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-149728
    β2AR agonist 3
    		Agonist
    β2AR agonist 3 (compound 9a) is a β2-adrenergic receptor (β2AR) agonist. β2AR agonist 3 can be used for type 2 diabetes research.
    β2AR agonist 3
  • HY-128483R
    Fusaric acid (Standard)
    		Inhibitor
    Fusaric acid (Standard) is the analytical standard of Fusaric acid (HY-128483). This product is intended for research and analytical applications. 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 (Standard)
  • HY-B0098S
    Doxazosin-d8
    		Antagonist
    Doxazosin-d8 is a deuterium labeled Doxazosin (UK 33274). Doxazosin is a quinazoline-derivative that selectively antagonizes postsynaptic α1 adrenergic receptors.
    Doxazosin-d<sub>8</sub>
  • HY-19057
    Vatinoxan
    		Antagonist 99.83%
    Vatinoxan (MK-467) is an alpha 2-adrenergic receptor antagonist. The peripheral selectivity of Vatinoxan determines that it has limited penetration across the blood-brain barrier and therefore has low concentrations in the central nervous system. Vatinoxan antagonizes alpha 2-adrenergic receptor receptors by binding to them, thereby reducing or preventing cardiovascular effects caused by α2-adrenergic agonists. Vatinoxan can be used in studies of cardiovascular effects, sedation and analgesia.
    Vatinoxan
  • HY-B0194AS
    Tizanidine-d4 hydrochloride
    		Agonist
    Tizanidine-d4 hydrochloride is deuterium labeled Tizanidine hydrochloride (HY-B0194A). Tizanidine hydrochloride, a skeletal muscle relaxant, is an orally effective central α2-adrenoceptor agonist (IC50 = 6.9 nmol). Tizanidine hydrochloride primarily exerts muscle relaxation effects by inhibiting the release of excitatory amino acids (glutamate and aspartate) from the presynaptic terminals of spinal cord interneurons. Tizanidine hydrochloride has anti-injury activity and can inhibit gastrointestinal (GI) transport. Tizanidine hydrochloride can inhibit the proliferation, migration, and invasion of lung cancer cells and induce cell apoptosis by upregulating Nischarin and inhibiting the AKT and Wnt3a/β-catenin signaling pathways. Tizanidine hydrochloride can be used to treat spasticity caused by diseases such as multiple sclerosis (MS), stroke, and spinal cord injury (SCI).
    Tizanidine-d<sub>4</sub> hydrochloride
  • HY-106933A
    Dabelotine methanesulfonate
    		Activator
    Dabelotine (methanesulfonate) is a cognitive enhancer. Dabelotine (methanesulfonate) can be used for Alzheimer disease (AD) research.
    Dabelotine methanesulfonate
  • HY-19091
    ICI-170777
    ICI-170777 is an orally active cardiotonic agent and type III Phosphodiesterase inhibitor, with an IC50 of 2.5 μM against cyclic AMP phosphodiesterase type III from canine cardiac fractions. ICI-170777 inhibits Aldrin epoxidase and pentobarbital metabolism. It enhances β-adrenergic receptor-mediated positive inotropic effects without causing chronotropic effects, while also exerting balanced arteriolar/venular vasodilator, platelet aggregation inhibitor and smooth muscle relaxant activities. ICI-170777 restores cardiac function in an acute canine heart failure model, exhibits additive effects when combined with Ouabain (HY-B1457), and shows no significant activity against multiple receptor classes or non-cardiac systems. ICI-170777 can be used in research related to congestive heart failure.
    ICI-170777
  • HY-105154
    Proxodolol free base
    		Antagonist
    Proxodolol free base is a β-adrenergic receptor blocker. Proxodolol free base can be used for the study of arterial hypertension.
    Proxodolol free base
  • HY-17416AS
    Guanfacine-13C,15N3
    Guanfacine-13C,15N3 is the 13C and 15N labeled Guanfacine. Guanfacine is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD).
    Guanfacine-<sup>13</sup>C,<sup>15</sup>N<sub>3</sub>
  • HY-178319
    Photoazolol-1
    		Antagonist
    Photoazolol-1 is a β-adrenergic receptor (βAR)-blocker derivative. Photoazolol-1 can transfer from an inverse agonist to a neutral antagonist upon photoactivation.
    Photoazolol-1
  • HY-A0019BS
    (R)-9-Hydroxy Risperidone-d4
    (R)-9-Hydroxy Risperidone-d4 is the deuterium labeled (R)-9-Hydroxy Risperidone.
    (R)-9-Hydroxy Risperidone-d<sub>4</sub>
  • HY-129029S1
    Bisoprolol-d5 fumarate (2:1)
    		Inhibitor
    Bisoprolol-d5 fumarate (2:1) is the deuterium labeled Bisoprolol. Bisoprolol is a potent, selective and orally active β1-adrenergic receptor blocker with little activity on β2-receptor. Bisoprolol has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.
    Bisoprolol-d<sub>5</sub> fumarate (2:1)
  • HY-116379
    RS-100329
    		Antagonist
    RS-100329 is an α1-adrenergic receptor (α1-AR) antagonist that effectively inhibits α1-adrenergic receptor-mediated contractions of lower urinary tract tissues in vitro and in vivo. RS-100329 can be used in the research of symptoms related to benign prostatic hyperplasia.
    RS-100329
  • HY-122272S2
    Paroxetine-d6-1
    		Inhibitor
    Paroxetine-d6-1 is a deuterated labeled Paroxetine. Paroxetine, a phenylpiperidine derivative, is a potent and selective serotonin reuptake inhibitor (SSRI). Paroxetine is a very weak inhibitor of norepinephrine (NE) uptake but it is still more potent at this site than the other SSRIs.
    Paroxetine-d<sub>6</sub>-1
  • HY-W909149
    TAAR1 agonist 3
    		Agonist
    TAAR1 agonist 3 is a trace amine-associated receptor 1 (TAAR1) agonist (pEC50=7.6). TAAR1 agonist 3 is also a full agonist of the α2A receptor (pEC50=6). TAAR1 agonist 3 can be used in the study of neuropsychiatric diseases.
    TAAR1 agonist 3
  • HY-14767
    Fasobegron
    		Agonist
    Fasobegron is a β3-adrenergic receptor agonist with a human EC50 of 4.8 nM. Fasobegron shows an EC50 of 250 nM for human β1-adrenergic receptors. Fasobegron can be used for the research of overactive bladder.
    Fasobegron
  • HY-W742256
    N-Nitroso nebivolol (mixture of diastereomers)
    		Control
    N-Nitroso nebivolol (mixture of diastereomers) is a nitrosamine and mutagenic.
    N-Nitroso nebivolol (mixture of diastereomers)
  • HY-121166
    Levobetaxolol
    		Antagonist
    Levobetaxolol is a potent and high affinity β-adrenergic antagonist with IC50 values of 33.2, 2970, 709 nM for guinea pig atrial β1, tracheal β2 and rat colonic β3 receptors, respectively. Levobetaxolol reduces IOP (intraocular pressure). Levobetaxolol exhibits a micromolar affinity for L-type Ca21-channels. Levobetaxolol decreases the effects of ischaemia/reperfusion injury in rats. Levobetaxolol has the potential for the research of glaucoma.
    Levobetaxolol
  • HY-B1098A
    Hydroxyamphetamine hydrobromide
    Hydroxyamphetamine (4-Hydroxyamphetamine) hydrobromide is a sympathomimetic agent, stimulates the sympathetic nervous system. Hydroxyamphetamine hydrobromide can be used in eye drops to dilate the pupil.
    Hydroxyamphetamine hydrobromide
  • HY-B1001
    Todralazine
    		Inhibitor
    Todralazine (Ecarazine) is an anti-hypertensive agent, acts as a β2AR blocker, with antioxidant and free radical scavenging activity.
    Todralazine
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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