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-135490
    Reproterol
    		Agonist
    Reproterol is a dual acting β2-adrenoceptor agonist and PDE inhibitor. The theophylline constituent of Reproterol inhibits phosphodiesterase activity induced by adenylyl cyclase. Reproterol has the potential for asthma research.
    Reproterol
  • HY-B0527AR
    Amitriptyline hydrochloride (Standard)
    		Antagonist
    Amitriptyline hydrochloride (Standard) is the analytical standard of Amitriptyline hydrochloride (HY-B0527A). This product is intended for research and analytical applications. Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
    Amitriptyline hydrochloride (Standard)
  • HY-14304A
    Zinterol hydrochloride
    		Agonist 99.51%
    Zinterol hydrochloride (MJ 9184 hydrochloride) is a potent and selective β2-adrenoceptor agonist. Zinterol hydrochloride increases ICa in a concentration-dependent manner with an EC50 of 2.2 nM. Zinterol hydrochloride induces ventricular arrhythmias in conscious heart failure rabbits.
    Zinterol hydrochloride
  • HY-W376701
    Guanadrel
    		Inhibitor 98.94%
    Guanadrel is an orally active postganglionic adrenergic inhibitor of spiroketal. Guanadre can be used in anti-hypertensive studies.
    Guanadrel
  • HY-123268A
    Ro 363 hydrochloride
    		Agonist
    Ro 363 hydrochloride, an effective inotropic stimulant, is a potent and highly selective β1-adrenoceptor agonist. Ro 363 hydrochloride is a cardiovascular modulator that reduces diastolic blood pressure and pronounces increases in myocardial contractility.
    Ro 363 hydrochloride
  • HY-N0132A
    Synephrine hydrochloride
    		Agonist 99.66%
    Synephrine (Oxedrine) hydrochloride, an alkaloid, is an α-adrenergic and β-adrenergic agonist derived from the Citrus aurantium. Synephrine hydrochloride is a sympathomimetic compound and can be used for weight loss.
    Synephrine hydrochloride
  • HY-A0142A
    Dapiprazole hydrochloride
    		Antagonist 99.87%
    Dapiprazole hydrochloride is a potent, selective and orally active alpha-1 adrenoceptor antagonist. Dapiprazole hydrochloride suppresses the opioid withdrawal symptoms. Dapiprazole hydrochloride is also used as eye drops for reversing mydriasis.
    Dapiprazole hydrochloride
  • HY-B0163A
    Detomidine hydrochloride
    		Agonist 99.83%
    Detomidine hydrochloride, an imidazole derivative, is a potent α2-adrenergic agonist. Detomidine hydrochloride produces dose-dependent analgesic effects.
    Detomidine hydrochloride
  • HY-B0354A
    Urapidil hydrochloride
    		Antagonist 99.97%
    Urapidil hydrochloride is an orally active α1-adrenoceptor antagonist and 5-HT1A receptor agonist with a pIC50 of 6.13 and 4.38 against α1- and α2-adrenoceptor, respectively. Urapidil hydrochloride shows antihypertensive effect.
    Urapidil hydrochloride
  • HY-12720A
    Apraclonidine hydrochloride
    		Agonist 98.96%
    Apraclonidine hydrochloride (ALO 2145), a selective α2 and weak α1 receptor agonist activity, effectively lowers intraocular pressure (IOP) in human eyes. Apraclonidine hydrochloride is a topical ophthalmic solution and has the ability to elevate the eye lid.
    Apraclonidine hydrochloride
  • HY-101393A
    CGP 12177 hydrochloride
    		Modulator 99.69%
    CGP 12177 ((±)-CGP 12177) hydrochloride is a β Adrenergic Receptor Ligand. CGP 12177 hydrochloride is a high affinity antagonist of β1- and β2-AR. CGP 12177 hydrochloride is also shown to interact, with a lower affinity, with the β3-AR and to exhibit a partial agonist activity on rodent and human β3-AR. CGP 12177 hydrochloride exhibits partial agonist properties for α1-AR in rat pulmonary artery.
    CGP 12177 hydrochloride
  • HY-12749
    Midodrine
    		99.67%
    Midodrine is a selective and orally active adrenergic α1-receptor agonist. Midodrine can strengthen vascular contraction. Midodrine can be used for the researches of cardiovascular disease, such as orthostatic hypotension.
    Midodrine
  • HY-B0769R
    Phenylephrine (Standard)
    		Agonist
    Phenylephrine (Standard) is the analytical standard of Phenylephrine. This product is intended for research and analytical applications. (R)-(-)-Phenylephrine is a selective α1-adrenoceptor agonist primarily used as a decongestant.
    Phenylephrine (Standard)
  • HY-15477A
    YS-49 monohydrate
    		Activator 99.56%
    YS-49 (monohydrate) is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
    YS-49 monohydrate
  • HY-B1111
    Amitraz
    		Agonist 99.65%
    Amitraz is a non-systemic acaricide and insecticide with alpha-adrenergic agonist activity that interacts with octopamine receptors in the central nervous system and inhibits monoamine oxidase and prostaglandin synthesis.
    Amitraz
  • HY-B0527AS
    Amitriptyline-d6 hydrochloride
    		Antagonist 99.65%
    Amitriptyline-d6 hydrochloride is the deuterium labeled Amitriptyline hydrochloride (HY-B0527A). Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
    Amitriptyline-d<sub>6</sub> hydrochloride
  • HY-12710
    Rauwolscine
    		Antagonist 98.27%
    Rauwolscine is a selective α2-adrenoceptor antagonist that inhibits tumor growth and induces apoptosis.
    Rauwolscine
  • HY-111326A
    Naphazoline nitrate
    		Agonist 99.12%
    Naphazoline (Naphthazoline) nitrate is an α-adrenergic receptor agonist. Naphazoline nitrate reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline nitrate reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF. Naphazoline nitrate can be used for non-bacterial conjunctivitis research.
    Naphazoline nitrate
  • HY-135119
    Salmeterol-d3
    		Inhibitor 98.91%
    Salmeterol-d3 is a deuterium labeled Salmeterol. Salmeterol is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively.
    Salmeterol-d<sub>3</sub>
  • HY-B0006S1
    Carvedilol-d4
    		Inhibitor 99.80%
    Carvedilol-d4 is the deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome.
    Carvedilol-d<sub>4</sub>
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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