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 (641):

Cat. No. Product Name Effect Purity
  • HY-13715
    Norepinephrine Agonist
    Norepinephrine (Levarterenol; L-Noradrenaline) is a potent adrenergic receptor (AR) agonist. Norepinephrine activates α1, α2, β1 receptors[1][2][3][4].
  • 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
    Zenidolol hydrochloride Antagonist 99.76%
    Zenidolol (ICI-118551) 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-B0769
    Phenylephrine Agonist
    (R)-(-)-Phenylephrine is a selective α1-adrenoceptor agonist primarily used as a decongestant.
  • HY-B0468
    Isoprenaline hydrochloride Agonist 99.86%
    Isoprenaline (Isoproterenol) hydrochloride is a non-selective, orally active β-adrenergic receptor agonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma[1][2][3][4][5][6].
  • HY-103216A
    RWJ52353 hydrochloride Agonist
    RWJ-52353 hydrochloride is an orally potent, highly selective α2D adrenergic receptor agonist (Ki: 1.5 nM) with potential analgesic effects. RWJ-52353 hydrochloride demonstrated analgesic activity in abdominal tests in rats and mice, and improved agitation in mice in the hot plate test and tail flick test. RWJ-52353 hydrochloride also regulates the organic cation transporter (OCT) subtype, inhibiting rOCT1 and rOCT2 with IC50s of 100 μM and 20 μM respectively; it also activates rOCT3, affecting [3H]-1- in cells. Methyl-4-phenylpyridinium ([3H]MPP) transport[1][2].
  • HY-112658
    p-Iodoclonidine hydrochloride Agonist
    p-Iodoclonidine hydrochloride is a partial agonist of α2-adrenergic receptor. p-Iodoclonidine hydrochloride also has minimal agonist activity in inhibiting adenylate cyclase in platelet membranes, and potentiates ADP induced platelet aggregation with an EC50 of 1.5 μM[1].
  • HY-135014
    Undecylenoyl phenylalanine Antagonist
    Undecylenoyl phenylalanine is an antagonist for α-melanocyte-stimulating hormone (MSH) and β-adrenergic receptor (β-ADR) to reduce the melanogenesis in melanocytes, reduces hyperpigmentation and thus ameliorates melasma lesions and solar lentigines[1].
  • HY-14299S
    Indacaterol-d3 Agonist
    Indacaterol-d3 is deuterium labeled Indacaterol.
  • 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[1][2].
  • HY-B0391S1
    Naftopidil-d5 Antagonist
    Naftopidil-d5 is deuterium labeled Naftopidil. Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia[1][2].
  • HY-B1392S
    Esmolol-d7 hydrochloride Inhibitor
    Esmolol-d7 (hydrochloride) is the deuterium labeled Esmolol hydrochloride. Esmolol hydrochloride is a beta adrenergic receptor blocker[1][2].
  • HY-12961A
    Bretylium tosylate 98.39%
    Bretylium (tosylate) is an inhibitor of the presynaptic release of vasoconstrictor neurotransmitters.
  • HY-112074
    Tiamenidine Agonist
    Tiamenidine (HOE 440) is an orally active α2-adrenergic receptor agonist with antihypertensive effect. Tiamenidine is used as an antihypertensive agent for hypertension research[1].
  • HY-12760S
    Indoramin-d5 Antagonist
    Indoramin-d5 is deuterium labeled Indoramin, which is a piperidine antiadrenergic agent.
  • HY-105124S
    Bufuralol-d9 hydrochloride
    Bufuralol-d9 (hydrochloride) is the deuterium labeled Bufuralol hydrochloride[1].
  • HY-14773
    Mirabegron Agonist 99.90%
    Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.
  • HY-120829S
    Bisoprolol-d5 hemifumarate
    Bisoprolol-d5 (hemifumarate) is deuterium labeled Bisoprolol (fumarate).
  • HY-B0527AS
    Amitriptyline-d6 hydrochloride Inhibitor 99.65%
    Amitriptyline-d6 (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[1][2][3].
  • HY-131104S
    Brombuterol-d9 Agonist
    Brombuterol-d9 is a deuterium labeled Brombuterol. Brombuterol is a β-adrenergic receptor agonist[1].