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-137388A
    p-F-HHSiD hydrochloride
    		Antagonist 99.0%
    p-F-HHSiD (p-Fluorohexahydrosiladifenidol) hydrochloride is a potent and selective M3 mAChR antagonist. p-F-HHSiD hydrochloride has antagonistic effects on other subtypes of the M receptor and the alpha1-adrenoceptor. p-F-HHSiD hydrochloride can be used for the researches of cancer, metabolic, neurological and cardiovascular disease such as, colon cancer, Alzheimer’s disease and diabetes.
    p-F-HHSiD hydrochloride
  • HY-14296A
    PF-610355 (hydrochloride)
    		Agonist
    PF-610355 hydrochloride is a β2-adrenergic receptor (β2-AR) full agonist with selectivity for β1-adrenergic receptors. PF-610355 hydrochloride increases intracellular cAMP levels, induces sustained tracheal smooth muscle relaxation, and inhibits acetylcholine-induced bronchoconstriction. PF-610355 hydrochloride can be used in research related to chronic obstructive pulmonary disease, asthma, and respiratory system diseases.
    PF-610355 (hydrochloride)
  • HY-B0556
    Tetrahydrozoline
    		Agonist 99.34%
    Tetrahydrozoline (Tetryzoline), a derivative of imidazoline, is an α-adrenergic agonist that causes vasoconstriction. Tetrahydrozoline is widely used for the research of nasal congestion and conjunctival congestion.
    Tetrahydrozoline
  • HY-B0532AR
    Trifluoperazine dihydrochloride (Standard)
    		Antagonist
    Trifluoperazine (dihydrochloride) (Standard) is the analytical standard of Trifluoperazine (dihydrochloride). This product is intended for research and analytical applications. Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis.
    Trifluoperazine dihydrochloride (Standard)
  • HY-106954
    Upidosin
    		Antagonist 99.48%
    Upidosin (Rec 15/2739) is an α-1 adrenoceptor (α-1 AR) antagonist. Upidosin shows moderate selectivity for the α-1A AR subtype. Upidosin shows uroselectivity in urethra and prostate with a Kb value of 2-3 nM higher than in ear artery and aorta with a Kb value of 20-100 nM. Upidosin inhibits [3H]prazosin binding to cloned human α-1A adrenergic receptor. Upidosin can be used for the research of urethral obstruction.
    Upidosin
  • HY-17501S
    Bambuterol-d9 hydrochloride
    		Agonist 99.88%
    Bambuterol-d9 (hydrochloride) is the deuterium labeled Bambuterol. Bambuterol ((±)-Bambuterol) hydrochloride is a long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma; it also is a prodrug of terbutaline.
    Bambuterol-d<sub>9</sub> hydrochloride
  • HY-P1376A
    G-Protein antagonist peptide TFA
    		Inhibitor
    G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis.
    G-Protein antagonist peptide TFA
  • HY-14296
    PF-610355
    		Agonist
    PF-610355 is a long-acting inhaled β2-adrenoreceptor agonist, with an EC50 of 0.26 nM. PF-610355 has the potential for the study of asthma and COPD.
    PF-610355
  • HY-W685943
    Heptaminol
    		≥98.0%
    Heptaminol is a fatty amine with pressor properties and a potential antihypotension agent. Heptaminol is also a competitive inhibitor of norepinephrine uptake and an inhibitor of nicotine-induced catecholamine release (IC50: 650 μM). Heptaminol does not inhibit norepinephrine release induced by 59 mM K+ but rather inhibits high-affinity Na+-dependent norepinephrine uptake.
    Heptaminol
  • HY-100635S
    Diacetolol-d7
    		Antagonist 99.9%
    Diacetolol-d7 is a deuterium labeled Diacetolol. Diacetolol is the major metabolite of Acebutolol. Diacetolol is a β-adrenoceptor blocking and anti-arrhythmic agent.
    Diacetolol-d<sub>7</sub>
  • HY-12710A
    Rauwolscine hydrochloride
    		Antagonist 99.92%
    Rauwolscine hydrochloride is a potent and specific α2 adrenergic receptor antagonist with a Ki of 12 nM.
    Rauwolscine hydrochloride
  • HY-A0077S1
    Perphenazine-d4
    		98.83%
    Perphenazine-d4 is the deuterium labeled Perphenazine. Perphenazine is a typical antipsychotic agent, inhibits 5-HT2Areceptor, Alpha-1A adrenergic receptor, Dopamine receptor D2/D3, D2L receptor, and Histamine H1 receptor, with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively.
    Perphenazine-d<sub>4</sub>
  • HY-N0166R
    Gramine (Standard)
    		Agonist
    Gramine (Standard) is the analytical standard of Gramine. This product is intended for research and analytical applications. Gramine (Donaxine) is an alkaloid, 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 (Standard)
  • HY-120246
    GS-5759
    		Agonist 99.21%
    GS-5759 is both a β₂-adrenergic receptor agonist and a PDE4 inhibitor. GS-5759 increases intracellular cAMP levels by activating the β₂ receptor, promoting bronchial dilation. GS-5759 inhibits PDE4 activity, reduces cAMP degradation, and enhances anti-inflammatory effects. GS-5759 exhibits potent bronchial dilation and anti-inflammatory capabilities in animal models. GS-5759 can be used for research on respiratory diseases such as chronic obstructive pulmonary disease (COPD).
    GS-5759
  • HY-131105S
    Cimbuterol-d9
    		Agonist
    Cimbuterol-d9 is the deuterium labeled Cimbuterol (HY-131105). Cimbuterol is a β-adrenergic agonist. β-adrenergic agonists act as bronchodilators and tocolytics. β-adrenergic agonists promote growth.
    Cimbuterol-d<sub>9</sub>
  • HY-116790
    (-)-Penbutolol
    		Antagonist 99.74%
    (-)-Penbutolol ((S)-Penbutolol) is a potent 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.
    (-)-Penbutolol
  • HY-A0252
    Bupranolol
    		Antagonist 98.90%
    Bupranolol is an orally active, competitive and non-selective β-adrenoceptor antagonist without intrinsic sympathomimetic activity.
    Bupranolol
  • HY-B1037S3
    Salbutamol-d9 acetate
    		Agonist 99.48%
    Salbutamol-d9 (Albuterol-d9) acetate is the deuterium labeled Salbutamol (HY-B1037). Salbutamol (Albuterol) is an orally active short-acting β2-adrenergic receptor agonist. Salbutamol promotes tumorigenesis in gastric cancer cells through the β2-AR/ERK/EMT pathway. Salbutamol can relax bronchial smooth muscle and is used to study bronchospasm induced by asthma and chronic obstructive pulmonary disease.
    Salbutamol-d<sub>9</sub> acetate
  • HY-179390
    KMCA-0011
    		Antagonist 99.88%
    KMCA-0011 is an orally active ɑ2C adrenoceptor antagonist (Ki = 56.7 nM). KMCA-0011 alleviates depressive behaviors by enhancing BDNF and synaptic plasticity. KMCA-0011 displays favorable metabolic stability, including high plasma stability (99.8% after 120 min). KMCA-0011 can be used for the research of depression.
    KMCA-0011
  • HY-B1675
    Levalbuterol
    		Agonist 99.79%
    Levalbuterol ((R)-Albuterol; (R)-Salbutamol) is a short-acting β2-adrenergic receptor agonist and the active (R)-enantiomer of Salbutamol. Levalbuterol is a more potent bronchodilator than Salbutamol and has the potential for the treatment of COPD.
    Levalbuterol
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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