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-101815
    Lidanserin
    		Antagonist ≥98.0%
    Lidanserin (ZK-33839) acts as a 5-HT2A and α1-adrenergic receptor antagonist.
    Lidanserin
  • HY-G0008A
    O-Desmethyl Mebeverine alcohol hydrochloride
    		≥98.0%
    O-Desmethyl Mebeverine alcohol hydrochloride is a metabolite of Mebeverine, which is a potent α1 repector inhibitor, causing relaxation of the gastrointestinal tract.
    O-Desmethyl Mebeverine alcohol hydrochloride
  • HY-118770
    Nafetolol
    		Antagonist 98.24%
    Nafetolol (K 5407), specifically effective on cardiac (β1)-adrenoceptors, is an orally active β blocking agent, with a t1/2 of ~ 2 h in dogs.
    Nafetolol
  • HY-136435
    Mapenterol hydrochloride
    		Agonist 99.56%
    Mapenterol hydrochloride is a type of β2-adrenoceptor agonist.
    Mapenterol hydrochloride
  • HY-17494S
    (Rac)-Timolol-d5 maleate
    		Antagonist ≥99.0%
    rac Timolol-d5 (maleate) is a labelled racemic (S)-Timolol maleate. (S)-Timolol Maleate (L-714,465 Maleate) is a non-cardioselective hydrophilic β-adrenoceptor blocker. (S)-Timolol Maleate is widely used as standard medication for intraocular pressure (glaucoma) by preventing the production of aqueous humor. (S)-Timolol Maleate can be used for hypertension, angina pectoris and myocardial infarction[1][2][3].
    (Rac)-Timolol-d<sub>5</sub> maleate
  • HY-17416A
    Guanfacine
    		Agonist
    Guanfacine 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
  • HY-120296
    5-Methylurapidil
    		Antagonist ≥98.0%
    5-Methylurapidil isα1A‐adrenoceptor antagonist. 5-Methylurapidil can be used for the research of cardiovascular diseases such as hypertension and heart failure.
    5-Methylurapidil
  • 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-B0532
    Trifluoperazine
    		Antagonist
    Trifluoperazine, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine is a potent α1-adrenergic receptor antagonist. Trifluoperazine is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine can be used for the research of schizophrenia. Trifluoperazine acts as a reversible inhibitor of influenza virus morphogenesis.
    Trifluoperazine
  • 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[1].
    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-B1506A
    Acepromazine maleate
    		Antagonist
    Acepromazine (Acetopromazine) maleate is a phenothiazine tranquilizer and is alpha-adrenoceptor antagonist[2.
    Acepromazine maleate
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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