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-103207
    Amibegron hydrochloride
    		Agonist ≥99.0%
    Amibegron hydrochloride is a selective β3-adrenoceptor agonist, with an EC50 of 3.5 nM for β-adrenoceptor in rat colon; Amibegron hydrochloride has anxiolytic and antidepressant activity.
    Amibegron hydrochloride
  • HY-121185
    Hexoprenaline
    		Agonist
    Hexoprenaline is an orally active and selective β-adrenergic receptor agonist. Hexoprenaline can dilate the bronchi. Hexoprenaline can activate adenylate cyclase and increases 14C-Aminopyrine uptake. Hexoprenaline exhibits anti-infection and anti-inflammmation effect. Hexoprenaline can increase placental weight and blood flow. Hexoprenaline can be used for the researches of inflammation, immunology, infection, endocrinology and neurological disease, such as asthma, chronic bronchitis, sepsis and intoxication of organophosphorus compounds.
    Hexoprenaline
  • HY-B0802R
    Terbutaline sulfate (Standard)
    		Agonist
    Terbutaline (sulfate) (Standard) is the analytical standard of Terbutaline (sulfate). This product is intended for research and analytical applications. Terbutaline sulfate is an orally active β2-adrenergic receptor agonist and an active metabolite of bambuterol. Terbutaline sulfate can be used in asthma symptom research.
    Terbutaline sulfate (Standard)
  • HY-117046A
    AVN-101 hydrochloride
    		Inhibitor 99.59%
    AVN-101 hydrochloride is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56  nM, and 1.17  nM, respectively). AVN-101 hydrochloride also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 hydrochloride can be studied in such diseases as general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis.
    AVN-101 hydrochloride
  • HY-100704
    Procaterol hydrochloride
    		Agonist 99.99%
    Procaterol hydrochloride is a selective intermediate-acting β2 adrenoreceptor agonist with an EC50 of 12.9 μM. Procaterol hydrochloride can inhibit inflammation both in vivo and in vitro.
    Procaterol hydrochloride
  • HY-B0374
    Moxonidine
    		Activator 99.72%
    Moxonidine (BDF5895) is an orally active imidazoline type 1 receptor (I1-R) agonist. Moxonidine activates imidazoline I1 receptors and α2 adrenoceptors, affecting oxidized low-density lipoprotein uptake. Moxonidine reduces atherosclerotic lesions and lowers blood pressure. Moxonidine can be used in the study of hypertension, heart failure, and atherosclerosis.
    Moxonidine
  • HY-N1433
    Phytolaccagenin
    		Inhibitor 99.86%
    Phytolaccagenin is a triterpenoid saponin aglycone, Antifungal agent, vasodilator, antihypertensive agent, and anti-inflammatory agent. Phytolaccagenin activates vascular and cardiac Muscarinic receptors, blocks cardiac β-adrenergic receptors, and inhibits voltage-dependent calcium channels in blood vessels. Phytolaccagenin inhibits the growth of Candida albicans and Cryptococcus neoformans. Phytolaccagenin induces vasodilation, produces negative inotropic and negative chronotropic effects, reduces mean arterial pressure, and inhibits LPS-induced inflammation. Phytolaccagenin exhibits enhanced antihypertensive effects in high salt-induced hypertensive rats. Phytolaccagenin can be used in the research of candidiasis, cryptococcosis, hypertension, and inflammation-related diseases.
    Phytolaccagenin
  • HY-19436
    Solabegron
    		Agonist 99.89%
    Solabegron (GW 427353) is a selective β3-adrenergic receptor agonist, stimulating cAMP accumulation in Chinese hamster ovary cells expressing the human β3-AR, with an EC50 value of 22 nM. Solabegron (GW 427353) is being developed for the treatment of overactive bladder and irritable bowel syndrome.
    Solabegron
  • HY-B0354A
    Urapidil hydrochloride
    		Antagonist 99.86%
    Urapidil hydrochloride is an orally active and blood-brain barrier permeability α1-adrenoceptor antagonist and 5-HT1A receptor agonist with a pIC50 of 6.13 and 4.38 against α1- and α2-adrenoceptor, respectively. Urapidil hydrochloride shows antihypertensive effect.
    Urapidil hydrochloride
  • HY-101355A
    CGP 20712 dihydrochloride
    		Antagonist 99.4%
    CGP 20712 dihydrochloride is a highly selective β1-adrenoceptor antagonist with an IC50 of 0.7 nM. CGP 20712 dihydrochloride exhibits ~10,000-fold selectivity over β2-adrenoceptors.
    CGP 20712 dihydrochloride
  • HY-B0381B
    Levobetaxolol hydrochloride
    		Inhibitor 99.17%
    Levobetaxolol hydrochloride is a beta-adrenergic receptor inhibitor (beta blocker) that can lower the pressure in the eye.
    Levobetaxolol hydrochloride
  • HY-101392A
    Harmane hydrochloride
    		Inhibitor 99.88%
    Harmane hydrochloride is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane hydrochloride inhibits the I1 imidazoline receptor (IC50 = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane hydrochloride inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane hydrochloride can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).
    Harmane hydrochloride
  • HY-15780S1
    Brexpiprazole-d8-1
    Brexpiprazole-d8-1 (OPC-34712-d8-1) is the deuterium labeled Brexpiprazole (HY-15780). Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM).
    Brexpiprazole-d<sub>8</sub>-1
  • HY-122272R
    Paroxetine (Standard)
    		Inhibitor
    Paroxetine (Standard) is the analytical standard of Paroxetine. This product is intended for research and analytical applications. Paroxetine is an oral inhibitor that falls under the category of selective serotonin reuptake inhibitors (SSRIs). Paroxetine is also a very weak norepinephrine (NE) reuptake inhibitor, capable of inducing cell apoptosis and having anti-tumor activity. Paroxetine has antidepressant, anti-anxiety, and pain-relieving effects, and it can help improve conditions like obsessive-compulsive disorder, panic disorder, post-traumatic stress disorder, premenstrual anxiety, and chronic headaches.
    Paroxetine (Standard)
  • HY-14541S
    Olanzapine-d3
    		Antagonist 99.78%
    Olanzapine-d3 (LY170053-d3) is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active 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 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic.
    Olanzapine-d<sub>3</sub>
  • HY-N0378S3
    D-Mannitol-2-13C
    		Activator 99.95%
    D-Mannitol-2-13C is the 13C labeled D-Mannitol (HY-N0378). D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β3-adrenergic receptor (β3-AR), PGC1α and PKA induced by means of white fat cells into brown fat cells. D-Mannitol is commonly used to maintain osmotic pressure between the plant cytoplasm and the culture medium and protect cells when the cell wall is weakened or even removed.
    D-Mannitol-2-<sup>13</sup>C
  • HY-148804
    Vemtoberant
    		Antagonist 98.03%
    Vemtoberant is a β3-adrenergic receptor inhibitor with a human Ki of 8.2 nM, and exhibits 400- to 600-fold selectivity over human β1-AR and β2-AR. Vemtoberant attenuates β3-AR-mediated cardiac inhibition. Vemtoberant can be used for the research of systolic heart failure.
    Vemtoberant
  • HY-B0527AS
    Amitriptyline-d6 hydrochloride
    		Antagonist 99.93%
    Amitriptyline-d6 hydrochloride is the deuterium labeled Amitriptyline hydrochloride (HY-B0527A). Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
    Amitriptyline-d<sub>6</sub> hydrochloride
  • HY-B0573BS
    Propranolol-d7
    		Antagonist ≥99.0%
    Propranolol-d7 is the deuterium labeled Propranolol. Propranolol 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. Propranolol inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
    Propranolol-d<sub>7</sub>
  • HY-12961A
    Bretylium tosylate
    		99.90%
    Bretylium (tosylate) is an inhibitor of the presynaptic release of vasoconstrictor neurotransmitters.
    Bretylium tosylate
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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