. Additionally, it has been used to alleviate orthostatic hypotension associated with Shy-Drager syndrome, making it a valuable reagent for cardiovascular research. -
βAR/mTAAR1 Agonist
Ractopamine is a potent β-adrenergic receptor (βAR) agonist, exhibiting a Kd value of approximately 25 nM for porcine β1AR and β2AR, and serves as an mTAAR1 agonist with an EC50 of 16 μM. This compound is known to facilitate muscle mass development, decrease fat deposition, reduce feed intake, and enhance both total cellular protein synthesis and growth rates in swine. Ractopamine is a valuable reagent for research focused on increasing lean tissue growth and improving production efficiency in livestock. -
β-adrenergic Receptor Antagonist
Esprolol is a potent β-adrenergic receptor antagonist with oral bioavailability. It is rapidly metabolized by blood and tissue esterases to yield the active metabolite amoxolol. This compound exhibits significant potential for investigating therapeutic approaches in exercise-induced angina and cardiovascular research.

