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-13458
    Droxidopa
    		98.80%
    Droxidopa (L-DOPS; SM5688) is a potent, orally active norepinephrine precursor. Droxidopa increases standing blood pressure, ameliorates symptoms of orthostatic hypotension and improves standing ability. Droxidopa has the potential for the research of neurogenic orthostatic hypotension (nOH) and alternative ADHD (attention deficit hyperactivity disorder).
    Droxidopa
  • HY-17034B
    Medetomidine hydrochloride
    		Agonist 99.80%
    Medetomidine hydrochloride is an orally active α2-adrenoceptor agonist (Ki: 1.08 nM). Medetomidine hydrochloride has sedative and analgesic effects. Medetomidine hydrochloride can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels.
    Medetomidine hydrochloride
  • HY-14301
    Olodaterol
    		Agonist 98.69%
    Olodaterol (BI1744) is a selective, long acting β2-adrenoceptor (β2-AR) agonist (EC50=0.1 nM and pKi= 9.14 for human β2-adrenoceptor, respectively). Olodaterol can be used for chronic obstructive pulmonary disease (COPD) and pulmonary fibrosis.
    Olodaterol
  • HY-B0781
    Promethazine hydrochloride
    		99.85%
    Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors.
    Promethazine hydrochloride
  • HY-14299
    Indacaterol
    		Agonist 99.98%
    Indacaterol is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol 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 can also be used in cardiovascular disease research.
    Indacaterol
  • HY-A0016
    Dronedarone
    		Inhibitor 99.93%
    Dronedarone (SR 33589), a derivative of amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone is a substrate for and a moderate inhibitor of CYP3A4.
    Dronedarone
  • HY-B0976
    Fenoterol
    		Agonist 99.08%
    Fenoterol (Th-1165), a sympathomimetic agent, is a selective and orally active β2-adrenoceptor agonist. Fenoterol is an effective bronchodilator and can be used for bronchospasm associated with asthma, bronchitis and other obstructive airway diseases research.
    Fenoterol
  • HY-B0802A
    Terbutaline
    		Agonist 99.77%
    Terbutaline is an orally active β2-adrenergic receptor agonist and an active metabolite of bambuterol. Terbutaline can be used in asthma symptom research.
    Terbutaline
  • HY-B0800
    Guanethidine sulfate
    		98.0%
    Guanethidine sulfate (Guanethidine monosulfate), an antihypertensive agent, is an adrenergic neurone blocking agent. Guanethidine sulfate enters noradrenergic nerve terminals by the neuronal amine carrier.
    Guanethidine sulfate
  • HY-B0432
    Propafenone
    		Antagonist 99.64%
    Propafenone (SA-79), a sodium-channel blocker, acts an antiarrhythmic agent. Propafenone also has high affinity for the β receptor (IC50=32 nM). Propafenone blocks the transient outward current (Ito) and the sustained delayed rectifier K current (Isus) with IC50 values of 4.9 μm and 8.6 μm, respectively. Propafenone suppresses esophageal cancer proliferation through inducing mitochondrial dysfunction and induce apoptosis.
    Propafenone
  • HY-103200
    SR59230A hydrochloride
    		Antagonist 99.81%
    SR59230A hydrochloride is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist with IC50s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively.
    SR59230A hydrochloride
  • HY-N0761
    Isoferulic acid
    		Inhibitor 99.91%
    Isoferulic acid (3-Hydroxy-4-methoxycinnamic acid) is an orally active cinnamic acid derivative. Isoferulic acid exhibits hypoglycemic, antiviral, and antioxidant activities. Isoferulic acid can also inhibit fructose- and glucose-mediated protein glycation. Isoferulic acid can be used in the research of diseases such as diabetes.
    Isoferulic acid
  • HY-14299A
    Indacaterol maleate
    		Agonist 99.82%
    Indacaterol maleate (QAB149) is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol maleate 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 maleate can also be used in cardiovascular disease research.
    Indacaterol maleate
  • HY-13575
    Blonanserin
    		Antagonist 99.62%
    Blonanserin (AD-5423) is a potent and orally active 5-HT2A (Ki=0.812 nM) and dopamine D2 receptor (Ki =0.142 nM) antagonist. Blonanserin is usually acts as an atypical antipsychotic agent and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension.
    Blonanserin
  • HY-19933
    Vibegron
    		Agonist 98.03%
    Vibegron (MK-4618) is a potent, highly selective and orally active β3-adrenoceptor agonist (EC50=1.1 nM). Vibegron can be used for severe urgency urinary incontinence related to overactive bladder.
    Vibegron
  • HY-101385
    L-765314
    		Agonist 99.92%
    L-765314 is a potent and selective α1b adrenergic receptor antagonist with Kis of 5.4 nM and 2.0 nM for rat and human α1b adrenergic receptor, respectively.
    L-765314
  • HY-A0066A
    Tolazoline hydrochloride
    		Antagonist 99.93%
    Tolazoline hydrochloride (Imidaline hydrochloride) is an α-adrenergic receptor antagonist. Tolazoline hydrochloride inhibits Noradrenaline (HY-13715)-induced cell contraction, modulates vascular resistance, increases arterial pressure, and reverses bradycardia and tachypnea. Tolazoline hydrochloride can be used to study erectile dysfunction, α2-adrenergic receptor agonist-related poisoning, and skin vascular disease research.
    Tolazoline hydrochloride
  • HY-B0431A
    Phenoxybenzamine hydrochloride
    		Antagonist 99.53%
    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.
    Phenoxybenzamine hydrochloride
  • HY-N2037
    Higenamine
    		Agonist 98.91%
    Higenamine (Norcoclaurine), a β2-AR agonist with antioxidant capability, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine is also a α1-adrenergic receptor antagonist with hypotensive effect. is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine protects myocyte Apoptosis and ischemia/reperfusion (I/R) injury through selective activation of beta2-adrenergic receptor (β2-AR). Higenamine also reduces I/R-induced myocardial infarction in mice. Higenamine can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine can be used to study cancer, inflammation, cardiorenal syndrome and other diseases.
    Higenamine
  • HY-128483
    Fusaric acid
    		Inhibitor 99.94%
    Fusaric acid is an orally active multi-pathway inhibitor with the activity of inducing oxidative stress and apoptosis. Fusaric acid can chelate divalent metal cations, damage mitochondrial membrane structure, and activate apoptosis-related proteases such as Caspase-3/7, -8, and -9. Fusaric acid also regulates Bax/Bcl-2 protein, inhibits fibrosis-related signaling pathways such as NF-κB, TGF-β1/SMADs, and PI3K/AKT/mTOR, and reduces collagen deposition. Fusaric acid is also a dopamine β-hydroxylase inhibitor, which reduces endogenous levels of norepinephrine and epinephrine in the brain, heart, spleen, and adrenal glands. Fusaric acid can play a role in myocardial fibrosis and improve cardiac hypertrophy in heart disease, and can also be used in the study of esophageal cancer and liver cancer.
    Fusaric acid
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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