1. GPCR/G Protein
    Neuronal Signaling
  2. 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 (346):

Cat. No. Product Name Effect Purity
  • HY-B0468
    Isoprenaline hydrochloride Agonist
    Isoprenaline hydrochloride is a non-selective β-adrenergic receptor agonist with potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities.
  • 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[1]. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].
  • 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-13715
    Norepinephrine Agonist
    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-B1562C
    Bopindolol fumarate Antagonist
    Bopindolol ((±)-Bopindolol) fumarate is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol fumarate is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol fumarate is a prodrug of pindolol and can be used for essential and renovascular hypertension research[1][2].
  • HY-120802
    Navafenterol Agonist
    Navafenterol (AZD-8871) is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile[1].
  • HY-103212
    Azepexole dihydrochloride Agonist
    Azepexole (B-HT 933) dihydrochloride is a potent and selective alpha 2-adrenoceptor agonist with pKis of 8.3, 7.6, and 7.5 for α2A-, α2B- and α2C-adrenoceptor subtypes, resepctively[1]. Azepexole dihydrochloride causes concentration-dependent inhibition of peristaltic contractions (IC50= 78.72 nM)[2].
  • HY-B0769
    Phenylephrine Agonist
    (R)-(-)-Phenylephrine is a selective α1-adrenoceptor agonist primarily used as a decongestant.
  • HY-13715B
    Norepinephrine bitartrate monohydrate Agonist
    Norepinephrine bitartrate monohydrate (Levarterenol bitartrate monohydrate; L-Noradrenaline bitartrate monohydrate) is a β1-selective adrenergic receptor agonist with EC50 of 5.37 μM.
  • 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
    CL316243 is a highly potent selective β3-adrenoceptor agonist with a EC50 of 3 nM, but is an extremely poor to β1/2- receptors[1].CL316243 is a effective stimulant of adipocyte lipolysis and increases brown adipose tissue thermogenesis and metabolic rate[2]. CL316243 has the potential for the treatment obesity, diabetes and urge urinary incontinence[3].
  • 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[1]. Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC50 of 0.15 nM[2].Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC50s of 1.8, and 13 μM, respectively[3].
  • 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[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].
  • 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[1][2].
  • 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[1][2][3].
  • 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[1][2][3].
  • 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[1][2][3].
  • HY-14773
    Mirabegron Agonist 99.79%
    Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.