1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. Adrenergic Receptor

Adrenergic Receptor

Beta Receptor

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-100672B
    (2R)-SR59230A
    Antagonist 99.88%
    (2R)-SR59230A is the isomer of SR59230A (HY-100672), and can be used as an experimental control. SR59230A is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist with IC50s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively.
    (2R)-SR59230A
  • HY-113833
    N-Methylindan-2-amine hydrochloride
    99.94%
    N-Methylindan-2-amine hydrochloride (compound 3b) is an N-alkylated congener of phenylethylamine that increases hot plate reaction time in mice without inducing dopaminergic effects. N-Methylindan-2-amine hydrochloride can be used to study central noradrenergic mechanisms.
    N-Methylindan-2-amine hydrochloride
  • HY-B2169
    Melperone
    Antagonist 99.84%
    Melperone is a butyrophenone with atypical antipsychotic properties. Melperone is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values ​​of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone is also a CYP2D6 inhibitor. Melperone can be used for the study of schizophrenia, and agitation in the elderly.
    Melperone
  • HY-B0556A
    Tetrahydrozoline hydrochloride
    Agonist 99.88%
    Tetrahydrozoline hydrochloride (Tetryzoline hydrochloride), a derivative of imidazoline, is an α-adrenergic agonist that causes vasoconstriction. Tetrahydrozoline hydrochloride is widely used for the research of nasal congestion and conjunctival congestion.
    Tetrahydrozoline hydrochloride
  • HY-B0371B
    (R)-Terazosin
    Antagonist 99.98%
    (R)-Terazosin is an active R-enantiomer of Terazosin. (R)-Terazosin is a potent α1-adrenoceptor antagonist with Ki values of 6.51 nM, 1.01 nM and 1.97 nM for α1a, α1b and α1d-adrenoceptor, respectively.
    (R)-Terazosin
  • HY-W795507
    Cyanopindolol
    Antagonist 99.24%
    Cyanopindolol is an β3-adrenoceptor antagonist. Cyanopindolol is a potent and selective antagonist at the presynaptic serotonin autoreceptor in the rat brain cortex. Cyanopindolol has binding affinity for 5-HT1A and 5-HT1B receptor (Ki: 2.1 and 3 nM respectively).
    Cyanopindolol
  • HY-B0010A
    Arformoterol
    Agonist 99.96%
    Arformoterol ((R,R)-Formoterol), the (R,R)-enantiomer of Formoterol, is a long-acting β2-adrenergic receptor (β2-AR) agonist, with a Kd of 2.9 nM. Arformoterol can be used for the research of chronic obstructive pulmonary disease (COPD).
    Arformoterol
  • HY-101355A
    CGP 20712 dihydrochloride
    Antagonist 99.4%
    CGP 20712 dihydrochloride is a highly selective β1-adrenoceptor antagonist with an IC50 of 0.7 nM. CGP 20712 dihydrochloride exhibits ~10,000-fold selectivity over β2-adrenoceptors.
    CGP 20712 dihydrochloride
  • HY-135115
    Oleuropein Aglycone
    98.46%
    Oleuropein Aglycone (3,4-DHPEA-EA) is a polyphenol and the aglycone form of oleuropein (HY-N0292), formed by enzymatic, acidic or acetylated hydrolysis of oleuropein. Dietary intake of oleuropein Aglycone (50 mg/kg diet) increases the number of neuronal autophagic vesicles, reverses cognitive deficits in the TgCRND8 transgenic mouse model of Alzheimer's disease, and reduces the levels of histone deacetylase 2 (HDAC2) in the cortex and hippocampus. Oleuropein Aglycone increases urinary norepinephrine, interscapular brown adipose tissue epinephrine, and UCP1 protein levels, and reduced plasma leptin levels and total abdominal adipose tissue weight in a rat model of high-fat diet-induced obesity. Oleuropein Aglycone also reduced lung neutrophil infiltration, lipid peroxidation, and IL-1β levels in a mouse model of carrageenan-induced pleurisy.
    Oleuropein Aglycone
  • HY-W702712
    3-Hydroxy xylazine
    Control
    3-Hydroxy xylazine is a metabolite of the α2-adrenergic receptor agonist Xylazine.
    3-Hydroxy xylazine
  • HY-B0459
    Scopine
    Agonist ≥98.0%
    Scopine is the metabolite of anisodine, which is a α1-adrenergic receptor agonist and used in the treatment of acute circulatory shock.
    Scopine
  • HY-101393A
    CGP 12177 hydrochloride
    Modulator 99.69%
    CGP 12177 ((±)-CGP 12177) hydrochloride is a β Adrenergic Receptor Ligand. CGP 12177 hydrochloride is a high affinity antagonist of β1- and β2-AR. CGP 12177 hydrochloride is also shown to interact, with a lower affinity, with the β3-AR and to exhibit a partial agonist activity on rodent and human β3-AR. CGP 12177 hydrochloride exhibits partial agonist properties for α1-AR in rat pulmonary artery.
    CGP 12177 hydrochloride
  • HY-U00205
    Dopexamine hydrochloride
    Agonist 99.71%
    Dopexamine hydrochloride is a β2 adrenergic receptor agonist.
    Dopexamine hydrochloride
  • HY-B1694A
    Methoxyphenamine hydrochloride
    Agonist ≥98.0%
    Methoxyphenamine hydrochloride, a non-regulated analog of Methamphetamine, is a β-adrenergic receptor agonist used as a bronchodilator.
    Methoxyphenamine hydrochloride
  • HY-B1111
    Amitraz
    Agonist 99.65%
    Amitraz is a non-systemic acaricide and insecticide with alpha-adrenergic agonist activity that interacts with octopamine receptors in the central nervous system and inhibits monoamine oxidase and prostaglandin synthesis.
    Amitraz
  • HY-12882
    Ifenprodil
    Antagonist 99.94%
    Ifenprodil (NP-120), a cerebral vasodilator, is a noncompetitive NMDA receptor antagonist. Ifenprodil exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM). Ifenprodil is an α1 adrenergic receptor antagonist. Ifenprodil inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil has reliable inhibitory effects against A/H1N1 strains (EC50 of 6.6 µM). Ifenprodil has neuroprotective, anticonvulsant and antinociceptive effects. Ifenprodil can be used for the study of cerebrovascular diseases and peripheral arterial obliterative disease.
    Ifenprodil
  • HY-162677
    MT-1207
    Antagonist 99.96%
    MT-1207 is an orally active and selective adrenergic α1 and 5-HT2A receptor antagonist. MT-1207 shows IC50<0.1 nM, 0.15 nM, 1.40 nM and 0.27 nM for α1A, α1B, α1D and 5-HT2A, respectively. MT-1207 achieves an effective blood pressure (BP) reduction in the 2K2C rat model without damaging renal function. MT-1207 is a potent multitarget inhibitor with the potential for vasodilatation research.
    MT-1207
  • HY-148804
    Vemtoberant
    Antagonist 99.08%
    Vemtoberant is an β3 Adrenergic Receptor antagonist. Vemtoberant can be used for research of β3 adrenergic receptor-mediated disorder, such as, heart failure.
    Vemtoberant
  • HY-114814
    ORM-10921 free base
    Antagonist 98.08%
    ORM-10921 free base is a selective α-2C adrenergic receptor antagonist with a Ki of 1.4 nM. ORM-10921 free base displays potent antidepressant and antipsychotic-like effects.
    ORM-10921 free base
  • HY-B0573BS
    Propranolol-d7
    Antagonist ≥99.0%
    Propranolol-d7 is the deuterium labeled Propranolol. 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. Propranolol inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
    Propranolol-d<sub>7</sub>
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