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-157502S
    Buctopamine-d9
    		Agonist
    Buctopamine-d9 is the deuterium labeled Buctopamine. Buctopamine is a β2 adrenoceptor agonist.
    Buctopamine-d<sub>9</sub>
  • HY-106863
    BRL 35135
    		Agonist
    BRL 35135 is a potent and selective β3-adrenergic receptor agonist. BRL 35135 can dose dependently increase energy expenditure, reduce weight, and only reduce fat without reducing muscle protein. BRL 35135 can significantly improve glucose tolerance and insulin sensitivity. BRL 35135 can be used to study metabolic conditions such as obesity and diabetes.
    BRL 35135
  • HY-W777360
    Harman-13C2,15N
    		Inhibitor
    Harman-13C2,15N is 13C and 15N labeled Harmane. Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane also inhibits haloperidol and serotonin, with IC50 values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).
    Harman-<sup>13</sup>C<sub>2</sub>,<sup>15</sup>N
  • 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 β1/β2 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-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
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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