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-12707
    Piribedil
    		Antagonist 99.39%
    Piribedil is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil is also a α2-adrenoceptors antagonist. Piribedil can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil has the potential for the research of parkinson's disease, circulatory disorders, cancers.
    Piribedil
  • HY-B1238
    Pronethalol
    		Inhibitor 99.88%
    Pronethalol ((±)-Pronethalo) is a non-selective β-adrenergic antagonist. Pronethalol is a potent inhibitor of Sox2 expression. Pronethalol protects against and to reverse Digitalis-induced ventricular arrhythmias and limits the cerebral arteriovenous malformation (AVMs).
    Pronethalol
  • HY-B1396
    Nefazodone hydrochloride
    		Antagonist 99.94%
    Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity.
    Nefazodone hydrochloride
  • HY-121251
    BI-167107
    		Agonist 99.98%
    BI-167107 is a high affinity, full agonist that binds to the β2 adrenergic receptor (β2AR) with a dissociation constant Kd of 84 pM.
    BI-167107
  • HY-14689
    Ecopipam hydrochloride
    		Antagonist 99.46%
    Ecopipam (SCH 39166) hydrochloride is a potent, selective and orally active antagonist of dopamine D1/D5 receptor, with Kis of 1.2 nM and 2.0 nM, respectively. Ecopipam hydrochloride shows more than 40-flod selectivity over D2, D4, 5-HT, and α2a receptor (Ki=0.98, 5.52, 0.08, and 0.73 μM, respectively). Ecopipam hydrochloride can be used for the research of schizophrenia and obesity.
    Ecopipam hydrochloride
  • HY-101392
    Harmane
    		Inhibitor 99.91%
    Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50 = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).
    Harmane
  • HY-N7142
    DL-Norepinephrine hydrochloride
    		Modulator 99.59%
    DL-Norepinephrine hydrochloride is a synthetic phenylethylamine. DL-Norepinephrine hydrochloride is a neurotransmitter targets α1 and β1 adrenoceptors. DL-Norepinephrine hydrochloride mimics the sympathomimetic actions of the endogenous norepinephrine．DL-Norepinephrine hydrochloride has an increasing effect on subendocardial oxygen tension.
    DL-Norepinephrine hydrochloride
  • HY-14560C
    Reboxetine mesylate
    		Inhibitor 99.87%
    Reboxetine mesylate (FCE20124 mesylate) is a potent, selective, and specific noradrenaline reuptake inhibitor (NARI) for the research of depression. Reboxetine mesylate inhibits the uptake of norepinephrine, with a Ki of 8 nM.
    Reboxetine mesylate
  • HY-B0362A
    Phentolamine mesylate
    		Antagonist 99.90%
    Phentolamine mesylate (Phentolamine methanesulfonate) is a reversible, non-selective, and orally active blocker of α1 and α2 adrenergic receptor that expands blood vessels to reduce peripheral vascular resistance. Phentolamine mesylate can be used for the research of pheochromocytoma-related hypertension, heart failure and erectile dysfunction.
    Phentolamine mesylate
  • HY-A0066A
    Tolazoline hydrochloride
    		Antagonist 99.93%
    Tolazoline hydrochloride (Imidaline hydrochloride) is an α-adrenergic receptor antagonist. Tolazoline hydrochloride inhibits Noradrenaline (HY-13715)-induced cell contraction, modulates vascular resistance, increases arterial pressure, and reverses bradycardia and tachypnea. Tolazoline hydrochloride can be used to study erectile dysfunction, α2-adrenergic receptor agonist-related poisoning, and skin vascular disease research.
    Tolazoline hydrochloride
  • HY-B0371A
    Terazosin hydrochloride dihydrate
    		Antagonist 99.93%
    Terazosin hydrochloride dihydrate is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin hydrochloride dihydrate works by relaxing blood vessels and the opening of the bladder. Terazosin hydrochloride dihydrate has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment.
    Terazosin hydrochloride dihydrate
  • HY-B0098A
    Doxazosin mesylate
    		Antagonist 98.49%
    Doxazosin mesylate (UK 33274 mesylate) is a quinazoline-derivative that selectively antagonizes postsynaptic α1-adrenergic receptors.
    Doxazosin mesylate
  • HY-B1110
    Nomifensine
    		Inhibitor 98.93%
    Nomifensine ((±)-Nomifensine) is a potent norepinephrine (NE) and dopamine (DA) reuptake inhibitor. Nomifensine inhibits uptake of NE, DA and 5-HT in rat brain synaptosomes, with IC50 values of 6.6 nM, 48 nM and 830 nM, and Ki values of 4.7 nM, 26 nM and 4000 nM, respectively. Nomifensine has antidepressant and analgesic effects. Nomifensine is used in neurodegenerative diseases, compound addiction, and pain research.
    Nomifensine
  • HY-B0432
    Propafenone
    		Antagonist 99.64%
    Propafenone (SA-79), a sodium-channel blocker, acts an antiarrhythmic agent. Propafenone also has high affinity for the β receptor (IC50=32 nM). Propafenone blocks the transient outward current (Ito) and the sustained delayed rectifier K current (Isus) with IC50 values of 4.9 μm and 8.6 μm, respectively. Propafenone suppresses esophageal cancer proliferation through inducing mitochondrial dysfunction and induce apoptosis.
    Propafenone
  • HY-107327
    Carazolol
    		Antagonist 99.71%
    Carazolol is a β1/β2 adrenoceptor antagonist of high potency used in the research of hypertension. Carazolol is also a potent, selective β3-adrenoceptor agonist.
    Carazolol
  • HY-N0132
    Synephrine
    		Agonist ≥98.0%
    Synephrine (Oxedrine), an alkaloid, is an α-adrenergic and β-adrenergic agonist derived from the Citrus aurantium. Synephrine is a sympathomimetic compound and can be used for weight loss.
    Synephrine
  • HY-B0659
    Brimonidine
    		Agonist 99.99%
    Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist.
    Brimonidine
  • HY-B0381
    Betaxolol
    		Inhibitor 99.76%
    Betaxolol is a selective beta1 adrenergic receptor blocker that can be used for the research of hypertension and glaucoma.
    Betaxolol
  • HY-N7142S
    DL-Norepinephrine-d6 hydrochloride
    		Modulator 99.75%
    DL-Norepinephrine-d6 (hydrochloride) is the deuterium labeled DL-Norepinephrine hydrochloride. DL-Norepinephrine hydrochloride is a synthetic phenylethylamine that mimics the sympathomimetic actions of the endogenous norepinephrine．DL-Norepinephrine hydrochloride is a neurotransmitter targets α1 and β1 adrenoceptors, has an increasing effect on subendocardial oxygen tension.
    DL-Norepinephrine-d<sub>6</sub> hydrochloride
  • HY-B0006C
    (R)-Carvedilol
    		Inhibitor 99.94%
    (R)-Carvedilol ((R)-BM 14190), the R-enantiomer of Carvedilol, is a non-selective β/α-1 blocker. (R)-Carvedilol exerts protection against the vascular or cardiac toxicity of Doxorubicin (DOX).
    (R)-Carvedilol
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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