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-P1582A
    ACTH (1-14) (TFA)
    		Activator 99.83%
    ACTH (1-14) (TFA) is a fragment of adrenocorticotrophin, which regulates cortisol and androgen production.
    ACTH (1-14) (TFA)
  • HY-19436
    Solabegron
    		Agonist 99.89%
    Solabegron (GW 427353) is a selective β3-adrenergic receptor agonist, stimulating cAMP accumulation in Chinese hamster ovary cells expressing the human β3-AR, with an EC50 value of 22 nM. Solabegron (GW 427353) is being developed for the treatment of overactive bladder and irritable bowel syndrome.
    Solabegron
  • HY-101355A
    CGP 20712 dihydrochloride
    		Antagonist 99.4%
    CGP 20712 dihydrochloride is a highly selective β1-adrenoceptor antagonist with an IC50 of 0.7 nM. CGP 20712 dihydrochloride exhibits ~10,000-fold selectivity over β2-adrenoceptors.
    CGP 20712 dihydrochloride
  • HY-B0381B
    Levobetaxolol hydrochloride
    		Inhibitor 99.31%
    Levobetaxolol hydrochloride is a beta-adrenergic receptor inhibitor (beta blocker) that can lower the pressure in the eye.
    Levobetaxolol hydrochloride
  • HY-B0194
    Tizanidine
    		Agonist 99.58%
    Tizanidine is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons.
    Tizanidine
  • HY-U00117
    Lusaperidone
    		Antagonist 99.81%
    Lusaperidone (R107474) is an α2 adrenergic receptor antagonist with Kis of 0.13 and 0.15 nM for α2A and α2C, respectively.
    Lusaperidone
  • HY-110033
    Ecopipam hydrobromide
    		Antagonist ≥99.0%
    Ecopipam (SCH 39166) hydrobromide 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 hydrobromide 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 hydrobromide can be used for the research of schizophrenia and obesity.
    Ecopipam hydrobromide
  • HY-B0194S
    Tizanidine-d4
    		Agonist 99.93%
    Tizanidine-d4 is the deuterium labeled Tizanidine. Tizanidine is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons[1][2].
    Tizanidine-d<sub>4</sub>
  • HY-135096
    Amitriptyline-d3 hydrochloride
    		Inhibitor 99.46%
    Amitriptyline-d3 hydrochloride is the deuterium labeled Amitriptyline (hydrochloride). Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity.
    Amitriptyline-d3 hydrochloride
  • HY-119541
    Ampreloxetine
    		Inhibitor 98.49%
    Ampreloxetine (TD-9855) is a potent and orally active norepinephrine (NE) and serotonin 5-HT inhibitor. Ampreloxetine has the potential for the research of neurogenic orthostatic hypotension.
    Ampreloxetine
  • HY-100490B
    Rilmenidine phosphate
    		Agonist ≥98.0%
    Rilmenidine phosphate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate is an alpha 2-adrenoceptor agonist. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
    Rilmenidine phosphate
  • HY-P3557
    Mibenratide
    		Antagonist 99.77%
    Mibenratide, a small cyclic peptide, is an adrenergic β1 receptor antagonist. Mibenratide can be used for heart failure research.
    Mibenratide
  • HY-12710
    Rauwolscine
    		Antagonist 98.27%
    Rauwolscine is a selective α2-adrenoceptor antagonist that inhibits tumor growth and induces apoptosis.
    Rauwolscine
  • 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-B1108R
    Labetalol hydrochloride (Standard)
    		Antagonist 99.94%
    Labetalol (hydrochloride) (Standard) is the analytical standard of Labetalol (hydrochloride). This product is intended for research and analytical applications.
    Labetalol hydrochloride (Standard)
  • HY-B0006S1
    Carvedilol-d4
    		Inhibitor 99.87%
    Carvedilol-d4 is the deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker[1]. 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[2]. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome[3].
    Carvedilol-d<sub>4</sub>
  • HY-B0573BS
    Propranolol-d7
    		Antagonist ≥99.0%
    Propranolol-d7 is the deuterium labeled Propranolol. Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].
    Propranolol-d<sub>7</sub>
  • HY-128515
    Metaterol
    		Agonist
    Metaterol is a beta-adrenergic receptor agonist.
    Metaterol
  • HY-128380
    Dibenamine hydrochloride
    		Antagonist 99.32%
    Dibenamine hydrochloride is a competitive and irreversible adrenergic blocking agent and is known to modify the pharmacological effects of epinephrine. Dibenamine hydrochloride cause a significant increase in the rate of destruction of I-epinephrine in the mouse.
    Dibenamine hydrochloride
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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