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-14561
    Idazoxan
    		Antagonist
    Idazoxan (RX 781094) is a potent antagonist of α2 adrenergic receptor (α2AR) and potential I2 imidazoline receptor agonist. Idazoxan can be used in the research of antidepression and schizophrenia. Idazoxan has oral bioactivity.
    Idazoxan
  • HY-176742
    ATR-258
    		Agonist
    ATR-258 is a GRK2-biased β2AR partial agonist. ATR-258 is a competitive β1AR antagonist and shows weak partial agonist activity at β3AR at 10 μM. ATR-258 promotes glucose control and decreases lipid accumulation in obese mice with reduced side effects. ATR-258 can be used for T2DM research.
    ATR-258
  • HY-B1481A
    Isoetharine
    		Agonist
    Isoetharine (Isoetarine) is an orally active selective agonist of β-adrenergic receptors. Isoetharine is a catechol-like agent and catechol O-methyltransferase (COMT) mediates its methylation. Isoetharine can promote the production of cAMP which stimulates the relaxation of smooth muscle cells and can be used as an emphysema, bronchitis and bronchodilator.
    Isoetharine
  • HY-17494A
    Timolol hemihydrate
    		Inhibitor
    Timolol (hemihydrate) is a β-blocker available for both topical and systemic administration. Timolol (hemihydrate) is primarily used to reduce intraocular pressure with open-angle glaucoma and ocular hypertension and Timolol (hemihydrate) also has cardioprotective effect.
    Timolol hemihydrate
  • HY-151198
    CHF-6366
    		Agonist
    CHF-6366 is a potent M3 muscarinic antagonist and β2-adrenergic receptors agonist with pKi values of 10.4 and 11.4, respectively. CHF-6366 is also a weak calcium channel inhibitor (IC50~50 μM). CHF-6366 inhibits bronchoconstriction in guinea pigs. CHF-6366 can be used to research chronic obstructive pulmonary disease (COPD).
    CHF-6366
  • HY-B0659AS
    Brimonidine-d4 D-tartrate
    		≥99.0%
    Brimonidine-d4 (D-tartrate) is the deuterium labeled Brimonidine D-tartrate.
    Brimonidine-d<sub>4</sub> D-tartrate
  • HY-13575A
    Blonanserin dihydrochloride
    		Antagonist
    Blonanserin dihydrochloride is a potent and orally active 5-HT2A and dopamine D2 receptor antagonist, with Ki values of 0.812 and 0.142 nM, respectively. Blonanserin dihydrochloride is usually acts as an atypical antipsychotic agent, and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension.
    Blonanserin dihydrochloride
  • HY-120408
    (±)-Scopolamine
    		Antagonist
    (±)-Scopolamine (Atroscine) is the racemic modification of Scopolamine. (±)-Scopolamine inhibits α-adrenergic receptor activity. (±)-Scopolamine has Ki values of 33 μM and 7.25 nM for α1-adrenerg receptor and muscarinic cholinergic receptor, respectively.
    (±)-Scopolamine
  • HY-B1615
    Clenbuterol
    		Agonist
    Clenbuterol (NAB-365) is a β2-adrenergic receptor agonist with an EC50 of 31.9 nM. Clenbuterol is a very potent inhibitor of the lipopolysaccharide (LPS)-induced release of TNF-α and IL-1β. Clenbuterol can inhibit the inflammatory process. Clenbuterol is a bronchodilator.
    Clenbuterol
  • HY-17494
    Timolol
    		Inhibitor
    Timolol is a β-blocker available for both topical and systemic administration. Topical Timolol is primarily used to reduce intraocular pressure with open-angle glaucoma and ocular hypertension. Timolol can also be used for the research of infantile hemangiomas, hypertension, myocardial infarction, migraine prophylaxis, and atrial fibrillation.Timolol also has cardioprotective effect.
    Timolol
  • HY-14560A
    (R,R)-Reboxetine mesylate
    (R,R)-Reboxetine mesylate is an antidepressant agent with great bioavailability. (R,R)-Reboxetine is the enantiomer of Reboxetine, which is a selective noradrenaline reuptake inhibitor. Reboxetine consists of (R,R) and (S,S) enantiomer, has low affinity for alpha-adrenergic and muscarinic receptors and low toxicity in animals.
    (R,R)-Reboxetine mesylate
  • HY-B1298A
    Methoxamine
    		Agonist
    Methoxamine is a selective alpha1-adrenergic receptor agonist. Methoxamine causes vasoconstriction and increased peripheral vascular resistance. Methoxamine hydrochloride significantly increased the overflow of ATP, ADP and AMP, but not adenosine, by a prazosin-sensitive mechanism in the rabbit pulmonary artery.
    Methoxamine
  • HY-103196
    Sotalol
    		Inhibitor
    Sotalol is an orally active, non-selective β-adrenergic receptor blocker. Sotalol is a potent antiarrhythmic agent that can be used for the research of pediatric arrhythmias. Sotalol blocks β-receptors, and potassium KCNH2 channels. Antiepileptic Agent.
    Sotalol
  • HY-148804A
    Vemtoberant mesylate
    		Antagonist
    Vemtoberant mesylate is an β3 Adrenergic Receptor antagonist. Vemtoberant mesylate can be used for research of β3 adrenergic receptor-mediated disorder, such as, heart failure.
    Vemtoberant mesylate
  • HY-15746A
    Dobutamine
    		Agonist
    Dobutamine is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine can increase cardiac output and correct hypoperfusion.
    Dobutamine
  • HY-101514
    β3-AR agonist 1
    		Agonist
    β3-AR agonist 1 (compound 15) is a highly potent, selective, and orally available β3-adrenergic receptor (β3-AR) agonist (EC50=18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold).
    β3-AR agonist 1
  • HY-B0532B
    Trifluoperazine dimaleate
    		Antagonist
    Trifluoperazine dimaleate, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dimaleate is a potent α1-adrenergic receptor antagonist. Trifluoperazine dimaleate is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dimaleate is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dimaleate can be used for the research of schizophrenia. Trifluoperazine dimaleate acts as a reversible inhibitor of influenza virus morphogenesis.
    Trifluoperazine dimaleate
  • HY-15746B
    Dobutamine tartrate
    		Agonist
    Dobutamine tartrate is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine tartrate is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine tartrate can increase cardiac output and correct hypoperfusion.
    Dobutamine tartrate
  • HY-105124S
    Bufuralol-d9 hydrochloride
    Bufuralol-d9 (hydrochloride) is the deuterium labeled Bufuralol hydrochloride.
    Bufuralol-d<sub>9</sub> hydrochloride
  • HY-116790BS
    (±)-Penbutolol-d9
    (±)-Penbutolol-d9 is the deuterium labeled (±)-Penbutolol.
    (±)-Penbutolol-d<sub>9</sub>
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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