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

Adrenergic Receptor

Beta Receptor

Adrenergic Receptor

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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 Isoform Specific Products:

Adrenergic Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-A0267
    Bitolterol
    		Agonist
    Bitolterol is a β2-adrenergic agonist with bronchodilator activity. Bitolterol is classified as a prodrug and is primarily used for the suppression of respiratory diseases. Bitolterol is considered safe for use during breastfeeding, as the amount that can enter breast milk is very limited.
    Bitolterol
  • HY-12980A
    Batefenterol Succinate
    		Agonist
    Batefenterol Succinate (GSK961081 Succinate) is a first-of-its-kind inhaled bifunctional bronchodilator with smooth muscle relaxant properties. The activities of Batefenterol Succinate include acting as a smooth muscle parasympathetic antagonist and a beta2-adrenoceptor agonist. Batefenterol Succinate is used to improve respiratory function, especially in patients with chronic obstructive pulmonary disease (COPD).
    Batefenterol Succinate
  • HY-14299D
    Indacaterol acetate
    		Agonist
    Indacaterol acetate is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol acetate inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol acetate can also be used in cardiovascular disease research.
    Indacaterol acetate
  • HY-122537
    Arotinolol hydrochloride
    Arotinolol hydrochloride is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol hydrochloride also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. Arotinolol hydrochloride is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases.
    Arotinolol hydrochloride
  • HY-B0431AS1
    Phenoxybenzamine (benzyl-2,3,4,5,6-d5) hydrochloride
    		Antagonist
    Phenoxybenzamine (benzyl-2,3,4,5,6-d5) (hydrochloride) is the deuterium labeled Phenoxybenzamine hydrochloride. Phenoxybenzamine hydrochloride is a nonselective, irreversible, orally active α-adrenoceptor antagonist that is commonly used for the research of hypertension, specifically caused by pheochromocytoma. Phenoxybenzamine hydrochloride also shows antitumor activity[1][2][3].
    Phenoxybenzamine (benzyl-2,3,4,5,6-d<sub>5</sub>) hydrochloride
  • HY-10121S2
    Asenapine-13C,d3
    		Inhibitor
    Asenapine-13C,d3 is 13C and deuterated labeled Asenapine (HY-10121). Asenapine (Org 5222), an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine can be used in the research of schizophrenia and bipolar disorder.
    Asenapine-<sup>13</sup>C,d<sub>3</sub>
  • HY-105925
    Mefenidil
    Mefenidil (MCN 2378) is a selective cerebral vasodilator that is not affected by beta-adrenergic blockade. Mefenidil can be used in the study of cardiovascular disease. In monkey models, mefenidil preferentially increases cerebral blood flow over systemic (femoral) blood flow. Mefenidil is also able to reduce systemic arterial pressure in anesthetized dogs.
    Mefenidil
  • HY-107327S1
    Carazolol-d7 hydrochloride
    Carazolol-d7 (hydrochloride) is the deuterium labeled Carazolol hydrochloride (HY-W517264). Carazolol hydrochloride is a highly potent antagonist of β1/β2 adrenoceptor. Carazolol hydrochloride is also a potent, selective β3-adrenoceptor agonist. Carazolol hydrochloride can be used in the research of hypertension.
    Carazolol-d<sub>7</sub> hydrochloride
  • HY-B0773
    Paroxetine mesylate
    		Inhibitor
    Paroxetine mesylate, a phenylpiperidine derivative, is a potent and selective serotonin reuptake inhibitor (SSRI). Paroxetine mesylate is a very weak inhibitor of norepinephrine (NE) uptake but it is still more potent at this site than the other SSRIs.
    Paroxetine mesylate
  • HY-106769C
    Fluparoxan hydrochloride
    		Antagonist
    Fluparoxan hydrochloride is an orally active, selective and competitive alpha 2-adrenoceptor antagonist. Fluparoxan hydrochloride is an anti-depressant agent.
    Fluparoxan hydrochloride
  • HY-N0132R
    Synephrine (Standard)
    		Agonist
    Synephrine (Standard) is the analytical standard of Synephrine. This product is intended for research and analytical applications. Synephrine (Oxedrine), an alkaloid, is an α-adrenergic and β-adrenergic agonist derived from the Citrus aurantium. Synephrine is a sympathomimetic compound and can be used for weight loss.
    Synephrine (Standard)
  • HY-106554
    Trimazosin
    		Antagonist
    Trimazosin is an orally active, quinazoline derivative which is structurally related to prazosin. Trimazosin shows hypotensive effect by selectively block α1-adrenoceptors.
    Trimazosin
  • HY-15413
    Edivoxetine
    		Inhibitor
    Edivoxetine (LY 2216684) is a potent and selective norepinephrine reuptake inhibitor. Edivoxetine can be used for the study of major depressive disorder (MDD) and attention-deficit/hyperactivity disorder (ADHD).
    Edivoxetine
  • HY-106973
    Nolomirole
    		Agonist
    Nolomirole (CHF 1035) is an orally active and selective DA2 dopaminergic receptor/α2-adrenoceptor agonist. Nolomirole attenuates the heart failure signs in the Monocrotaline (HY-N0750)-induced congestive heart failure model. Nolomirole increases cardiac output.
    Nolomirole
  • 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.
    RWJ52353 hydrochloride
  • HY-B0391A
    Naftopidil dihydrochloride
    		Antagonist
    Naftopidil dihydrochloride (KT-611 dihydrochloride) 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 dihydrochloride has antiproliferative effects. Naftopidil dihydrochloride can be used for the research of prostate hyperplasia.
    Naftopidil dihydrochloride
  • HY-163363
    β-AR antagonist 2
    		Antagonist
    β-AR antagonist 2 (compound 43) is an antagonist of β-AR (IC50: 0.17 μM). β-AR-IN-1 inhibits the growth of mouse A549 xenograft tumors and shows cardioprotective efficacy against DOX-induced HF in C57 mice.
    β-AR antagonist 2
  • HY-B1296S1
    Promethazine-d4
    Promethazine-d4 is a deuterated-labeled promethazine (HY-B0781). Promethazine is an orally active H1 receptor and mAChR antagonist with antihistamine (H1), sedative, antiemetic, anticholinergic, and anti-motion sickness properties.
    Promethazine-d<sub>4</sub>
  • HY-127128
    Flestolol sulfate
    		Inhibitor
    Flestolol (ACC-9089) sulfate is a competitive, ultra-short-acting beta-adrenergic blocking agent. Flestolol sulfate shows a half-life of approximately 6.5 minutes. Flestolol sulfate has the potential for the research of chest pain.
    Flestolol sulfate
  • HY-17034AR
    Dexmedetomidine hydrochloride (Standard)
    		Agonist
    Dexmedetomidine (hydrochloride) (Standard) is the analytical standard of Dexmedetomidine (hydrochloride). This product is intended for research and analytical applications. 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.
    Dexmedetomidine hydrochloride (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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