Catalog No.
Product Name
Application
Product Information
Citations
-
vasopressor/antihypotensive agent
Midodrine D6 hydrochloride is deuterium labeled Midodrine, which is a vasopressor/antihypotensive agent. - Indoramin D5 is deuterium labeled Indoramin, which is a piperidine antiadrenergic agent.
-
β1-selective adrenergic receptor agonist
Norepinephrine hydrochloride (Levarterenol hydrochloride; L-Noradrenaline hydrochloride) is a β1-selective adrenergic receptor agonist with EC50 of 5.37 μM. - Bretylium (tosylate) is an inhibitor of the presynaptic release of vasoconstrictor neurotransmitters.
-
β-adrenoceptor antagonist
(+)-Penbutolol is a β-adrenoceptor antagonist, with an IC50 of 0.74 μM. -
beta-adrenoceptor agonist
Bambuterol ((??)-Bambuterol; KWD-2183) is a long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma; it also is a prodrug of terbutaline. -
β-adrenergic receptor (βAR) antagonist
(R)-Propranolol hydrochloride is a less active enantiomer of the β-adrenoceptor antagonist propranolol. Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively.
-
β2-AR agonist
Higenamine (Norcoclaurine), a β2-AR agonist, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries.- Ana Rubio, .et al. , Drug Test Anal, 2023, Jul 31 PMID: 37525530
-
alpha2-Adrenergic receptor agonist
Flutonidine is an alpha2-Adrenergic receptor agonist. -
beta-adrenoceptor antagonist
DL 071-IT is a potent non-selective beta-adrenoceptor antagonist. . - Oleuropein Aglycone (3,4-DHPEA-EA) is a bioactive polyphenol and the aglycone form of oleuropein, generated through enzymatic, acidic, or acetylated hydrolysis. It exhibits a broad range of pharmacological effects. In a TgCRND8 transgenic mouse model of Alzheimer’s disease, dietary supplementation (50 mg/kg) increases neuronal autophagic vesicles, reverses cognitive deficits, and reduces histone deacetylase 2 (HDAC2) levels in the cortex and hippocampus. In a high-fat diet-induced obesity rat model, Oleuropein Aglycone elevates urinary norepinephrine, interscapular brown adipose tissue epinephrine, and UCP1 protein levels, while reducing plasma leptin levels and total abdominal fat mass. Additionally, in a carrageenan-induced pleurisy mouse model, it mitigates lung neutrophil infiltration, lipid peroxidation, and IL-1β production. These findings highlight its potential in neurodegenerative, metabolic, and inflammatory disease research.
-
ErbB2 inhibitor
AG-825 is a selective, ATP-competitive inhibitor of ErbB2 (HER2) tyrosine kinase, with an IC₅₀ of 0.35 μM. It exhibits both anticancer and anti-inflammatory activities and has been shown to significantly accelerate apoptosis in human neutrophils. AG-825 also increases β₁-adrenergic receptor (β₁AR) density, suggesting potential cardiomodulatory effects. Due to its multifaceted biological activity, AG-825 is a valuable compound for research in oncology, inflammation, and cardiovascular disease. -
Adrenergic Receptor Antagonist
Propranolol hydrochloride is a nonselective β-adrenergic receptor antagonist that effectively crosses the blood-brain barrier. It exhibits high affinity for both β1AR and β2AR receptors, with Ki values of 1.8 nM and 0.8 nM, respectively, and inhibits [3H]-DHA binding in rat brain membranes with an IC50 of 12 nM. This reagent is widely used in research related to hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy. -
Antihypertensive Agent
Indoramin is an orally active antihypertensive agent targeting the α1A-adrenoceptor. This compound works by selectively blocking α1-adrenoceptors, leading to vasodilation and a reduction in blood pressure. Indoramin is utilized in cardiovascular research to study blood pressure regulation and the mechanisms of hypertension. -
β2-Adrenergic Receptor Agonist
Levalbuterol hydrochloride is a potent β2-adrenergic receptor agonist and the active (R)-enantiomer of Salbutamol. It exhibits enhanced bronchodilator activity, making it a valuable reagent in respiratory research. Primarily, it is utilized in studies focusing on the treatment of chronic obstructive pulmonary disease (COPD) and other airway obstruction disorders. -
α-adrenergic Receptor Agonist
Naphazoline (Naphthazoline) hydrochloride is a potent α-adrenergic receptor agonist. Naphazoline hydrochloride reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline hydrochloride reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF. Naphazoline hydrochloride can be used for non-bacterial conjunctivitis research. -
β1-Adrenergic Blocker
Esmolol hydrochloride is an ultra-short-acting cardioselective β1-adrenergic blocker, primarily targeting the β1-adrenergic receptors. This compound demonstrates significant antiarrhythmic properties and is effective in mitigating post-resuscitation myocardial dysfunction. Additionally, esmolol hydrochloride inhibits aldose reductase activity, reducing advanced glycation end products and enhancing fibroblast migration, which contributes to improved diabetic wound healing. It serves as a valuable tool for research into cardiac diseases, including arrhythmias and diabetic foot ulcers. -
β2-adrenergic receptor Antagonist
Zenidolol is a selective β2-adrenergic receptor antagonist, exhibiting a Ki value of 0.7 nM for the β2 receptor, alongside higher Ki values for β1 and β3 receptors at 49.5 nM and 611 nM, respectively. This compound demonstrates significant antitumor activity by inducing apoptosis, inhibiting tumor sphere formation, and downregulating the HIF pathway in tumor cells. Additionally, Zenidolol has a unique vasodilatory effect specific to pulmonary vessels in mouse models and can serve as an intraocular pressure-lowering agent in ophthalmic research applications. -
Adrenergic Receptor Agonist
Tizanidine hydrochloride is a selective α2-adrenoceptor agonist that serves as an effective skeletal muscle relaxant. It primarily promotes muscle relaxation by reducing the presynaptic release of excitatory amino acids, such as glutamate and aspartate, within spinal cord interneurons. In addition to its central effects, Tizanidine hydrochloride demonstrates potential anti-cancer properties by inhibiting lung cancer cell proliferation, migration, and invasion, while promoting apoptosis via the modulation of the AKT and Wnt3a/β-catenin signaling pathways. This compound is clinically relevant for the management of spasticity associated with conditions like multiple sclerosis, stroke, and spinal cord injury. -
Adrenergic Receptor Agonist
Tizanidine is a selective α2-adrenoceptor agonist that functions primarily as a skeletal muscle relaxant. It exerts muscle relaxation effects by inhibiting the release of excitatory amino acids, thereby modulating synaptic activity in the spinal cord. Additionally, Tizanidine demonstrates anti-cancer properties by inhibiting proliferation, migration, and invasion of lung cancer cells, as well as inducing apoptosis through the upregulation of Nischarin and suppression of the AKT and Wnt3a/β-catenin pathways. This compound is utilized clinically for the management of spasticity associated with conditions such as multiple sclerosis, stroke, and spinal cord injury. -
α/β-Adrenergic Agonist
Etilefrine is an α/β-adrenergic agonist primarily targeting α1 and β1 receptors. Its activity induces vasoconstriction by stimulating α1 receptors, leading to increased peripheral resistance, while β1 receptor activation enhances myocardial contractility and elevates heart rate, resulting in improved blood pressure and cardiac output. Additionally, Etilefrine modulates the AMPK/Akt signaling pathway, influencing phosphorylation levels. This compound is applicable in cardiovascular research, notably in studies related to postural hypotension, chylothorax, and conditions characterized by low cardiac output. -
Indole Alkaloid
Tetrahydroalstonine is an indole alkaloid that acts as a selective antagonist of the α₂-adrenergic receptor. This compound demonstrates neuroprotective effects and has been shown to modulate autophagy-lysosomal function through the activation of the Akt/mTOR signaling pathway. Additionally, Tetrahydroalstonine significantly mitigates injury to primary cortical neurons induced by oxygen-glucose deprivation/reperfusion, making it a valuable tool for research into neuroprotection and cellular stress responses. -
α/β-Adrenergic Agonist
Etilefrine hydrochloride is an α/β-adrenergic agonist that selectively activates α1 and β1 adrenergic receptors. By stimulating α1 receptors, it induces vascular smooth muscle contraction, thereby increasing peripheral resistance and blood pressure. Additionally, activation of β1 receptors enhances myocardial contractility and heart rate, improving cardiac output. Etilefrine hydrochloride is valuable for cardiovascular research, particularly in studies related to postural hypotension, chylothorax, and the management of low cardiac output conditions. -
α-Adrenergic Receptor Agonist
Naphazoline is a potent α-adrenergic receptor agonist that exerts its biological activity through vasoconstriction and the reduction of vascular hyperpermeability. It effectively diminishes the levels of inflammatory mediators, including TNF-α, IL-1β, IL-6, IFN-γ, IL-4, as well as IgE, GMCSF, and NGF. Naphazoline is widely utilized in research related to non-bacterial conjunctivitis and other conditions involving inflammation and vascular function. -
α-Adrenergic Receptor Agonist
Naphazoline nitrate is an α-adrenergic receptor agonist that effectively induces vasoconstriction and reduces vascular hyperpermeability. It has been shown to lower the levels of inflammatory mediators such as TNF-α, IL-1β, IL-6, as well as cytokines including IFN-γ and IL-4. Naphazoline nitrate is utilized in research related to non-bacterial conjunctivitis, providing insight into its effects on inflammation and vascular response. -
Dopamine Receptor Antagonist
Perphenazine is a potent dopamine receptor antagonist, specifically targeting D2 and D3 receptors with Ki values of 0.56 nM and 0.43 nM, respectively, while also interacting with the 5-HT2A receptor and the Alpha-1A adrenergic receptor. This compound demonstrates inhibitory effects on cancer cell proliferation and promotes apoptosis. Perphenazine is valuable for research into psychiatric disorders, cancer biology, and inflammatory processes. -
Antiarrhythmic Agent
Dronedarone is a class III antiarrhythmic agent primarily targeting ion channels to manage atrial fibrillation (AF) and atrial flutter. It effectively inhibits multiple ion currents, including potassium, sodium, and L-type calcium currents, while also displaying antiadrenergic properties through noncompetitive binding to β-adrenergic receptors. Additionally, Dronedarone acts as a moderate inhibitor and substrate for CYP3A4, making it valuable for pharmacological studies in cardiac rhythm disorders. -
Adrenergic Receptor Antagonist
Dibenamine is an alpha-adrenergic receptor antagonist that inhibits both basal and histamine-stimulated gastric acid secretion. Its primary pharmacological activity renders it useful in studying conditions characterized by excessive gastric acid production. Additionally, Dibenamine can be employed in research concerning adrenergic signaling pathways and their impact on gastric physiology. -
Dopamine Receptors Blocker
Trifluoperazine dihydrochloride is a dopamine receptor antagonist, primarily used in the study of schizophrenia. This compound demonstrates significant activity as an α1-adrenergic receptor blocker and acts as a potent inhibitor of NUPR1, exhibiting anticancer properties. Additionally, it functions as a calmodulin inhibitor and has been shown to inhibit P-glycoprotein, impacting multidrug resistance. Trifluoperazine dihydrochloride is also recognized for its reversible inhibition of influenza virus morphogenesis, making it valuable for various research applications in neuropharmacology and virology. -
Adrenergic Receptor Agonist
Salbutamol is a short-acting β2-adrenergic receptor agonist that primarily targets the β2-adrenergic receptor. It is well-known for its ability to promote relaxation of bronchial smooth muscle, making it a valuable tool in the study of bronchospasm related to asthma and chronic obstructive pulmonary disease. Additionally, Salbutamol has been implicated in promoting tumorigenesis in gastric cancer cells via the β2-AR/ERK/EMT signaling pathway, highlighting its relevance in cancer research. -
β/α-1 Blocker
Carvedilol phosphate hemihydrate is a non-selective β/α-1 adrenergic receptor blocker. It demonstrates significant biological activity by inhibiting lipid peroxidation with an IC50 of 5 μM and acts as a multiple-action antihypertensive agent, with potential applications in treating angina and congestive heart failure. Additionally, carvedilol phosphate hemihydrate has been identified as an autophagy inducer that suppresses the NLRP3 inflammasome, making it valuable for research in inflammation and cardiovascular diseases. -
Adrenergic Receptor Inhibitor
Penbutolol sulfate is a potent adrenergic receptor inhibitor, primarily acting as a β-adrenoceptor and 5-HT receptor antagonist, with Ki values of 11.6 nM and 11.9 nM for 5-HT in rat cornu ammonis 1 (CA1) and human CA3 regions, respectively. This compound demonstrates significant biological activity through modulation of neurotransmitter signaling pathways, making it valuable for research applications involving cardiovascular studies and neuropharmacology. -
Serotonin Receptor Antagonist
Setiptiline maleate is a serotonin receptor antagonist targeting multiple pathways in neurotransmitter regulation. As a tetracyclic antidepressant (TeCA), it functions primarily as a noradrenergic and specific serotonergic antidepressant (NaSSA), inhibiting norepinephrine reuptake and antagonizing α2-adrenergic receptors. Setiptiline maleate further interacts with serotonin receptor subtypes, including 5-HT2A, 5-HT2C, and/or 5-HT3, while also acting as an H1 receptor inverse agonist, demonstrating potential utility in depression and anxiety research. -
5-HT1A Receptor Agonist
Tandospirone citrate is a selective partial agonist of the 5-HT1A receptor, exhibiting a binding affinity with a Ki value of 27 nM. It demonstrates significant selectivity over other serotonin and adrenergic receptors, including SR-2, SR-1C, α1, α2, D1, and D2, with Ki values ranging from 1300 to 41000 nM. This compound is primarily used in research related to psychiatric disorders and anxiety management, making it a valuable tool for exploring serotonergic pathways and their implications in mental health. -
5-HT1AR Agonist/α1-Adrenergic Receptor Antagonist
Enciprazine is an orally active non-benzodiazepine anxiolytic that primarily functions as a 5-HT1A receptor agonist and an α1-adrenergic receptor antagonist. This compound has demonstrated the ability to modulate electroencephalogram activity by decreasing δ and θ wave power while increasing α and fast β wave power. With its anti-aggressive properties, Enciprazine exhibits minimal sedative and ataxic side effects. Additionally, it influences plasma corticosterone levels and activates the hypothalamic-pituitary-adrenal axis, making it a valuable tool for research into anxiety disorders, generalized anxiety syndrome, and psychosis. -
Adrenergic Receptor Antagonist
Tertatolol is a potent antagonist of beta-adrenoceptors and 5-HT receptors. It exhibits unique renal vasodilatory effects, making it a valuable tool for investigating cardiovascular and renal physiology. Tertatolol is utilized in research applications focusing on the modulation of adrenergic signaling and its implications in various pathological conditions. -
Stable Isotope
Pindolol-d7 is a deuterated form of Pindolol, primarily targeting the 5-HT 1A (Ki=33 nM) and 5-HT 1B receptors, as well as β1/β2-adrenergic receptors. This stable isotope is utilized in research to investigate the pharmacokinetics and metabolic pathways of Pindolol. The compound demonstrates significant anti-anxiety and antidepressant activities, making it valuable for studies related to psychiatric disorders and neuropharmacology. -
Stable Isotope
Melperone-d4 hydrochloride is a deuterium-labeled derivative of Melperone hydrochloride, a butyrophenone with atypical antipsychotic properties. It acts as a multireceptor antagonist, exhibiting binding affinities (Kd values) of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Additionally, Melperone-d4 displays weak interactions with several other receptors and inhibits CYP2D6. This reagent is particularly valuable for investigating schizophrenia and managing agitation in geriatric populations. -
Adrenergic Receptor Antagonist
(4E)-SUN9221 is a potent antagonist of the α1-adrenergic receptor and the 5-HT2 receptor, demonstrating significant biological activity in modulating cardiovascular responses. This compound exhibits antihypertensive effects and inhibits platelet aggregation, making it a valuable tool for research in hypertension and thrombosis. Its ability to selectively target these receptors provides insights into adrenergic signaling and related pathological conditions. -
5-HT1/5-HT2/adrenergic (α1) Receptors Antagonist
Centpropazine is a non-selective antagonist of serotonin (5-HT1/5-HT2) and adrenergic (α1) receptors. It modulates monoamine neurotransmission by reducing the reuptake of serotonin and norepinephrine, leading to antidepressant effects. This compound is valuable for research into depression and related mood disorders, facilitating insights into neurotransmitter dynamics and their role in mental health. -
Triple Reuptake Inhibitor
Tedatioxetine is a serotonin and norepinephrine-preferring triple reuptake inhibitor (TRI) that also functions as an antagonist of 5-HT2A, 5-HT2C, 5-HT3, and α1A-adrenergic receptors. This compound exhibits significant biological activity in modulating neurotransmitter levels, making it relevant for research in neuropharmacology. Its mechanism of action positions it as a valuable tool in studies related to mood disorders and anxiety. -
Piperazine
1-(3-Fluorophenyl)piperazine (hydrochloride) is a selective blocker of the 5-HT receptor 1A and an adrenergic receptor antagonist. This compound exhibits significant biological activity relevant to research in neuropharmacology, particularly in the study of serotonergic and adrenergic signaling pathways. It can be utilized in various applications, including the investigation of anxiety, depression, and other mood disorders. -
5-HT6 Receptor Agonist
ST1936 oxalate is a selective agonist of the 5-HT6 receptor, demonstrating high nanomolar affinity with a Ki value of 13 nM for the human receptor. It exhibits additional binding affinity for 5-HT7 and 5-HT2B receptors with Ki values of 168 nM and 245 nM, respectively, as well as moderate binding to α2 adrenergic receptors in both human and rat models (Ki of 300 nM). This compound is valuable for research applications focused on serotonergic signaling and its implications in neuropharmacology.
