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-N7142S
    DL-Norepinephrine-d6 hydrochloride
    		Modulator 99.88%
    DL-Norepinephrine-d6 (hydrochloride) is the deuterium labeled DL-Norepinephrine hydrochloride. DL-Norepinephrine hydrochloride is a synthetic phenylethylamine that mimics the sympathomimetic actions of the endogenous norepinephrine．DL-Norepinephrine hydrochloride is a neurotransmitter targets α1 and β1 adrenoceptors, has an increasing effect on subendocardial oxygen tension[1].
    DL-Norepinephrine-d<sub>6</sub> hydrochloride
  • HY-107915
    Levonordefrin
    		98.62%
    Levonordefrin, a common alternative to levoepinephrine as a vasoconstrictor in dental local agent that can suppress or relieve pain, is usually used in fivefold higher concentrations. Levonordefrin is generally considered equivalent to epinephrine.
    Levonordefrin
  • HY-B0802A
    Terbutaline
    		Agonist 99.77%
    Terbutaline is an orally active β2-adrenergic receptor agonist and an active metabolite of bambuterol. Terbutaline can be used in asthma symptom research.
    Terbutaline
  • HY-14301
    Olodaterol
    		Agonist 98.47%
    Olodaterol (BI1744) is a selective, long acting β2-adrenoceptor (β2-AR) agonist (EC50=0.1 nM and pKi= 9.14 for human β2-adrenoceptor, respectively). Olodaterol can be used for chronic obstructive pulmonary disease (COPD) and pulmonary fibrosis.
    Olodaterol
  • HY-B0573A
    (S)-(-)-Propranolol hydrochloride
    		Antagonist 99.95%
    (S)-(-)-Propranolol hydrochloride is a β-adrenergic receptor antagonist with log Kd values of -8.16, -9.08, and -6.93 for β1, β2, and β3, respectively. (S)-(-)-Propranolol hydrochloride the active enantiomer of propranolol and can be s used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
    (S)-(-)-Propranolol hydrochloride
  • HY-B0432
    Propafenone
    		Antagonist 99.93%
    Propafenone (SA-79), a sodium-channel blocker, acts an antiarrhythmic agent. Propafenone also has high affinity for the β receptor (IC50=32 nM). Propafenone blocks the transient outward current (Ito) and the sustained delayed rectifier K current (Isus) with IC50 values of 4.9 μm and 8.6 μm, respectively. Propafenone suppresses esophageal cancer proliferation through inducing mitochondrial dysfunction and induce apoptosis.
    Propafenone
  • HY-17495A
    Carteolol hydrochloride
    		Antagonist 99.96%
    Carteolol hydrochloride (OPC-1085 hydrochloride) is a non-selective beta blocker used to treat glaucoma.
    Carteolol hydrochloride
  • HY-B0702
    Nicergoline
    		Inhibitor 99.06%
    Nicergoline, an ergoline derivative ester of bromonicotinic acid, is a potent, selective and orally active antagonist of α1A-adrenoceptor. Nicergoline has vasodilator effects. Nicergoline also has ameliorative effects on cognitive function in mouse models of Alzheimer's disease.
    Nicergoline
  • HY-B0381A
    Betaxolol hydrochloride
    		Inhibitor 99.30%
    Betaxolol Hydrochloride is a selective beta1 adrenergic receptor blocker that can be used for the research of hypertension and glaucoma.
    Betaxolol hydrochloride
  • HY-16736A
    Centanafadine hydrochloride
    		Inhibitor 99.93%
    Centanafadine (hydrochloride) is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively.
    Centanafadine hydrochloride
  • HY-100490A
    Rilmenidine hemifumarate
    		Inhibitor 99.82%
    Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an alpha 2-adrenoceptor agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine hemifumarate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
    Rilmenidine hemifumarate
  • HY-A0295
    (R)-Propranolol hydrochloride
    		Antagonist 99.36%
    (R)-Propranolol hydrochloride is a less active enantiomer of the β-adrenoceptor antagonist propranolol (HY-B0573). 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.
    (R)-Propranolol hydrochloride
  • HY-14689
    Ecopipam hydrochloride
    		Antagonist 99.46%
    Ecopipam (SCH 39166) hydrochloride is a potent, selective and orally active antagonist of dopamine D1/D5 receptor, with Kis of 1.2 nM and 2.0 nM, respectively. Ecopipam hydrochloride shows more than 40-flod selectivity over D2, D4, 5-HT, and α2a receptor (Ki=0.98, 5.52, 0.08, and 0.73 μM, respectively). Ecopipam hydrochloride can be used for the research of schizophrenia and obesity.
    Ecopipam hydrochloride
  • HY-B1392
    Esmolol hydrochloride
    		Inhibitor 99.92%
    Esmolol hydrochloride is a beta adrenergic receptor blocker.
    Esmolol hydrochloride
  • HY-14301A
    Olodaterol hydrochloride
    		Agonist 98.87%
    Olodaterol (BI1744) hydrochloride is a selective, long acting β2-adrenoceptor (β2-AR) agonist (EC50=0.1 nM and pKi= 9.14 for human β2-adrenoceptor, respectively). Olodaterol can be used for chronic obstructive pulmonary disease (COPD) and pulmonary fibrosis.
    Olodaterol hydrochloride
  • HY-101392
    Harmane
    		Inhibitor 99.91%
    Harmane is an inhibitor that binds to benzodiazepine receptors (with an IC50 value of 7 μM), has an IC50 of 24 μM for muscarinic acetylcholine receptors (QNB), an IC50 of 2.8 μM for opioid receptors, and IC50 values of 163 and 101 μM for spironolactone and serotonin, respectively. Harmane is a selective monoamine oxidase inhibitor (with IC50 values of 0.5 μM for MAO A and 5 μM for MAO B). Harman inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing levodopa (L-DOPA)-induced toxicity in PC12 cells. Harmane lowers blood pressure in rats through the I1 imidazoline receptor (I1 receptor) and has antidepressant, anxiolytic, anticonvulsant, and analgesic effects. Harmane enhances the mutagenicity induced by 2-acetylaminofluorene (AAF) .
    Harmane
  • HY-13788
    LY 344864
    		Agonist 98.93%
    LY 344864 is a selective, orally active 5-HT1F receptor agonist with a Ki of 6 nM. LY 344864 is a full agonist producing an effect similar in magnitude to serotonin itself. LY 344864 can cross the blood brain barrier to some extent.
    LY 344864
  • HY-N4225
    Aaptamine
    		Antagonist 99.16%
    Aaptamine, a spongean alkaloid isolated from a sea sponge Aaptos aaptos, is a competitive antagonist of α-adrenoceptor and activates the p21 promoter in a p53-independent manner.
    Aaptamine
  • HY-B1486
    Oxprenolol hydrochloride
    		Antagonist 99.86%
    Oxprenolol hydrochloride (Ba 39089) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle.
    Oxprenolol hydrochloride
  • HY-17453
    Salmeterol xinafoate
    		Agonist 99.96%
    Salmeterol (GR 33343X) xinafoate is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively.
    Salmeterol xinafoate
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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