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-17457
    Levalbuterol hemitartrate
    Agonist 98.71%
    Levalbuterol (Levosalbutamol) hemitartrate is a β2-adrenergic receptor agonist and PI3K inhibitor. Levalbuterol hemitartrate inhibits PI3K activity, reduces NF-κB and Rb protein expression, activates the cAMP/PKA pathway, and stimulates cAMP release. Levalbuterol hemitartrate relaxes airway smooth muscle, reduces intracellular calcium levels, and inhibits spasmogen-induced contractions. Levalbuterol hemitartrate can be used for the research of moderate-to-severe asthma.
    Levalbuterol hemitartrate
  • HY-106523
    Nipradolol
    Inhibitor
    Nipradolol (KT-210; K-351) is a potent blocker of alpha-1-adrenergic receptors. Nipradolol inhibits the increase of intraocular pressure (IOP) in an albino rabbit model induced by Phenylephrine (HY-B0769). Nipradolo suppresses the noradrenaline (NA)-induced muscles contraction, also exhibits vasodilator activity on the dog coronary artery.
    Nipradolol
  • HY-100935S
    Cimaterol-d7
    Agonist
    Cimaterol-d7 is the deuterium labeled Cimaterol. Cimaterol is a potent agonist of β-adrenergic receptors (pEC50s=8.13, 8.78, and 6.62 for human β1, β2, and β3, respectively). Cimaterol has been used in farmed animals to increase carcass mass and to alter muscle and fat deposition.
    Cimaterol-d<sub>7</sub>
  • HY-W777156
    Carazolol-d6 hydrochloride
    Carazolol-d6 (hydrochloride) is deuterium labeled Carazolol hydrochloride (HY-W517264). Carazolol hydrochloride is a highly potent antagonist of β12 adrenoceptor. Carazolol hydrochloride is also a potent, selective β3-adrenoceptor agonist. Carazolol hydrochloride can be used in the research of hypertension.
    Carazolol-d<sub>6</sub> hydrochloride
  • HY-106418A
    SGB-1534 hydrochloride
    Antagonist
    SGB-1534 hydrochloride is an orally active, selective and competitive antagonist of the alpha 1-adrenoceptor and the 5-HT2 receptor. SGB-1534 hydrochloride can inhibit vasoconstriction and lower blood pressure. SGB-1534 hydrochloride can be used for the research of cardiovascular disease, such as hypertension.
    SGB-1534 hydrochloride
  • HY-B0006BS
    (S)-Carvedilol-d4
    Inhibitor
    (S)-Carvedilol-d4 is deuterium labeled (S)-Carvedilol. (S)-Carvedilol, the S-enantiomer of Carvedilol, is a non-selective β/α-1 blocker. (S)-Carvedilol exerts protection against the vascular or cardiac toxicity of Doxorubicin (DOX).
    (S)-Carvedilol-d<sub>4</sub>
  • HY-108901R
    Formoterol hemifumarate hydrate (Standard)
    Agonist
    Formoterol (hemifumarate hydrate) (Standard) is the analytical standard of Formoterol (hemifumarate hydrate). This product is intended for research and analytical applications. Formoterol hemifumarate hydrate is a selective, long-acting beta 2-adrenoceptor agonist. Formoterol is a bronchodilator used for the research of the asthma and chronic obstructive pulmonary disease (COPD). Formoterol hemifumarate hydrate induces mitochondrial biogenesis and promotes cognitive recovery after traumatic brain injury.
    Formoterol hemifumarate hydrate (Standard)
  • HY-P1582
    ACTH (1-14)
    Activator
    ACTH (1-14) is a fragment of adrenocorticotrophin, which regulates cortisol and androgen production.
    ACTH (1-14)
  • HY-U00237B
    L-771688 hydrochloride
    Antagonist
    L-771688 hydrochloride is a potent and highly selective α1A-adrenoceptor antagonist (Kd=43-90 pM). L-771688 hydrochloride is effective against cloned human, rat and dog α1A-adrenergic receptors. L-771688 exhibits high affinity (Ki ≤ 1 nM) and over 500-fold selectivity over the α1B and α1D isoforms. L-771688 potently antagonizes norepinephrine-induced responses at these receptors. Inhibits contractions induced by phenylephrine or A-61603 in rat, dog, human and monkey models.
    L-771688 hydrochloride
  • 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-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-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-19291
    DL-017
    Antagonist
    DL-017 is a Quinazoline derivative. DL-017 shows inhibitory constants of approximately 0.90 nM for α1-adrenergic receptors and 404 nM for Na+ channels. DL-017 exerts antihypertensive effect.
    DL-017
Cat. No. Product Name / Synonyms Application Reactivity

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