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-B0194S
    Tizanidine-d4
    		Agonist 99.93%
    Tizanidine-d4 is the deuterium labeled Tizanidine (HY-B0194). Tizanidine, a skeletal muscle relaxant, is an orally effective central α2-adrenoceptor agonist (IC50 = 6.9 nmol). Tizanidine primarily exerts muscle relaxation effects by inhibiting the release of excitatory amino acids (glutamate and aspartate) from the presynaptic terminals of spinal cord interneurons. Tizanidine has anti-injury activity and can inhibit gastrointestinal (GI) transport. Tizanidine can inhibit the proliferation, migration, and invasion of lung cancer cells and induce cell apoptosis by upregulating Nischarin and inhibiting the AKT and Wnt3a/β-catenin signaling pathways. Tizanidine can be used to treat spasticity caused by diseases such as multiple sclerosis (MS), stroke, and spinal cord injury (SCI).
    Tizanidine-d<sub>4</sub>
  • HY-12980
    Batefenterol
    		Agonist 99.72%
    Batefenterol (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and β2-adrenoceptor agonist; displays high affinity for hM2, hM3 muscarinic and hβ2-adrenoceptor with Ki values of 1.4, 1.3 and 3.7 nM, respectively.
    Batefenterol
  • HY-101325A
    BRL-37344
    		Agonist
    BRL-37344 (Fosigotifator (THAM sodium)) is a specific β3-adrenergic receptor agonist. BRL-37344 treatment significantly lowers the body weight of obese mice.
    BRL-37344
  • 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-B1435
    Moxisylyte hydrochloride
    		Antagonist 99.65%
    Moxisylyte (hydrochloride) is (alpha 1-blocker) antagonist, it can vasodilates cerebral vessels without reducing blood pressure.
    Moxisylyte hydrochloride
  • HY-100490A
    Rilmenidine hemifumarate
    		Inhibitor 99.82%
    Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an alpha 2-adrenoceptor agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine hemifumarate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
    Rilmenidine hemifumarate
  • HY-P1376A
    G-Protein antagonist peptide TFA
    		Inhibitor
    G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis.
    G-Protein antagonist peptide TFA
  • HY-12706
    Spiroxatrine
    		Antagonist 99.18%
    Spiroxatrine (R 5188) is a selective, dual antagonist of 5-HT1α and α2-adrenergic, with the Ki values of 3.94, 224000, 118.5 nM for 5-HT1α, 5-HT1β and 5-HT2, respectively. Spiroxatrine (R 5188) has a sedative effect.
    Spiroxatrine
  • 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-13713
    LY377604
    		Modulator 99.54%
    LY377604 is a human β3-adrenergic receptor agonist with an EC50 of 2.4 nM and also a β1- and β2-adrenergic receptor antagonist.
    LY377604
  • HY-119802
    Practolol
    		Antagonist 99.80%
    Practolol is a potent and selective β1-adrenergic receptor antagonist. Practolol can be used for the research of cardiac arrhythmias.
    Practolol
  • 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-107398
    1-(2,3-Dichlorophenyl)ethanamine hydrochloride
    		99.93%
    1-(2,3-Dichlorophenyl)ethanamine hydrochloride is a phenylethanolamine N-methyltransferase (PNMT) inhibitor. 1-(2,3-Dichlorophenyl)ethanamine hydrochloride effectively reduces blood pressure of spontaneously hypertensive. 1-(2,3-Dichlorophenyl)ethanamine hydrochloride can be used for the research of blood pressure.
    1-(2,3-Dichlorophenyl)ethanamine hydrochloride
  • 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-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-101416
    Vanilpyruvic acid
    		98.28%
    Vanilpyruvic acid is a catecholamine metabolite and precursor to vanillactic acid.
    Vanilpyruvic acid
  • HY-B0527AR
    Amitriptyline hydrochloride (Standard)
    		Inhibitor
    Amitriptyline (hydrochloride) (Standard) is the analytical standard of Amitriptyline (hydrochloride). This product is intended for research and analytical applications. 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 hydrochloride (Standard)
  • HY-17503R
    Metoprolol (Standard)
    		Antagonist
    Metoprolol (Standard) is the analytical standard of Metoprolol. This product is intended for research and analytical applications. Metoprolol is an orally active, selective β1-adrenoceptor antagonist. Metoprolol shows anti-inflammation, antitumor and anti-angiogenic properties.
    Metoprolol (Standard)
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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