Catalog No.
Product Name
Application
Product Information
Citations
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β3 Receptor Agonist
BMS-210285 is a selective β3 adrenergic receptor agonist, demonstrating a Ki of 9 nM at the human β3-adrenoceptor. With an intrinsic activity of 83% relative to isoproterenol, it modulates metabolic pathways associated with energy expenditure and lipolysis. This compound is significant for research applications focusing on obesity and type 2 diabetes, aiding in the exploration of therapeutic strategies targeting metabolic disorders. -
Adrenergic Receptor
Metaraminol is a sympathomimetic agent that primarily targets alpha-1 adrenergic receptors. It is utilized in clinical settings to counteract hypotension resulting from vasodilation, particularly in critically ill patients unresponsive to volume resuscitation. Additionally, metaraminol may serve as an adjunct for enhancing cardiac contractility, warranting further exploration of its effectiveness in various medical scenarios. -
MABA
β2AR agonist /M-receptor antagonist-1 functions as a dual muscarinic antagonist and beta-2 adrenergic receptor agonist (MABA). This compound effectively induces relaxation of Carbachol-induced contractions, both in the absence and presence of Propranolol, as well as Histamine-induced contractions. It is valuable for research applications investigating the modulation of bronchoconstriction and potential therapeutic strategies for respiratory disorders. -
Deuterated Brombuterol Hydrochloride
Brombuterol-d9 hydrochloride is a deuterated form of Brombuterol hydrochloride, which acts as a selective β-adrenergic receptor agonist. This compound is utilized in research to study the mechanisms of β-adrenergic signaling and its physiological effects. Brombuterol-d9 hydrochloride can aid in pharmacokinetic studies and the development of novel therapeutic agents targeting β-adrenergic pathways. -
α2-Adrenoceptor Agonist
UK 14819 is a potent α2-adrenoceptor agonist that selectively activates alpha-2 adrenergic receptors. This compound effectively inhibits stimulation-induced contractions in rabbit distal colon, demonstrating an IC50 value of 6.66 nM. UK 14819 is primarily used in pharmacological research to investigate the role of α2-adrenoceptors in gastrointestinal motility and related physiological processes. -
Adrenergic Receptor Agonist
Synephrine hemitartrate is an alkaloid that acts as an α-adrenergic and β-adrenergic agonist, derived from Citrus aurantium. This sympathomimetic compound is primarily utilized in research related to metabolic processes and weight management. Its ability to stimulate adrenergic receptors makes it a valuable reagent for studies focused on energy expenditure and thermogenesis. -
G protein-coupled Bile Acid Receptor Ligand
3-MPPI is a selective G protein-coupled receptor (GPCR) ligand with a strong affinity for the α1-adrenergic receptor, exhibiting a Ki value of 0.21 nM, while its activity on the 5-HT1A receptor is significantly lower at 50 nM. This compound effectively modulates the signaling pathways associated with the α1-adrenergic receptor. Research applications of 3-MPPI include studies on hypertension, the effects of stress-induced anxiety-like behavior, and investigations into levodopa-induced dyskinesia. -
Arrestin-3 Modulator
Arrestin-3 modulator-1 is a selective modulator that interacts with arrestin-3 at the interdomain interface. This compound enhances the recruitment of arrestin-3 to phosphorylation-deficient β2-adrenergic receptors, as evidenced by increased Förster resonance energy transfer (FRET) levels in cellular assays. Arrestin-3 modulator-1 is valuable for studying congenital disorders such as retinal degeneration, hyperthyroidism, and obesity, offering insights into the molecular mechanisms underlying these conditions. -
Adrenergic Receptor Activator
(R)-Midodrine hydrochloride is an adrenergic receptor activator that primarily functions as a vasopressor. It demonstrates significant peripheral alpha(1)-adrenoreceptor agonistic activity, leading to arterial and venous vasoconstriction. This compound is particularly useful in the study and management of symptomatic postural hypotension and related cardiovascular research applications. -
β2 Adrenergic Receptor agonist
Vilanterol acetate is a long-acting agonist of the β2 adrenergic receptor. It exhibits pEC50 values of 9.4 for β2-AR, and lower affinities for β1-AR and β3-AR at 6.4 and 6.1, respectively. By selectively activating airway β2 adrenergic receptors, Vilanterol acetate enhances cAMP levels, leading to relaxation of bronchial smooth muscle. This compound is valuable for research in asthma and related respiratory disorders. -
5-HT Receptor Inhibitor
Metrenperone is a selective inhibitor of the 5-HT2 receptor, exhibiting significant antagonist activity on α1 and α2 adrenergic receptors, as well as anti-H1 and anti-dopaminergic effects. It demonstrates notable biological activities, including the reduction of blood pressure, enhancement of bradycardia during peripheral ischemia, and inhibition of serotonin-induced platelet aggregation. Additionally, Metrenperone antagonizes serotonin-mediated vasoconstriction and is involved in promoting the repair of acutely damaged collagen tissue, making it valuable for various research applications in cardiovascular and vascular biology. -
M3 mAChR Antagonist
p-F-HHSiD (p-Fluorohexahydrosiladifenidol) functions as a selective antagonist of the M3 muscarinic acetylcholine receptor (mAChR). This compound exhibits antagonistic activity against various muscarinic receptor subtypes as well as the alpha-1 adrenergic receptor. p-F-HHSiD is valuable for research in cancer, metabolic disorders, neurological pathologies, and cardiovascular diseases, including colon cancer, Alzheimer's disease, and diabetes. -
α1-Adrenergic Receptor Antagonist
A55453 is a potent α1-adrenergic receptor antagonist, structurally related to prazosin. It demonstrates high affinity for α1-adrenergic receptors and is utilized as a valuable probe in research applications focusing on cardiovascular function and pharmacological studies. The use of 125I-A55453 allows for enhanced detection and analysis of receptor interactions in various experimental settings. -
β3/β1 Adrenergic Receptor Agonist
BMS-196085 is a potent and selective full agonist targeting the human β3 adrenergic receptor, exhibiting a Ki value of 21 nM. Additionally, it demonstrates partial agonist activity at the β1 receptor. This compound is valuable for research applications related to obesity and type-II diabetes, offering insights into adrenergic receptor modulation for therapeutic strategies. -
Antiprion Agent
Chloroguanabenz acetate is an antiprion agent and a derivative of the α2-adrenergic receptor agonist guanabenz. It effectively inhibits prion formation in both yeast and mammalian in vitro assays. Additionally, Chloroguanabenz acetate has been shown to decrease levels of the truncated Huntingtin derivative Htt48 in HEK293T cells, making it a valuable tool in the investigation of Huntington's disease. -
Stable Isotope
Betaxolol-d7 hydrochloride is a deuterium-labeled analog of Betaxolol hydrochloride, functioning primarily as a selective beta-1 adrenergic receptor blocker. This stable isotope is instrumental in pharmacokinetic studies and metabolic investigations, particularly in the context of hypertension and glaucoma research. Its unique labeling enables precise tracking and quantification in various biological assays, facilitating advanced research into cardiovascular and ocular conditions. -
Stable Isotope
Ractopamine-d6 is a deuterium-labeled analogue of Ractopamine, a potent β-adrenergic receptor (βAR) agonist with a Kd of approximately 25 nM for both pig β1AR and β2AR. This stable isotope enables detailed studies of protein metabolism and is instrumental in research focused on enhancing lean tissue growth and improving production efficiency in swine. Its application is crucial for understanding the biochemical pathways influenced by β-adrenergic signaling in agricultural and animal health settings. -
Adrenergic Receptor Inhibitor
Bamosiran is a small interfering RNA that specifically targets the β-adrenergic receptor 2. This compound is recognized for its ability to significantly reduce intraocular pressure, making it valuable in the study of ocular conditions. Its role as an adrenergic receptor inhibitor aids in investigating therapeutic strategies for glaucoma and other eye disorders. -
β2-adrenergic Receptor Agonist
β2AR agonist 3 is a selective agonist of the β2-adrenergic receptor, involved in mediating various physiological responses. This compound has demonstrated potential in the modulation of metabolic pathways and holds promise for research in type 2 diabetes. Its application may facilitate investigations into β2AR-related mechanisms and therapeutic approaches in metabolic disorders. -
α1 Adrenergic Receptors Antagonist
Doxazosin-d8 is a deuterium-labeled derivative of Doxazosin, a selective antagonist of postsynaptic α1 adrenergic receptors. This compound exhibits potent inhibitory effects on α1 receptor-mediated pathways, making it valuable for studying cardiovascular function and related pharmacological effects. Doxazosin-d8 can be utilized in research applications focusing on hypertension, benign prostatic hyperplasia, and other conditions influenced by α1 adrenergic signaling. -
Alpha 2-adrenergic Receptor Antagonist
Vatinoxan is an alpha 2-adrenergic receptor antagonist that selectively inhibits α2-adrenergic receptors, primarily affecting the peripheral nervous system due to limited central nervous system penetration. By binding to these receptors, Vatinoxan mitigates cardiovascular responses typically induced by α2-adrenergic agonists. This compound is valuable in research related to cardiovascular physiology, sedation, and analgesia. -
β-Adrenergic Receptor Blocker
Proxodolol free base is a selective β-adrenergic receptor blocker. It exhibits efficacy in reducing blood pressure and may be utilized in research focused on arterial hypertension and related cardiovascular conditions. This compound can aid in elucidating the mechanisms of β-adrenergic signaling and its impact on cardiovascular health. -
Stable Isotope
Guanfacine-13C,15N3 is a stable isotope-labeled form of Guanfacine, an orally active noradrenergic α2A adrenergic receptor agonist. This compound exhibits high selectivity for the α2A receptor subtype, contributing to its pharmacological effects such as hypotension and sedation. Guanfacine-13C,15N3 serves as a valuable tool in research applications focused on prefrontal cortex cognitive disorders, including Tourette's syndrome and attention deficit hyperactivity disorder (ADHD). -
Drug Derivative
Photoazolol-1 is a β-adrenergic receptor (βAR) blocker derivative that exhibits unique light-dependent activity. Upon photoactivation, Photoazolol-1 transitions from an inverse agonist to a neutral antagonist, making it a valuable tool for studies involving receptor modulation. This compound's distinct photochemical properties enable innovative research applications in drug development and receptor behavior analysis. -
α1-AR Antagonist
RS-100329 is a selective antagonist of the α1-adrenergic receptor (α1-AR), demonstrating effective inhibition of α1-AR-mediated contractions in lower urinary tract tissues both in vitro and in vivo. This compound is valuable for research applications related to the symptomatic management of benign prostatic hyperplasia, facilitating studies on urinary tract dynamics and receptor signaling pathways. -
β3-Adrenergic Receptor Agonist
Fasobegron is a potent β3-adrenergic receptor agonist, exhibiting a human EC50 of 4.8 nM. Additionally, it demonstrates an EC50 of 250 nM for human β1-adrenergic receptors. This compound is primarily utilized in research related to the treatment of overactive bladder. -
β2AR Blocker
Todralazine is a β2 adrenergic receptor (β2AR) blocker that exhibits antioxidant properties and free radical scavenging activity. This compound demonstrates potential in the regulation of blood pressure through its anti-hypertensive effects. It is a valuable reagent for research applications focused on cardiovascular physiology and the modulation of adrenergic signaling pathways. -
Inotropic Compound
Butopamine hydrochloride is an orally active inotropic compound that primarily targets beta-adrenergic receptors. It is known to enhance cardiac output by increasing heart rate and contractility, making it a valuable tool in cardiovascular research. Its potency may surpass that of Dobutamine, positioning it as an important agent for studies focused on heart function and related conditions. -
Beta 3 Receptor Agonist
BMS-194449 is a selective agonist for the beta-3 adrenergic receptor, exhibiting a binding affinity characterized by a Ki value of 160 nM. This compound is instrumental for research into metabolic disorders, particularly obesity and non-insulin dependent diabetes. Its activation of beta-3 receptors plays a critical role in regulating energy expenditure and lipid metabolism, making it a valuable tool for investigations in these areas. -
β-Adrenergic Receptor Blocker
Proxodolol is a β-adrenergic receptor blocker that inhibits β-adrenergic signaling pathways. It is primarily used in research to investigate its effects on arterial hypertension and related cardiovascular conditions. This compound serves as a valuable tool in studying the physiological implications of β-blockade in various therapeutic contexts. -
β2-AR Agonist
Arformoterol maleate is a long-acting β2-adrenergic receptor (β2-AR) agonist, with a half-maximal effective concentration (Kd) of 2.9 nM. This compound is primarily utilized in research related to chronic obstructive pulmonary disease (COPD), demonstrating significant bronchodilation and improving airflow in affected individuals. Its pharmacological properties make it valuable for studying respiratory diseases and the underlying mechanisms of β2-AR signaling. -
Adrenergic Receptor
Parethoxycaine hydrochloride is an anesthetic that acts primarily on the adrenergic receptors, exhibiting nerve conduction blocking activity. It demonstrates non-selective inhibitory effects on the responses of various stimulants in smooth muscle tissues, such as the rat vas deferens and guinea pig ileum. This compound also enhances the action of norepinephrine and its derivatives influence calcium transport processes, displaying distinct effects on calcium dose-response relationships. Parethoxycaine hydrochloride is valuable for research applications involving the modulation of adrenergic signaling and calcium dynamics in neuronal and smooth muscle systems. -
I2 Ligand
Metrazoline is an imidazoline I2 receptor ligand with low affinity for adrenergic receptors. This compound is used in research to study its role in modulating neuroprotective and antihypertensive effects. It serves as a valuable tool for investigating the physiological and pharmacological functions associated with imidazoline receptors in both in vitro and in vivo settings. -
4-Hydroxypropranolol Metabolite
(±)-4-Hydroxy propranolol β-D-glucuronide is a glucuronidated metabolite of the β-adrenergic receptor antagonist, 4-Hydroxypropranolol. It primarily serves as a marker for metabolic studies involving propranolol administration. This compound is valuable for research exploring drug metabolism, pharmacokinetics, and the therapeutic effects of β-blockers in cardiovascular studies. -
Adrenergic Receptor
(3aR,9aR)-Fluparoxan is a highly selective and potent antagonist of the α2B adrenergic receptor. This compound demonstrates significant potential in neurodevelopmental disorder and neurodegenerative disease research by promoting neurological recovery and function. Its unique mechanism of action positions (3aR,9aR)-Fluparoxan as a valuable tool in neuroscience studies, facilitating the exploration of related therapeutic pathways. -
α2-Adrenoceptor Ligand
TDIQ hydrochloride is a selective ligand for the α2-adrenergic receptors, exhibiting high affinity with Ki values of 75 nM, 95 nM, and 65 nM for the α2A, α2B, and α2C subtypes, respectively. This compound serves as a valuable tool for studying the physiological roles of α2-adrenoceptors and their potential therapeutic applications in various neuropsychiatric and cardiovascular disorders. Its specificity makes it suitable for pharmacological investigations and drug development in receptor-targeted therapies. -
Vasorelaxant Agent
Vasorelaxant agent-2 is an effective vasorelaxant agent that targets the α1A-adrenergic receptor, displaying an affinity of pD2=5.4. This compound demonstrates notable vasodilatory activity, evidenced by an EC50 of 0.79 μM in rat aortic rings. It is a valuable tool for research on vascular function and the modulation of blood pressure. -
α2-adrenoceptor Antagonist
A 80426 mesylate is an α2-adrenoceptor antagonist that modulates neurotransmitter release by inhibiting presynaptic α2-adrenergic receptors. This compound demonstrates potential in the study of antidepressant mechanisms and is utilized in research exploring mood disorders and anxiety. Its ability to enhance noradrenergic neurotransmission makes it a valuable tool for investigating therapeutic strategies within the central nervous system. -
Vasopressor
Mephentermine hemisulfate is a sympathomimetic amine that functions primarily as a vasopressor. It is utilized to increase blood pressure by stimulating adrenergic receptors, leading to vasoconstriction and increased heart rate. This compound has applications in cardiovascular research, particularly in studies related to blood pressure regulation and adrenergic signaling pathways. -
β Adrenergic Receptor Antagonist
Soquinolol is a selective β adrenergic receptor antagonist primarily used in cardiovascular research. This compound exhibits significant inhibition of β-adrenergic signaling, making it valuable for studying cardiac dysfunction and heart failure mechanisms. Its application extends to investigations into therapeutic strategies for managing hypertension and arrhythmias. -
ADRB2 Agonist
Mabuterol hydrochloride is a selective, orally active agonist of the beta-2 adrenergic receptor (ADRB2). This compound demonstrates key biological activity by inhibiting cell proliferation and reducing intracellular calcium levels induced by PDGF-BB. Additionally, Mabuterol hydrochloride downregulates protein expression of Drp-1, cyclin D1, and PCNA, while enhancing Mfn-2 expression in response to PDGF-BB. These properties make Mabuterol hydrochloride valuable for research in cellular signaling and related therapeutic applications. -
Platelet Aggregation Inhibitor
D-RGDW is a synthetic peptide containing the Arg-Gly-Asp (RGD) sequence, which targets the αIIbβ3 integrin. It effectively inhibits platelet aggregation, making it a valuable tool for research into thrombosis and hemostasis. D-RGDW can be utilized in various biochemical studies focused on vascular biology and the mechanisms of platelet activation. -
Glycoprotein IIb/IIIa Receptor/Platelet Aggregation Antagonist
Lamifiban TFA is a nonpeptide antagonist of the glycoprotein IIb/IIIa receptor, which plays a critical role in platelet aggregation. This compound effectively inhibits platelet aggregation and has shown potential in enhancing thrombolytic therapy to restore coronary arterial patency. Lamifiban TFA is a valuable tool for research in acute coronary syndromes and related cardiovascular conditions. -
Glycoprotein IIb/IIIa Receptor/Platelet Aggregation Antagonist
Lamifiban is a nonpeptide antagonist of the glycoprotein IIb/IIIa receptor, targeting platelet aggregation processes. It has demonstrated efficacy in restoring coronary arterial patency when used in combination with thrombolytic therapy. Lamifiban is a valuable compound for research focused on acute coronary syndromes and related cardiovascular conditions. -
Glycoprotein IIb-IIIa/Platelet Aggregation Inhibitor
Variabilin is a potent antagonist of glycoprotein IIb-IIIa, functioning primarily as a platelet aggregation inhibitor. Isolated from the hard tick Dermacentor variabilis, Variabilin effectively inhibits platelet aggregation induced by various agonists, including ADP, collagen, and thrombin receptor peptide SFLLRNP. Additionally, it hinders platelet adhesion to immobilized fibrinogen (Fg) and blocks the binding of purified human GPIIb-IIIa to immobilized Fg. This compound is valuable for research applications in hematology and thrombosis. -
CB1R/AMPK Modulator
CB1R/AMPK Modulator 1 is a potent modulator of the cannabinoid receptor type 1 (CB1R) and adenosine monophosphate-activated protein kinase (AMPK), exhibiting a Ki of 0.81 nM and an IC50 of 3.9 nM for CB1R. This compound effectively activates AMPK, leading to significant reductions in food intake and body weight. Additionally, it enhances glucose tolerance and insulin sensitivity, making it a valuable tool for research in metabolic disorders and obesity-related studies. -
A2B Receptor Antagonist
PSB-603 is a potent and highly selective antagonist of the A2B adenosine receptor, exhibiting a Ki value of 0.553 nM. This compound demonstrates minimal affinity for human and rat A1, A2A, and human A3 receptors at concentrations up to 10 μM. PSB-603 is primarily utilized in research exploring adenosine receptor signaling pathways and their implications in various physiological and pathological processes. -
Adenosine A3 Receptor Antagonist
MRS 1523 is a selective antagonist of the adenosine A3 receptor, demonstrating Ki values of 18.9 nM and 113 nM for human and rat A3 receptors, respectively. It exhibits significant selectivity with 140-fold and 18-fold greater affinity for the A3 receptor over A1 and A2A receptors in rat models. MRS 1523 has been shown to produce an antihyperalgesic effect by blocking N-type calcium channels and inhibiting action potentials in isolated rat dorsal root ganglion (DRG) neurons, making it valuable for research in pain mechanisms and receptor activity. -
A2B Adenosine Receptor Antagonist
PSB-1115 is a selective antagonist of the A2B adenosine receptor, providing a valuable tool for investigating adenosine signaling pathways. It effectively inhibits the contraction induced by 2,4,6-trinitrobenzenesulfonic acid (TNBS) in response to acetylcholine (ACh). This compound is relevant for research in inflammation, smooth muscle function, and potential therapeutic interventions targeting adenosine receptors. -
A3 Adenosine Receptor Antagonist
DPTN dihydrochloride is a potent and selective antagonist of the A3 adenosine receptor (A3AR), exhibiting Ki values of 1.65 nM for human, 9.61 nM for mouse, and 8.53 nM for rat receptors. This compound is valuable for research applications investigating the physiological roles of A3AR in various biological processes, including immunomodulation and tumor growth regulation. DPTN's selectivity makes it an important tool for studies aimed at elucidating the therapeutic potential of A3AR modulation in human and animal models.
