1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. Adrenergic Receptor

Adrenergic Receptor

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 Related Products (337):

Cat. No. Product Name Effect Purity
  • HY-B0468
    Isoprenaline hydrochloride
    Agonist ≥99.0%
    Isoprenaline hydrochloride is a non-selective β-adrenergic receptor agonist with potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities.
  • HY-13951
    ICI 118,551 hydrochloride
    Antagonist 99.64%
    ICI 118,551 (hydrochloride) is a highly selective β2 adrenergic receptor antagonist, with Kis of 0.7, 49.5 and 611 nM for β2, β1 and β3 receptors, respectively.
  • HY-B0573
    Propranolol hydrochloride
    Antagonist
    Propranolol hydrochloride 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. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
  • HY-13715
    Norepinephrine
    Agonist ≥98.0%
    Norepinephrine (Levarterenol; L-Noradrenaline) is a β1-selective adrenergic receptor agonist with EC50 of 5.37 μM.
  • HY-B0471
    Phenylephrine hydrochloride
    Agonist 99.95%
    (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
  • HY-103211
    L748337
    Inhibitor 98.02%
    L748337 is a potent β3-adrenergic receptor antagonist and displays selectivity over β1 and β2 receptors. The Ki values of L748337 for β3-, β2- and β1-adrenoceptors are 4.0 nM, 204 nM and 390 nM, respectively. L748337 couples predominantly to Gi to activate MAPK signaling and increases phosphorylation of Erk1/2 with pEC50 value of 11.6. L748337 can be used for the research of cancer, nonalcoholic fatty liver disease (NAFLD), and cardiovascular related diseases.
  • HY-14301
    Olodaterol
    Agonist 98.37%
    Olodaterol (BI1744) is a selective, long acting β2-adrenoceptor2-AR) agonist (EC50=0.1 nM and pKi= 9.14 for human β2-adrenoceptor, respectively). Olodaterol can be used for chronic obstructive pulmonary disease (COPD) and pulmonary fibrosis.
  • HY-19933
    Vibegron
    Agonist 98.26%
    Vibegron (MK-4618) is a potent, highly selective β3-adrenoceptor agonist (EC50=1.1 nM). Vibegron can be used for severe urgency urinary incontinence related to overactive bladder.
  • HY-13715B
    Norepinephrine bitartrate monohydrate
    Agonist ≥98.0%
    Norepinephrine bitartrate monohydrate (Levarterenol bitartrate monohydrate; L-Noradrenaline bitartrate monohydrate) is a β1-selective adrenergic receptor agonist with EC50 of 5.37 μM.
  • HY-B0769
    Phenylephrine
    Agonist ≥98.0%
    (R)-(-)-Phenylephrine is a selective α1-adrenoceptor agonist primarily used as a decongestant.
  • HY-12987
    Pimozide
    Antagonist 99.88%
    Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
  • HY-116771A
    CL 316243
    Agonist ≥98.0%
    CL316243 is a highly potent selective β3-adrenoceptor agonist with a EC50 of 3 nM, but is an extremely poor to β1/2- receptors.CL316243 is a effective stimulant of adipocyte lipolysis and increases brown adipose tissue thermogenesis and metabolic rate. CL316243 has the potential for the treatment obesity, diabetes and urge urinary incontinence.
  • HY-B0193A
    Prazosin hydrochloride
    Antagonist 99.93%
    Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders. Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC50 of 0.15 nM.Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC50s of 1.8, and 13 μM, respectively.
  • HY-N0127
    Yohimbine Hydrochloride
    Antagonist 99.69%
    Yohimbine Hydrochloride is an alpha 2-adrenoreceptor antagonist, blocking the pre- and postsynaptic alpha-2 adrenoreceptors and causing an increased release of noradrenaline and dopamine.
  • HY-B0006
    Carvedilol
    Inhibitor 99.85%
    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.
  • HY-17498
    Atenolol
    Antagonist 99.61%
    Atenolol ((RS)-Atenolol) is a cardioselective β1-adrenergic receptor blocker, with a Ki of 697 nM atβ1-adrenoceptor in guine pig left ventricle membrane. Atenolol can be used for the research of hypertension and angina pectoris.
  • HY-15477
    YS-49
    Activator 98.65%
    YS-49 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.
  • HY-17034A
    Dexmedetomidine hydrochloride
    Agonist 99.39%
    Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine hydrochloride shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine hydrochloride exhibits anxiolysis, sedation, and modest analgesia effects.
  • HY-14773
    Mirabegron
    Agonist 99.79%
    Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.
  • HY-B0527A
    Amitriptyline hydrochloride
    Inhibitor 99.56%
    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.
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