2. Vías de señalización
  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. Nom du produit Effet Pureté Chemical Structure
  • HY-12463
    Carmoterol hydrochloride
    		Agonist 98.73%
    Carmoterol hydrochloride is a highly potent, selective and long-acting β2-adrenoceptor agonist with the pEC50 of 10.19. Carmoterol has 53 times higher affinity for the β2-adrenoceptors than for the β1-adrenoceptors. Carmoterol hydrochloride can be used for the research of asthma and chronic obstructive pulmonary disease (COPD).
    Carmoterol hydrochloride
  • HY-B0194A
    Tizanidine hydrochloride
    		Agonist 99.93%
    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 hydrochloride
  • HY-B0527AR
    Amitriptyline hydrochloride (Standard)
    		Antagonist
    Amitriptyline hydrochloride (Standard) is the analytical standard of Amitriptyline hydrochloride (HY-B0527A). This product is intended for research and analytical applications. 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 hydrochloride (Standard)
  • HY-15844
    AG-825
    		Activator 98.13%
    AG-825 is a selective, ATP-competitive, tyrosine phosphorylation ErbB2 inhibitor with an IC50 of 0.35 μM. AG825 significantly accelerates Apoptosis of human neutrophils. AG-825 increases β1AR density. AAG-825 has anticancer and anti-inflammatory activities. AAG-825 can be used in cardiovascular disease research.
    AG-825
  • HY-14539S2
    Clozapine-d4
    		Inhibitor 99.80%
    Clozapine-d4 is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors.
    Clozapine-d<sub>4</sub>
  • HY-B1270
    Isoxsuprine hydrochloride
    		Agonist 99.95%
    Isoxsuprine hydrochloride is a beta-adrenergic receptor agonist with Kis of 13.65 μΜ and 3.48 μΜ for myometrial and placcntal beta-adrenergic receptor, respectively. Isoxsuprine hydrochloride is also a NMDA receptor antagonist.
    Isoxsuprine hydrochloride
  • HY-B1421
    Ractopamine hydrochloride
    		Agonist 99.2%
    Ractopamine hydrochloride (LY031537) is a potent and orally active β-adrenergic receptor (βAR) agonist with Kd value of ~25 nM for pig β1AR and β2AR. Ractopamine hydrochloride also is a mTAAR1 agonist with an EC50 of 16 μM. Ractopamine hydrochloride promotes muscle mass development, limits fat deposition, reduces feed consumption, increases total cellular protein synthesis, and improves growth rate and feed efficiency in finishing swine. Ractopamine hydrochloride can be used for researching to increase lean tissue growth and improve production efficiency in pigs.
    Ractopamine hydrochloride
  • HY-B1613A
    Clebopride malate
    		Antagonist 99.41%
    Clebopride malate is an orally active dopamine Receptor antagonist. Clebopride malate acts on dopamine D2 receptors and has antiemetic and prokinetic effects. Clebopride malate can be used in the study of functional gastrointestinal disorders.
    Clebopride malate
  • HY-155879
    (±)-N-Methylcoclaurine
    		Antagonist 98.22%
    (±)-N-Methylcoclaurine is a selective α2-adrenoceptor antagonist.
    (±)-N-Methylcoclaurine
  • HY-16413
    Protokylol hydrochloride
    		Agonist 99.07%
    Protokylol hydrochloride (Caytine hydrochloride; JB-251 hydrochloride) is the hydrochloride salt form of Protokylol (HY-114630). Protokylol hydrochloride is an agonist for β2-adrenergic receptor and TRPV1. Protokylol hydrochloride exhibits activity as a bronchodilator.
    Protokylol hydrochloride
  • HY-B0769R
    Phenylephrine (Standard)
    		Agonist
    Phenylephrine (Standard) is the analytical standard of Phenylephrine. This product is intended for research and analytical applications. (R)-(-)-Phenylephrine is a selective α1-adrenoceptor agonist primarily used as a decongestant.
    Phenylephrine (Standard)
  • HY-14299AR
    Indacaterol maleate (Standard)
    		Agonist
    Indacaterol (maleate) (Standard) is the analytical standard of Indacaterol (maleate). This product is intended for research and analytical applications. 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 (Standard)
  • HY-W015061R
    Phenylacetylglycine (Standard)
    		Activator
    Phenylacetylglycine (Standard) is the analytical standard of Phenylacetylglycine. This product is intended for research and analytical applications. Phenylacetylglycine is a gut microbial metabolite that can activate β2AR. Phenylacetylglycine protects against cardiac injury caused by ischemia/reperfusion.
    Phenylacetylglycine (Standard)
  • HY-B0225B
    Methyldopa hydrate
    		Agonist 99.95%
    Methyldopa hydrate (L-(-)-α-Methyldopa hydrate), a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa hydrate is a proagent and is metabolized (α-Methylepinephrine) in the central nervous system.
    Methyldopa hydrate
  • HY-B0194S
    Tizanidine-d4
    		Agonist 99.93%
    Tizanidine-d4 is the deuterium labeled Tizanidine (HY-B0194). Tizanidine, a skeletal muscle relaxant, is an orally effective central α2-adrenoceptor agonist (IC50 = 6.9 nmol). Tizanidine 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 has anti-injury activity and can inhibit gastrointestinal (GI) transport. Tizanidine 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 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>
  • HY-116790A
    (+)-Penbutolol
    		Antagonist
    (+)-Penbutolol is a β-adrenoceptor antagonist, with an IC50 of 0.74 μM. (+)-Penbutolol is an optical isomer of l-penbutolol with Na+ channel-blocking action.
    (+)-Penbutolol
  • HY-A0144A
    Etilefrine hydrochloride
    		Agonist 99.90%
    Etilefrine hydrochloride is a sympathetic nerve agonist and AMPK activator that selectively targets α1/β1 adrenergic receptors. Etilefrine hydrochloride stimulates α1 adrenergic receptors, leading to contraction of vascular smooth muscle and increased peripheral resistance. Etilefrine hydrochloride also stimulates β1 receptors to enhance myocardial contractility and increase heart rate, thereby increasing blood pressure and improving cardiac output. Etilefrine hydrochloride also bidirectionally regulates the AMPK/Akt pathway and modulates the phosphorylation levels. Etilefrine hydrochloride can be used in cardiovascular research, such as postural hypotension, chylothorax, and improving low cardiac output.
    Etilefrine hydrochloride
  • HY-171978A
    LM-189 free base
    		Agonist 99.70%
    LM-189 free base, a G protein alpha subunit I (Gαi)-biased agonist, is a Gαi-biased ligand of β2-adrenergic receptor (β2AR). LM-189 free base stabilizes a distinct conformation in TM6 and increases the dynamics of ICL2. LM-189 free base can be used to develop the Gαi-biased β2AR agonists.
    LM-189 free base
  • HY-B1696
    Methyldopate
    		Agonist
    Methyldopate is an ethyl ester proagent of α-Methyldopa (α-MD; HY-B0225). Methyldopa (L-(-)-α-Methyldopa) is an α-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopate has the potential for severe hypertension research .
    Methyldopate
  • HY-N8728
    Aposcopolamine
    		98.23%
    Aposcopolamine is an alkaloid that can be isolated from Datura ferox. Aposcopolamin can closely binds with ACHE, ADRA2A and CHRM2. Aposcopolamine can be used for the research of Alzheimer's disease.
    Aposcopolamine
Cat. No. Nom du produit / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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