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 (301):

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-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[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-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-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-101392
    Harmane Inhibitor 99.73%
    Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively). Harmane exhibits comutagenic effect[1][2][3][4].
  • HY-131007
    FFN270 hydrochloride
    FFN270 hydrochloride, a fluorescent tracer of norepinephrine, is a fluorescent substrate of the norepinephrine and vesicular monoamine transporters. FFN270 hydrochloride exhibits two resolved absorption/excitation maxima depending on solvent pH (FFN270 ex: 320 nm or 365 nm, em: 475 nm) and can function as ratiometric fluorescent pH-sensors[1].
  • HY-101755
    Tedatioxetine hydrobromide Antagonist 99.98%
    Tedatioxetine (Lu AA24530) hydrobromide acts as a serotonin and norepinephrine (NE)-preferring triple reuptake inhibitor (TRI) and 5-HT2A, 5-HT2C, 5-HT3 and α1A-adrenergic receptor antagonist[1]
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  • HY-13715
    Norepinephrine Agonist
    Norepinephrine (Levarterenol; L-Noradrenaline) 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-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-14541
    Olanzapine Antagonist 99.89%
    Olanzapine (LY170053) is a selective monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic[1][2].
  • HY-B0193A
    Prazosin hydrochloride Antagonist 99.93%
    Prazosin hydrochloride is an alpha-adrenergic blocker and is a sympatholytic drug used to treat high blood pressure and anxiety, PTSD, and panic disorder.
  • 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-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-14773
    Mirabegron Agonist 99.79%
    Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.
  • HY-B0769
    Phenylephrine Agonist
    (R)-(-)-Phenylephrine is a selective α1-adrenoceptor agonist primarily used as a decongestant.
  • HY-17034A
    Dexmedetomidine hydrochloride Agonist 98.54%
    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-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-17503A
    Metoprolol Succinate Inhibitor 99.54%
    Metoprolol Succinate (Toprol XL) is a selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension.