2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Adrenergic Receptor

Adrenergic Receptor

Beta Receptor

Adrenergic Receptor

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Adrenergic receptors are a class of G protein-coupled receptors that are targets of the catecholamines, especially norepinephrine and epinephrine. Many cells possess these receptors, and the binding of a catecholamine to the receptor will generally stimulate the sympathetic nervous system. The sympathetic nervous system is responsible for the fight-or-flight response, which includes widening the pupils of the eye, mobilizing energy, and diverting blood flow from non-essential organs to skeletal muscle. There are two main groups of adrenergic receptors, α and β, with several subtypes. α receptors have the subtypes α1 and α2. β receptors have the subtypes β1, β2 and β3. All three are linked to Gs proteins, which in turn are linked to adenylate cyclase. Agonist binding thus causes a rise in the intracellular concentration of the second messenger cAMP. Downstream effectors of cAMP include cAMP-dependent protein kinase (PKA), which mediates some of the intracellular events following hormone binding.

Adrenergic Receptor Isoform Specific Products:

Adrenergic Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-14301
    Olodaterol
    		Agonist 98.47%
    Olodaterol (BI1744) is a selective, long acting β2-adrenoceptor (β2-AR) agonist (EC50=0.1 nM and pKi= 9.14 for human β2-adrenoceptor, respectively). Olodaterol can be used for chronic obstructive pulmonary disease (COPD) and pulmonary fibrosis.
    Olodaterol
  • HY-16736A
    Centanafadine hydrochloride
    		Inhibitor 99.93%
    Centanafadine (hydrochloride) is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively.
    Centanafadine hydrochloride
  • HY-17503B
    Metoprolol tartrate
    		Antagonist 99.98%
    Metoprolol tartrate is an orally active, selective β1-adrenoceptor antagonist. Metoprolol tartrate shows anti-inflammation, antitumor and anti-angiogenic properties.
    Metoprolol tartrate
  • HY-B0802
    Terbutaline sulfate
    		Agonist 99.95%
    Terbutaline sulfate is an orally active β2-adrenergic receptor agonist and an active metabolite of bambuterol. Terbutaline sulfate can be used in asthma symptom research.
    Terbutaline sulfate
  • HY-N2037
    Higenamine
    		Agonist 98.91%
    Higenamine (Norcoclaurine), a β2-AR agonist with antioxidant capability, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine is also a α1-adrenergic receptor antagonist with hypotensive effect. is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine protects myocyte Apoptosis and ischemia/reperfusion (I/R) injury through selective activation of beta2-adrenergic receptor (β2-AR). Higenamine also reduces I/R-induced myocardial infarction in mice. Higenamine can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine can be used to study cancer, inflammation, cardiorenal syndrome and other diseases.
    Higenamine
  • HY-B0799
    Dihydroergotoxine mesylate
    		Inhibitor 99.88%
    Dihydroergotoxine mesylate (Ergoloid mesylates) is an α-adrenergic blocking agent. Dihydroergotoxine mesylate binds with high affinity to the GABAA receptor associated Cl- channel. Dihydroergotoxine mesylate also interacts with central dopaminergic and serotonergic receptors. Dihydroergotoxine mesylate displays antiproliferative, antihypertensive and neuroprotective activity.Dihydroergotoxine mesylate (Ergoloid mesylates) is an α-adrenergic blocking agent. Dihydroergotoxine mesylate binds with high affinity to the GABAA receptor associated Cl- channel. Dihydroergotoxine mesylate also interacts with central dopaminergic and serotonergic receptors. Dihydroergotoxine mesylate displays antiproliferative, antihypertensive and neuroprotective activity.
    Dihydroergotoxine mesylate
  • HY-B0573A
    (S)-(-)-Propranolol hydrochloride
    		Antagonist 99.95%
    (S)-(-)-Propranolol hydrochloride is a β-adrenergic receptor antagonist with log Kd values of -8.16, -9.08, and -6.93 for β1, β2, and β3, respectively. (S)-(-)-Propranolol hydrochloride the active enantiomer of propranolol and can be s used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
    (S)-(-)-Propranolol hydrochloride
  • HY-123012
    Lubabegron
    		Modulator 98.40%
    Lubabegron is a potent modulator of β-adrenergic receptor (β-AR). Lubabegron demonstrates antagonistic behavior at the β1 and β 2 receptor subtypes and agonistic behavior at the β 3 receptor subtype in cattle. Lubabegron reduces NH3 gas emissions from an animal or its waste. Lubabegron is available as an animal supplement.
    Lubabegron
  • HY-129040A
    Iobenguane sulfate
    		Activator 99.78%
    Iobenguane sulfate (MIBG sulfate) is an analogue of the neurotransmitter norepinephrine with antitumor activity. Radioiodinated Iobenguane sulfate is clinically used as a tumor-targeted radiopharmaceutical in the diagnosis and treatment of adrenergic tumors. Iobenguane sulfate is a high-affinity substrate for cholera toxin that interferes with cellular mono(ADP-ribosylation).
    Iobenguane sulfate
  • HY-A0008
    Talipexole dihydrochloride
    		Agonist 99.80%
    Talipexole dihydrochloride (B-HT 920 dihydrochloride) is a dopamine D2 receptor agonist, α2-adrenoceptor agonist and 5-HT3 receptor antagonist, which displays antiParkinsonian activity.
    Talipexole dihydrochloride
  • HY-103213
    JP1302 dihydrochloride
    		Antagonist 99.62%
    JP1302 dihydrochloride is a potent, selective, high affinity antagonist of the α2C-adrenoceptor, with a Kb of 16 nM and a Ki of 28 nM for the human α2C-receptor. JP1302 dihydrochloride shows antidepressant and antipsychotic-like effects. JP1302 dihydrochloride can be used for neuropsychiatric disorders and renal dysfunction research.
    JP1302 dihydrochloride
  • HY-B0391
    Naftopidil
    		Antagonist 98.47%
    Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia.
    Naftopidil
  • HY-17501A
    Bambuterol hydrochloride
    		Agonist 99.93%
    Bambuterol hydrochloride ((±)-Bambuterol hydrochloride; KWD-2183 hydrochloride) is a long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma; it also is a proagent of terbutaline.
    Bambuterol hydrochloride
  • HY-B0702
    Nicergoline
    		Inhibitor 99.31%
    Nicergoline, an ergoline derivative ester of bromonicotinic acid, is a potent, selective and orally active antagonist of α1A-adrenoceptor. Nicergoline has vasodilator effects. Nicergoline also has ameliorative effects on cognitive function in mouse models of Alzheimer's disease.
    Nicergoline
  • HY-B0225
    Methyldopa
    		Agonist 98.25%
    Methyldopa (L-(-)-α-Methyldopa), a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa is a proagent and is metabolized (α-Methylepinephrine) in the central nervous system.
    Methyldopa
  • HY-B1154
    Penbutolol sulfate
    		Antagonist 98.72%
    Penbutolol sulfate ((-)-Terbuclomine) is a potent β-adrenoceptor and 5-HT receptor antagonist with Ki of 11.6 nM and 11.9 nM for 5-HT in rat cornu ammonis 1 (CA1) and human CA3.
    Penbutolol sulfate
  • HY-101336
    RS 17053 hydrochloride
    		Antagonist 99.93%
    RS 17053 hydrochloride is a potent and selective α1A adrenoceptor antagonist, with a pKi value of 9.1 in native cell membrane and a pA2 value of 9.8 in functional assays.
    RS 17053 hydrochloride
  • HY-100543
    Zenidolol
    		Antagonist 99.60%
    Zenidolol (ICI-118551) is a selective β2 adrenergic receptor antagonist. Zenidolol inhibits β2-, β1- and β3-adrenergic receptor with Ki values of 0.7, 49.5 and 611 nM, respectively. Zenidolol can be used as an ocular hypotensive agent used for ophthalmic disease research.
    Zenidolol
  • HY-B0436
    Salbutamol hemisulfate
    		Agonist ≥98.0%
    Salbutamol (Albuterol) hemisulfate is an orally active short-acting β2-adrenergic receptor agonist. Salbutamol hemisulfate promotes tumorigenesis in gastric cancer cells through the β2-AR/ERK/EMT pathway. Salbutamol hemisulfate can relax bronchial smooth muscle and is used to study bronchospasm induced by asthma and chronic obstructive pulmonary disease.
    Salbutamol hemisulfate
  • HY-B0381A
    Betaxolol hydrochloride
    		Inhibitor 99.30%
    Betaxolol Hydrochloride is a selective beta1 adrenergic receptor blocker that can be used for the research of hypertension and glaucoma.
    Betaxolol hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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