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-13715BR
    Norepinephrine bitartrate monohydrate (Standard)
    		Agonist
    Norepinephrine (bitartrate monohydrate) (Standard) is the analytical standard of Norepinephrine (bitartrate monohydrate). This product is intended for research and analytical applications. Norepinephrine (Levarterenol; L-Noradrenaline) bitartrate monohydrate is a potent adrenergic receptor (AR) agonist. Norepinephrine activates α1, α2, β1 receptors.
    Norepinephrine bitartrate monohydrate (Standard)
  • HY-12707A
    Piribedil dihydrochloride
    		Antagonist
    Piribedil dihydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil dihydrochloride is also a α2-adrenoceptors antagonist. Piribedil dihydrochloride can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil dihydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers.
    Piribedil dihydrochloride
  • HY-119873
    Celiprolol
    		Antagonist
    Celiprolol (REV 5320) is a potent, cardioselective and orally active β1-andrenoceptor r antagonist with partial β2 agonist activity, with Ki values of 0.14-8.3 μM. Celiprolol has antihypertensive and antianginal activity, and can be used for the research of cardiovascular disease such as high blood pressure.
    Celiprolol
  • HY-B2195
    Aldioxa
    		Antagonist
    Aidioxa has the ability to improve delayed gastric emptying in rats. It can partially improve delayed gastric emptying caused by clonidine or restraint stress. The allyltoin part of Aidioxa restores gastric emptying activity by antagonizing α-2 adrenergic receptors. Its aluminum hydroxide part is involved in restoring gastric compliance. Aidioxa can improve both delayed gastric emptying and impaired gastric compliance, both of which play an important role in functional dyspepsia (FD). Aidioxa is a candidate agent for inhibiting FD.
    Aldioxa
  • HY-B0566R
    Guanabenz Acetate (Standard)
    		Agonist
    Guanabenz (Acetate) (Standard) is the analytical standard of Guanabenz (Acetate). This product is intended for research and analytical applications. Guanabenz (Acetate) (BR-750) is an alpha-2 selective adrenergic agonist used as an antihypertensive agent.
    Guanabenz Acetate (Standard)
  • HY-17416S
    Guanfacine-d2 hydrochloride
    		Agonist
    Guanfacine-d2 (hydrochloride) is the deuterium labeled Guanfacine hydrochloride. Guanfacine hydrochloride, an anti-hypertensive agent, is a selective α2A-adrenoceptor agonist with Kd of 31 nM and displays 60-fold selectivity over α2B-adrenoceptors.
    Guanfacine-d<sub>2</sub> hydrochloride
  • HY-14300AS
    Vilanterol-d4 trifenatate
    		Agonist
    Vilanterol-d4 (trifenatate) is deuterium labeled Vilanterol (trifenatate).Vilanterol (GW642444) acetate is a long-acting β2 adrenergic receptor agonist. Vilanterol acetate has pEC50 values for β2-AR, β1-AR, and β3-AR of 9.4, 6.4, and 6.1, respectively. Vilanterol acetate selectively activates airway β2 adrenergic receptors, increases cAMP and thus relaxes bronchial smooth muscle. Vilanterol acetate can be used in asthma research.
    Vilanterol-d<sub>4</sub> trifenatate
  • HY-15394A
    (Rac)-Rotigotine
    		Antagonist
    (Rac)-Rotigotine (N-0437) is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
    (Rac)-Rotigotine
  • HY-16736
    Centanafadine
    		Inhibitor 99.62%
    Centanafadine 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
  • HY-106874B
    rel-Delequamine
    rel-Delequamine (rel-RS-15385-197) is an orally active, brain-penetrant, potent and selective M2-adrenoceptor antagonist and α2-adrenoceptor antagonist. rel-Delequamine has a pKi of 9.45 for α2-adrenoceptors in the rat cortex. rel-Delequamine augments K+-evoked release of noradrenaline with an EC50 of 1 nM.
    rel-Delequamine
  • HY-17503BS
    Metoprolol-d6 tartrate
    		Antagonist
    Metoprolol-d6 (tartrate) is the deuterium labeled Metoprolol tartrate. Metoprolol is an orally active, selective β1-adrenoceptor antagonist. Metoprolol shows anti-inflammation, antitumor and anti-angiogenic properties.
    Metoprolol-d<sub>6</sub> tartrate
  • HY-B1035C
    ent-Levobunolol hydrochloride
    		Inhibitor
    ent-Levobunolol ((R)-Bunolol) hydrochloride is a competitive β-adrenergic receptor blocker. ent-Levobunolol hydrochloride inhibits the transmission of sympathetic nerve impulses, reduces the production of aqueous humor, and constricts blood vessels in the eye, thereby reducing intraocular pressure. ent-Levobunolol hydrochloride is promising for research of ocular hypertension diseases such as glaucoma.
    ent-Levobunolol hydrochloride
  • HY-123368
    Zolertine hydrochloride
    		Inhibitor
    Zolertine hydrochloride is an α-adrenoceptor antagonist with a pKi of 6.81 in rat liver (α1B-adrenoceptors) and 6.35 in rabbit liver (α1A-adrenoceptors) membranes.
    Zolertine hydrochloride
  • HY-B1486AS
    Oxprenolol-d7
    		Antagonist
    Oxprenolol-d7 is the deuterium labeled Oxprenolol. Oxprenolol (Ba 39089 free base) 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-d<sub>7</sub>
  • HY-B0532AS
    Trifluoperazine-d3 dihydrochloride
    		Antagonist
    Trifluoperazine-d3 (dihydrochloride) is deuterium labeled Trifluoperazine (dihydrochloride). 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-d<sub>3</sub> dihydrochloride
  • HY-15394S1
    (Rac)-Rotigotine-d3 hydrochloride
    		Antagonist
    (Rac)-Rotigotine-d3 hydrochloride is a deuterium labeled (Rac)-Rotigotine (hydrochloride) (HY-15394). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
    (Rac)-Rotigotine-d<sub>3</sub> hydrochloride
  • HY-B0659S
    Brimonidine-d4
    		Agonist
    Brimonidine-d4 is the deuterium labeled Brimonidine. Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist.
    Brimonidine-d<sub>4</sub>
  • HY-17034BS1
    Medetomidine-13C,d3 hydrochloride
    		Agonist
    Medetomidine-13C,d3 (hydrochloride) is a deuterated labeled Medetomidine (hydrochloride). Medetomidine hydrochloride is an orally active α2-adrenoceptor agonist (Ki: 1.08 nM). Medetomidine hydrochloride has sedative and analgesic effects. Medetomidine hydrochloride can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels.
    Medetomidine-<sup>13</sup>C,d<sub>3</sub> hydrochloride
  • HY-B0010S
    Formoterol-d6
    		Agonist
    Formoterol-d6 is the deuterium labeled Formoterol. Formoterol ((±)Formoterol) is a potent, selective and long-acting β2-adrenoceptor agonist.
    Formoterol-d<sub>6</sub>
  • HY-121312
    Flutonidine
    		Activator
    Flutonidine (ST-600) is a Clonidine (HY-12721) analogue that shows antihypertensive and sympatholytic effects. The initial hypertension produced by Flutonidine is due to stimulation of the peripheral α1, α2 adrenoceptors and the subsequent fall in blood pressure is due to the stimulation of central α2 adrenoceptors. Flutonidine reduces the arrhythmogenic and lethal effects of ouabain. Flutonidine is promising for research of ventricular arrhythmias caused by cardiac glycosides.
    Flutonidine
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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