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-12709A
    ARC 239 dihydrochloride
    		Antagonist 99.20%
    ARC 239 dihydrochloride is a selective α2B/2C adrenoceptor antagonist (pKd values are 5.95, 7.41 and 7.56 at α2A, α2B, and α2C receptors respectively). ARC 239 dihydrochloride binds to CHO cell membranes expressing human recombinant a2A-, a2B- or a2C-adrenoceptor subtypes with pKis of 5.6, 8.4, and 7.08, respectively.
    ARC 239 dihydrochloride
  • HY-U00205
    Dopexamine hydrochloride
    		Agonist 98.04%
    Dopexamine hydrochloride is a β2 adrenergic receptor agonist.
    Dopexamine 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-135270
    ADRA1D receptor antagonist 1
    		Antagonist 98.03%
    ADRA1D receptor antagonist 1 is a potent, selective and orally active α1D adrenoceptor antagonist, with a Ki of 1.6 nM.
    ADRA1D receptor antagonist 1
  • 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>
  • HY-101416
    Vanilpyruvic acid
    		98.28%
    Vanilpyruvic acid is a catecholamine metabolite and precursor to vanillactic acid.
    Vanilpyruvic acid
  • HY-12390
    Lofepramine
    		Inhibitor 99.0%
    Lofepramine (Lopramine) is a modified tricyclic and orally active antidepressant. Lofepramine inhibits the uptake of Noradrenaline (NA) (HY-13715) and 5-hydroxytryptamine (5-HT) with IC50s of 2.7 μM and 11 μM, respectively. Lofepramine exerts its antidepressant activity by promoting noradrenergic neurotransmission. Lofepramine also enhances serotonergic neurotransmission by inhibiting neuronal uptake of 5-HT and tryptophan pyrrolase. Lofepramine exhibits significant anxiolytic properties. .
    Lofepramine
  • 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-B0010D
    Arformoterol tartrate
    		Agonist 99.63%
    Arformoterol ((R,R)-Formoterol) tartrate, the (R,R)-enantiomer of Formoterol, is a long-acting β2-adrenergic receptor (β2-AR) agonist, with a Kd of 2.9 nM. Arformoterol tartrate can be used for the research of chronic obstructive pulmonary disease (COPD).
    Arformoterol tartrate
  • HY-139643A
    CXCR7 antagonist-1 hydrochloride
    		Antagonist 99.41%
    CXCR7 antagonist-1 hydrochloride is a CXCR7 antagonist that inhibits the binding of the SDF-1 chemokine (also known as the CXCL12 chemokine) or I-TAC (also known as CXCL11) to the chemokine receptor CXCR7. CXCR7 antagonist-1 hydrochloride is useful in preventing tumor cell proliferation, tumor formation, inflammatory diseases, and many other diseases.
    CXCR7 antagonist-1 hydrochloride
  • HY-100606
    l-Pindolol
    		Agonist 99.89%
    l-Pindolol ((-)-pindolol) is a reversible, competitive and orally active 5-HT1A/1B antagonist. l-Pindolol is a partial β-adrenoceptor agonist. l-Pindolol can be used for the research of neurological disease.
    l-Pindolol
  • HY-14539S2
    Clozapine-d4
    		Inhibitor 99.82%
    Clozapine-d4 is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors.
    Clozapine-d<sub>4</sub>
  • HY-B1231
    Heptaminol hydrochloride
    		98.0%
    Heptaminol (RP-2831) hydrochloride is a vasoconstrictor used in the study of hypotension, especially orthostatic hypotension. Heptaminol is also a skin cancer proliferation inhibitor that inhibits immune inflammation induced by the tumor promoting factor 12-O-tetradecanoylphorbol-13-acetate (TPA) in an NO-dependent manner. Heptaminol also acts as a sympathomimetic amine, exerting indirect sympathetic effects. Heptaminol is also an antagonist of catecholamine release and uptake and can increase intracellular free calcium levels.
    Heptaminol 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-D1606
    BODIPY FL prazosin
    		Inhibitor 99.71%
    BODIPY FL prazosin is a fluorescent α1-adrenergic antagonist with Ki values of 14.5, 43.3 nM for α1a-AR and α1b-AR, respectively. BODIPY FL prazosin also is a fluorescent ligand with the excitation and emission wavelengths are 485 and 535 nm, respectively. BODIPY FL prazosin can be used for study the differences in the subcellular localization of α1-adrenoceptor subtypes.
    BODIPY FL prazosin
  • 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-B1613A
    Clebopride malate
    		Antagonist 99.41%
    Clebopride malate is an orally active dopamine Receptor antagonist. Clebopride malate acts on dopamine D2 receptors and has antiemetic and prokinetic effects. Clebopride malate can be used in the study of functional gastrointestinal disorders.
    Clebopride malate
  • HY-135026
    DL-Norepinephrine tartrate
    		Modulator
    DL-Norepinephrine tartrate is a neurotransmitter, which targets adrenergic receptors, and causes large-amplitude sleep-like electrical activity in the neocortex and suppresses electroencephalography (EEG) activity in the hippocampus. DL-Norepinephrine tartrate results in head shake, difficulty walking, and frequent posture changes in rats model.
    DL-Norepinephrine tartrate
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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