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-105124
    Bufuralol
    		Antagonist 99.25%
    Bufuralol (Ro 3-4787) is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity. Bufuralol hydrochloride is a CYP2D6 probe substrate.
    Bufuralol
  • HY-121251
    BI-167107
    		Agonist 99.61%
    BI-167107 is a high affinity, full agonist that binds to the β2 adrenergic receptor (β2AR) with a dissociation constant Kd of 84 pM.
    BI-167107
  • HY-B0431A
    Phenoxybenzamine hydrochloride
    		Antagonist 99.53%
    Phenoxybenzamine hydrochloride is a nonselective, irreversible, orally active α-adrenoceptor antagonist that is commonly used for the research of hypertension, specifically caused by pheochromocytoma. Phenoxybenzamine hydrochloride also shows antitumor activity.
    Phenoxybenzamine hydrochloride
  • HY-101392
    Harmane
    		Inhibitor 99.91%
    Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50 = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).
    Harmane
  • HY-103210
    DSP-4 hydrochloride
    		98.0%
    DSP-4 hydrochloride is a highly and selective adrenergic neurotoxin. DSP-4 hydrochloride can cross the blood brain barrier. DSP-4 hydrochloride can be used for the temporary selective degradation of the central and peripheral noradrenergic neurons.
    DSP-4 hydrochloride
  • HY-13715R
    Norepinephrine (Standard)
    		Agonist
    Norepinephrine (Standard) is the analytical standard of Norepinephrine. This product is intended for research and analytical applications. Norepinephrine (Levarterenol; L-Noradrenaline) is a potent adrenergic receptor (AR) agonist. Norepinephrine activates α1, α2, β1 receptors.
    Norepinephrine (Standard)
  • HY-B0203
    Nebivolol
    		Inhibitor 99.94%
    Nebivolol (R 065824) is an orally active beta receptor blocker and has the high beta(1)-receptor affinity. Nebivolol has direct vasodilator properties and adrenergic blocking characteristics. Nebivolol can be used for the research of kinds of diseases such as hypertension, coronary artery disease, congestive heart failure and ischemic heart disease.
    Nebivolol
  • HY-14301
    Olodaterol
    		Agonist 99.85%
    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-128483
    Fusaric acid
    		Inhibitor 99.94%
    Fusaric acid is an orally active multi-pathway inhibitor with the activity of inducing oxidative stress and apoptosis. Fusaric acid can chelate divalent metal cations, damage mitochondrial membrane structure, and activate apoptosis-related proteases such as Caspase-3/7, -8, and -9. Fusaric acid also regulates Bax/Bcl-2 protein, inhibits fibrosis-related signaling pathways such as NF-κB, TGF-β1/SMADs, and PI3K/AKT/mTOR, and reduces collagen deposition. Fusaric acid is also a dopamine β-hydroxylase inhibitor, which reduces endogenous levels of norepinephrine and epinephrine in the brain, heart, spleen, and adrenal glands. Fusaric acid can play a role in myocardial fibrosis and improve cardiac hypertrophy in heart disease, and can also be used in the study of esophageal cancer and liver cancer.
    Fusaric acid
  • HY-B0076
    Bisoprolol hemifumarate
    		Inhibitor 99.84%
    Bisoprolol hemifumarate is a potent, selective and orally active β1-adrenergic receptor blocker with little activity on β2-receptor. Bisoprolol hemifumarate has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.
    Bisoprolol hemifumarate
  • HY-B0098
    Doxazosin
    		Antagonist 99.85%
    Doxazosin (UK 33274) is a quinazoline-derivative that selectively antagonizes postsynaptic α1-adrenergic receptors.
    Doxazosin
  • HY-17034B
    Medetomidine hydrochloride
    		Agonist 99.87%
    Medetomidine hydrochloride is an orally active α2-adrenoceptor agonist (Ki: 1.08 nM). Medetomidine hydrochloride has sedative and analgesic effects. Medetomidine hydrochloride can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels.
    Medetomidine hydrochloride
  • HY-B0432
    Propafenone
    		Antagonist 99.96%
    Propafenone (SA-79), a sodium-channel blocker, acts an antiarrhythmic agent. Propafenone also has high affinity for the β receptor (IC50=32 nM). Propafenone blocks the transient outward current (Ito) and the sustained delayed rectifier K current (Isus) with IC50 values of 4.9 μm and 8.6 μm, respectively. Propafenone suppresses esophageal cancer proliferation through inducing mitochondrial dysfunction and induce apoptosis.
    Propafenone
  • HY-139643
    CXCR7 antagonist-1
    		Antagonist 99.85%
    CXCR7 antagonist-1 is a CXCR7 antagonist that inhibits the binding of the SDF-1 chemokine (also known as the CXCL12 chemokine) or I-TAC (also known as CXCL11) to the chemokine receptor CXCR7. CXCR7 antagonist-1 is useful in preventing tumor cell proliferation, tumor formation, inflammatory diseases, and many other diseases.
    CXCR7 antagonist-1
  • HY-N0761
    Isoferulic acid
    		Inhibitor 99.91%
    Isoferulic acid (3-Hydroxy-4-methoxycinnamic acid) is an orally active cinnamic acid derivative. Isoferulic acid exhibits hypoglycemic, antiviral, and antioxidant activities. Isoferulic acid can also inhibit fructose- and glucose-mediated protein glycation. Isoferulic acid can be used in the research of diseases such as diabetes.
    Isoferulic acid
  • HY-118470
    Butaxamine hydrochloride
    		Inhibitor 99.87%
    Butaxamine (Butoxamin) hydrochloride is a specific β2-adrenergic receptor blocker. Butaxamine hydrochloride inhibits the decreases in urine volume in ethanol-anesthetized, water-diuretic rats.
    Butaxamine hydrochloride
  • HY-B2233
    Phosphorylcholine chloride
    		Agonist 99.95%
    Phosphorylcholine chloride (Phosphocholine chloride) is the main phospholipid component in eukaryotic biofilms. Phosphorylcholine chloride exists in commensal or pathogenic bacteria associated with eukaryotes in prokaryotes. Phosphorylcholine chloride exhibits a surprising range of immunomodulatory properties.
    Phosphorylcholine chloride
  • HY-13458
    Droxidopa
    		99.72%
    Droxidopa (L-DOPS; SM5688) is a potent, orally active norepinephrine precursor. Droxidopa increases standing blood pressure, ameliorates symptoms of orthostatic hypotension and improves standing ability. Droxidopa has the potential for the research of neurogenic orthostatic hypotension (nOH) and alternative ADHD (attention deficit hyperactivity disorder).
    Droxidopa
  • HY-19334
    L755507
    		Agonist 98.89%
    L755507 is a potent, selective agonist of β3-AR with an IC50 of 35 nM. L755507 enhances the homology-directed repair (HDR)-mediated genome editing.
    L755507
  • HY-101385
    L-765314
    		Agonist 99.92%
    L-765314 is a potent and selective α1b adrenergic receptor antagonist with Kis of 5.4 nM and 2.0 nM for rat and human α1b adrenergic receptor, respectively.
    L-765314
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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