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. Nombre del producto Efecto Pureza Chemical Structure
  • 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-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
  • 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-N0757
    8-​O-​Acetylharpagide
    		Agonist 99.75%
    8-O-Acetylharpagide is an orally active iridoid glycoside compound. 8-O-Acetylharpagide exhibits anti-aging activity at low doses and anticancer activity at high doses. 8-O-Acetylharpagide induces late-stage apoptosis and necrosis-like death in cancer cells, and downregulates anti-apoptotic proteins such as Akt, p-Akt and Bcl-2. 8-O-Acetylharpagide is mainly metabolized in rats via demethylation, hydrolysis and glucuronidation, and its active metabolites downregulate the AKT/NF-κB/MMP9 signaling axis. 8-O-Acetylharpagide exerts vasoconstrictive effects by activating vascular α-adrenoceptor.
    8-​O-​Acetylharpagide
  • HY-155879
    (±)-N-Methylcoclaurine
    		Antagonist 98.22%
    (±)-N-Methylcoclaurine is a selective α2-adrenoceptor antagonist.
    (±)-N-Methylcoclaurine
  • HY-B0528AR
    Octopamine hydrochloride (Standard)
    		Agonist
    Octopamine (hydrochloride) (Standard) is the analytical standard of Octopamine (hydrochloride). This product is intended for research and analytical applications. Octopamine ((±)-p-Octopamine) hydrochloride, a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates. Octopamine hydrochloride can stimulate alpha2-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha2-ARs. Octopamine hydrochloride increased glycogenolysis, glycolysis, oxygen uptake, gluconeogenesis and the portal perfusion pressure.
    Octopamine hydrochloride (Standard)
  • 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-12710
    Rauwolscine
    		Antagonist 98.78%
    Rauwolscine is a selective α2-adrenoceptor antagonist that inhibits tumor growth and induces apoptosis.
    Rauwolscine
  • HY-B0446
    Naphazoline hydrochloride
    		Agonist 99.38%
    Naphazoline (Naphthazoline) hydrochloride is a potent α-adrenergic receptor agonist. Naphazoline hydrochloride reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline hydrochloride reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF. Naphazoline hydrochloride can be used for non-bacterial conjunctivitis research.
    Naphazoline hydrochloride
  • HY-B1435
    Moxisylyte hydrochloride
    		Antagonist 99.65%
    Moxisylyte (Thymoxamine) hydrochloride is a selective α1A-adrenergic receptor antagonist. Moxisylyte hydrochloride competitively antagonizes the activation mediated by norepinephrine. Moxisylyte hydrochloride relaxes penile cavernous smooth muscle and aids erectile function. Moxisylyte hydrochloride is applicable to research related to erectile dysfunction and multiple system atrophy.
    Moxisylyte hydrochloride
  • HY-111013
    VK-II-86
    		Antagonist
    VK-II-86 is a Carvedilol (HY-B0006) analogue lacking antagonist activity at β-adrenoceptors, in hypokalaemia. VK-II-86 prevents hypokalaemia-induced ventricular arrhythmia through multi-channel effects. VK-II-86 prevents all hypokalaemia-induced changes in ion channel activity and oxidative stress.
    VK-II-86
  • HY-B0416
    Gallamine Triethiodide
    		Activator 99.56%
    Gallamine Triethiodide is a blood-brain barrier-permeable skeletal muscle relaxant. Gallamine Triethiodide induces skeletal muscle paralysis by blocking acetylcholine. Gallamine Triethiodide directly stimulates intracardiac β receptors. Gallamine Triethiodide prolongs the duration of afterdischarge in the cat cerebral cortex. Gallamine Triethiodide can be used in studies related to convulsive disorders.
    Gallamine Triethiodide
Cat. No. Nombre del producto / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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