2. シグナル伝達
  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
製品番号 製品名 製品効果 純度 構造式
  • HY-B0010
    Formoterol fumarate

    Formoterol (fumarate)

    		Agonist 99.95%
    Formoterol fumarate ((±)Formoterol fumarate) is a selective β2-adrenoceptor agonist. Formoterol fumarate is at least as β2-adrenoceptor selective as Salbutamol (HY-B1037) and Terbutaline (HY-B0802A). Formoterol fumarate abolishs the contraction induced by Acetylcholine in bronchioles. Formoterol fumarate can be used for the research of chronic obstructive pulmonary disease and bronchial asthma.
    Formoterol fumarate
  • HY-10122
    Silodosin

    シロドシン

    		Antagonist 99.89%
    Silodosin (KAD 3213; KMD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH.
    Silodosin
  • HY-B0527
    Amitriptyline Antagonist 99.94%
    Amitriptyline is an orally active tricyclic antidepressant (TCA). Amitriptyline 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 is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline can reduce inflammation, angiogenesis and fibrosis. Amitriptyline binds to DAT (with Ki = 2.58 μM). Amitriptyline 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 can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
    Amitriptyline
  • HY-W015061
    Phenylacetylglycine

    Phenylacetylglycine

    		Activator 99.42%
    Phenylacetylglycine is a gut microbial metabolite that can activate β2AR. Phenylacetylglycine protects against cardiac injury caused by ischemia/reperfusion.
    Phenylacetylglycine
  • HY-B0532A
    Trifluoperazine dihydrochloride

    Trifluoperazine (dihydrochloride)

    		Antagonist 99.98%
    Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis.
    Trifluoperazine dihydrochloride
  • HY-12721
    Clonidine

    クロニジン

    		Agonist 99.94%
    Clonidine is an alpha 2-adrenergic agonist.
    Clonidine
  • HY-12380A
    Atipamezole

    アチパメゾール

    		Antagonist 99.97%
    Atipamezole (MPV 1248) is a potent α2-adrenoceptor antagonist with a Ki of 1.6 nM.
    Atipamezole
  • HY-135878
    2',5'-Dideoxyadenosine

    2',5'-Dideoxyadenosine

    		Inhibitor 99.86%
    2',5'-Dideoxyadenosine is a potent and non-competitive adenylyl cyclase inhibitor via binding the P-site with an IC50 of 3 µM . 2',5'-Dideoxyadenosine is a nucleoside analog and exerts a potent antiadrenergic action in heart.
    2',5'-Dideoxyadenosine
  • HY-17416
    Guanfacine hydrochloride

    グアンファシン塩酸塩

    		Agonist 99.98%
    Guanfacine hydrochloride is an orally active and blood-brain barrier permeability 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 hydrochloride
  • HY-B0982
    Pindolol

    ピンドロール

    		Antagonist 99.92%
    Pindolol (LB-46) is the antagonist for 5-HT 1A (Ki=33 nM) and 5-HT 1B. Pindolol is the antagonist for β1/β2-adrenergic receptor. Pindolol exhibits anti-anxiety and antidepressant effects.
    Pindolol
  • HY-B0527A
    Amitriptyline hydrochloride

    アミトリプチリン塩酸塩

    		Antagonist 99.94%
    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
  • HY-10791
    Ritanserin

    Ritanserin

    		Inhibitor 99.68%
    Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors.
    Ritanserin
  • HY-B1108
    Labetalol hydrochloride

    ラベタロール 塩酸塩

    		Antagonist 99.90%
    Labetalol (AH5158) hydrochloride is an orally available, selective α1-adrenergic recepto and non-selective β-adrenergic receptor competitive antagonist. Labetalol hydrochloride is an antihypertensive molecule that partially crosses the blood-brain barrier and has little effect on cardiac output. Labetalol hydrochloride can be used in the study of cardiovascular diseases, such as hypertension during pregnancy.
    Labetalol hydrochloride
  • HY-B0409A
    Clonidine hydrochloride

    クロニジン 塩酸塩

    		Agonist 99.94%
    Clonidine hydrochloride is an agonist of α2-adrenoceptor and potent antihypertensive agent.
    Clonidine hydrochloride
  • HY-B1614
    Clenbuterol hydrochloride

    Clenbuterol (hydrochloride)

    		Agonist 99.98%
    Clenbuterol (NAB-365) hydrochloride, a selective β2-adrenergic agonist, enhances skeletal muscle strength and hypertrophy. Clenbuterol hydrochloride induces growth factor mRNA, activates astrocytes, and protects rat brain tissue against ischemic damage.
    Clenbuterol hydrochloride
  • HY-B0352
    Mirtazapine

    ミルタザピン

    		Antagonist 99.94%
    Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively.
    Mirtazapine
  • HY-B0661
    Tamsulosin Antagonist 99.80%
    Tamsulosin ((R)-(-)-YM12617 free base) is an orally active antagonist of α1-adrenergic receptor. Tamsulosin induces Apoptosis. Tamsulosin is used for the research of prostatic hyperplasia. Tamsulosin attenuates abdominal aortic aneurysm growth and inhibits inflammation in animal models.
    Tamsulosin
  • HY-12380
    Atipamezole hydrochloride Antagonist 99.97%
    Atipamezole (MPV-1248) hydrochloride is a potent α2-adrenoceptor antagonist with a Ki of 1.6 nM.
    Atipamezole hydrochloride
  • HY-103211
    L748337 Inhibitor 99.0%
    L748337 is a potent β3-adrenergic receptor antagonist and displays selectivity over β1 and β2 receptors. The Ki values of L748337 for β3-, β2- and β1-adrenoceptors are 4.0 nM, 204 nM and 390 nM, respectively. L748337 couples predominantly to Gi to activate MAPK signaling and increases phosphorylation of Erk1/2 with pEC50 value of 11.6. L748337 can be used for the research of cancer, nonalcoholic fatty liver disease (NAFLD), and cardiovascular related diseases.
    L748337
  • HY-17385
    Atomoxetine hydrochloride

    アトモキセチン 塩酸塩

    		99.91%
    Atomoxetine (Tomoxetine) hydrochloride is a selective noradrenaline reuptake inhibitor with Ki values of 5 nM, 77 nM and 1451 nM for norepinephrine (NE), serotonin (5-HT) and dopamine (DA) transporters, respectively. Atomoxetine hydrochloride is a potent Na+ channels (VGSCs) blocker. Atomoxetine hydrochloride can be used for attention-deficit hyperactivity disorder (ADHD) research.
    Atomoxetine hydrochloride
製品番号 製品名 / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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