1. GPCR/G Protein
  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 (130):

Cat. No. Product Name Effect Purity
  • HY-13951
    ICI 118,551 hydrochloride Antagonist
    ICI 118,551 (hydrochloride) is a highly selective β2 adrenergic receptor antagonist, with Ki values of 0.7, 49.5 and 611 nM for β2, β1 and β3 receptors, respectively.
  • HY-14300A
    Vilanterol trifenatate Agonist
    Vilanterol trifenatate is a long-acting β2-adrenoceptor2-AR) agonist with 24 h activity. The pEC50s for β2-AR,β1-AR and β3-AR is 10.37±0.05, 6.98±0.03 and 7.36±0.03, respectively.
  • HY-17453
    Salmeterol xinafoate Agonist
    Salmeterol(GR 33343X) xinafoate is a long-acting beta2-adrenergic receptor agonist drug that is prescribed for the treatment of asthma and chronic obstructive pulmonary disease(COPD).
  • HY-N0127
    Yohimbine Hydrochloride Antagonist
    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-14773
    Mirabegron Agonist
    Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.
  • HY-14301
    Olodaterol Agonist
    Olodaterol (BI1744) is a long acting β2-adrenoceptor agonist with an EC50 of 1.4±0.08 nM.
  • HY-10122
    Silodosin Antagonist
    Silodosin (Rapaflo; KMD-3213) is an α1-adrenoceptor antagonist with high uroselectivity; In treatment of dysuria.
  • HY-14299
    Indacaterol Agonist
    Indacaterol(Onbrez; Arcapta) is an ultra-long-acting β-adrenoceptor agonist.
  • HY-B0076
    (±)-Bisoprolol (hemifumarate) Inhibitor
    Bisoprolol is a selective type β1 adrenergic receptor blocker.
  • HY-14300
    Vilanterol Agonist
    Vilanterol (GW642444; GW 642444X) is a novel, inhaled, long-acting β(2) agonist with inherent 24-h activity under development as a once-daily combination therapy with an inhaled corticosteroid for COPD and asthma.
  • HY-B0006
    Carvedilol Inhibitor
    Carvedilol(BM14190) is a non-selective beta blocker/alpha-1 blocker with an IC50 of 3.8 μM for inhibition of LDL oxidation.
  • HY-A0008
    B-HT 920 Agonist
    B-HT 920(Talipexole 2Hcl) is a dopamine D2 receptor agonist, α2-adrenoceptor agonist and 5-HT3 receptor antagonist, which displays antiParkinsonian activity.
  • HY-17380
    (S)-Timolol Maleate Antagonist
    (S)-Timolol maleate, is a potent non-selective β-adrenergic receptor antagonist (Ki values are 1.97 and 2.0 nM for β1 and β2 receptor subtypes respectively).
  • HY-B0098A
    Doxazosin mesylate Antagonist
    Doxazosin mesylate(UK 33274) is a quinazoline-derivative that selectively antagonizes postsynaptic α1-adrenergic receptors.
  • HY-11100
    Asenapine maleate Inhibitor
    Asenapine maleate is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and D2 angonist with Ki values of 0.03-4.0 nM, 1.3nM,respectively, and an antipsychotic.
  • HY-17416
    Guanfacine hydrochloride Agonist
    Guanfacine Hcl, an anti-hypertensive agent, is a selective α2A-adrenoceptor agonist with Kd of 31 nM and displays 60-fold selectivity over α2B-adrenoceptors.
  • HY-B0010
    Formoterol Fumarate Agonist
    Formoterol fumarate(Foradil) is a potent, selective and long-acting β2-adrenoceptor agonist.
  • HY-10121
    Asenapine Inhibitor
    Asenapine(Org 5222) inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 nM.
  • HY-14302
    Salmeterol Agonist
    Salmeterol is a long-acting beta2-adrenergic receptor (beta 2AR) agonist used clinically to treat asthma.
  • HY-B0010A
    Formoterol Agonist
    Formoterol(Arformoterol) is a novel highly β2-selective adrenergic agonist and holds promise as a β2-agonist that could impart selective beneficial metabolic effects.