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-B0982
    Pindolol
    		Agonist 99.91%
    Pindolol (LB-46) is a nonselective β-blocker with partial beta-adrenergic receptor agonist activity, also functions as a 5-HT1A receptor weak partial antagonist (Ki=33nM).
    Pindolol
  • HY-135878
    2',5'-Dideoxyadenosine
    		Inhibitor 99.93%
    2',5'-Dideoxyadenosine is a potent and non-competitive adenylyl cyclase inhibitor via binding the P-site with an IC50 of 3 µM . 2',5'-Dideoxyadenosine is a nucleoside analog and exerts a potent antiadrenergic action in heart.
    2',5'-Dideoxyadenosine
  • HY-12721
    Clonidine
    		Agonist 99.94%
    Clonidine is an alpha 2-adrenergic agonist.
    Clonidine
  • HY-14300A
    Vilanterol trifenatate
    		Agonist 99.61%
    Vilanterol trifenatate (GW642444 trifenatate) is a long-acting β2-adrenoceptor (β2-AR) agonist with inherent 24-hour activity. The pEC50s for β2-AR, β1-AR and β3-AR are 10.37, 6.98 and 7.36, respectively.
    Vilanterol trifenatate
  • HY-103211
    L748337
    		Inhibitor 99.67%
    L748337 is a potent β3-adrenergic receptor antagonist and displays selectivity over β1 and β2 receptors. The Ki values of L748337 for β3-, β2- and β1-adrenoceptors are 4.0 nM, 204 nM and 390 nM, respectively. L748337 couples predominantly to Gi to activate MAPK signaling and increases phosphorylation of Erk1/2 with pEC50 value of 11.6. L748337 can be used for the research of cancer, nonalcoholic fatty liver disease (NAFLD), and cardiovascular related diseases.
    L748337
  • HY-17416
    Guanfacine hydrochloride
    		Agonist 99.96%
    Guanfacine hydrochloride is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD).
    Guanfacine hydrochloride
  • HY-12380A
    Atipamezole
    		Antagonist 99.84%
    Atipamezole (MPV 1248) is a potent α2-adrenoceptor antagonist with a Ki of 1.6 nM.
    Atipamezole
  • HY-B0566
    Guanabenz Acetate
    		Agonist 98.77%
    Guanabenz (Acetate) (BR-750) is an alpha-2 selective adrenergic agonist used as an antihypertensive agent.
    Guanabenz Acetate
  • HY-B0661
    Tamsulosin
    		Antagonist 99.77%
    Tamsulosin ((R)-(-)-YM12617 free base) is an orally active antagonist of α1-adrenergic receptor. Tamsulosin induces Apoptosis. Tamsulosin is used for the research of prostatic hyperplasia. Tamsulosin attenuates abdominal aortic aneurysm growth and inhibits inflammation in animal models.
    Tamsulosin
  • HY-N0166
    Gramine
    		Agonist 99.80%
    Gramine (Donaxine) is a natural alkaloid isolated from giant reed, acts as an active adiponectin receptor (AdipoR) agonist, with IC50s of 3.2 and 4.2 μM for AdipoR2 and AdipoR1, respectively. Gramine is also a human and mouse β2-Adrenergic receptor (β2-AR) agonist. Gramine (Donaxine) has anti-tumor, anti-viral and anti-inflammatory properties.
    Gramine
  • 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-10122
    Silodosin
    		Antagonist 99.82%
    Silodosin (KAD 3213; KMD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH.
    Silodosin
  • 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-B0409A
    Clonidine hydrochloride
    		Agonist 99.96%
    Clonidine hydrochloride is an agonist of α2-adrenoceptor and potent antihypertensive agent.
    Clonidine hydrochloride
  • HY-10791
    Ritanserin
    		Inhibitor 99.68%
    Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors.
    Ritanserin
  • HY-A0077
    Perphenazine
    		99.95%
    Perphenazine is an orally active dopamine receptor and histamine-1 receptor antagonist, with Ki values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine also binds to Alpha-1A adrenergic receptor. Perphenazine inhibits cancer cell proliferation, and induces apoptosis. Perphenazine can be used in the research of mental disease, cancer, inflammation.
    Perphenazine
  • HY-A0019
    Paliperidone
    		Antagonist 99.43%
    Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia.
    Paliperidone
  • HY-B0659A
    Brimonidine tartrate
    		Agonist 99.57%
    Brimonidine tartrate (UK 14304 tartrate) is a full α2-adrenergic receptor (α2-AR) agonist.
    Brimonidine tartrate
  • HY-B0528A
    Octopamine hydrochloride
    		Agonist 99.90%
    Octopamine ((±)-p-Octopamine) hydrochloride, a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates. Octopamine hydrochloride can stimulate alpha2-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha2-ARs. Octopamine hydrochloride increased glycogenolysis, glycolysis, oxygen uptake, gluconeogenesis and the portal perfusion pressure.
    Octopamine hydrochloride
  • HY-B0527
    Amitriptyline
    		Inhibitor 99.94%
    Amitriptyline is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline has antidepressant activity.
    Amitriptyline
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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