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-B1506AR
    Acepromazine maleate (Standard)
    		Antagonist
    Acepromazine (maleate) (Standard) is the analytical standard of Acepromazine (maleate). This product is intended for research and analytical applications. Acepromazine (Acetopromazine) maleate is a phenothiazine tranquilizer and is alpha-adrenoceptor antagonist[2.
    Acepromazine maleate (Standard)
  • HY-W710337
    Colterol hydrochloride-d9
    Colterol hydrochloride-d9 is the deuterium labeled Colterol hydrochloride (HY-128510A). Colterol hydrochloride is the hydrochloride salt form of Colterol (HY-128510). Colterol hydrochloride is the agonist for adrenergic receptor, and exhibits good affinity to β1-adrenoreceptor (heart) and β2-adrenoreceptor (lung) with IC50 of 645 nM and 147 nM. Colterol hydrochloride exhibits potential as a bronchodilator.
    Colterol hydrochloride-d<sub>9</sub>
  • HY-149503
    4-Hydroxy nebivolol hydrochloride
    		Inhibitor
    4-Hydroxy nebivolol (4-OH nebivolol) hydrochloride is an active β-blocking hydroxylated metabolite of Nebivolol (HY-B0203).
    4-Hydroxy nebivolol hydrochloride
  • HY-N1919A
    Ajmalicine hydrochloride
    		Inhibitor
    Ajmalicine (Raubasine) hydrochloride is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine hydrochloride is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine hydrochloride also can be used as anti-hypertensive, and serpentine, with sedative activity.
    Ajmalicine hydrochloride
  • HY-139727
    S(-)-Bisoprolol
    S(-)-Bisoprolol is a S(-)-enantiomer of Bisoprolol. Bisoprolol is a potent, selective and orally active β1-adrenergic receptor blocker. Bisoprolol has little activity on β2-receptor and has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.
    S(-)-Bisoprolol
  • HY-19037
    SM-2470
    		Antagonist
    SM-2470 is a potent α1-adrenoceptor antagonist, has sympathetic nerve activity in anesthetized rats. SM-2470 is an antihypertensive agent. SM-2470 exhibits hypocholesterolaemic effect by the inhibition of cholesterol absorption related to the reduction of cholesterol solubilization.
    SM-2470
  • HY-W717221
    Medetomidine-d5 (d5-Major)
    Medetomidine-d5 (d5-Major) is the deuterium labeled Medetomidine (HY-17034). Medetomidine is an orally active α2-adrenoceptor agonist (Ki: 1.08 nM). Medetomidine has sedative and analgesic effects. Medetomidine can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels.
    Medetomidine-d<sub>5</sub> (d5-Major)
  • HY-106720C
    (+)-Amosulalol
    		Inhibitor
    (+)-Amosulalol ((+)-YM 09538) is an isomer of Amosulalol (HY-106720), an orally active dual inhibitor of α1/β1-adrenergic receptors. Amosulalol exhibits antihypertensive activity by inhibiting α1-adrenergic receptors. Amosulalol reduces the reflex increase in heart rate and plasma renin activity (PRA) in spontaneously hypertensive rats (SHR) by inhibiting β1-adrenergic receptors.
    (+)-Amosulalol
  • HY-117046
    AVN-101
    		Inhibitor
    AVN-101 is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56  nM, and 1.17  nM, respectively). AVN-101 also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 can be studied in such diseases as general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis.
    AVN-101
  • HY-135242
    LY87130 free base
    LY87130 free base is an octopamine-N-methyltransferase inhibitor with epinephrine-inhibiting activity. LY87130 free base can significantly reduce the basal level of epinephrine in the hypothalamus after administration. LY87130 free base has no significant effect on the basal levels of norepinephrine, 3,4-dihydroxyphenylacetic acid (DOPAC) and 5-hydroxyindoleacetic acid (5-HIAA) in the hypothalamus.
    LY87130 free base
  • HY-121843
    Ronactolol
    		Antagonist
    Ronactolol, an aminopropanol derivative with β-adrenoceptor blocking activity.
    Ronactolol
  • HY-W653969
    Arotinolol-d5 hydrochloride
    		Antagonist
    Arotinolol-d5 (hydrochloride) is deuterium labeled Arotinolol. Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases.
    Arotinolol-d<sub>5</sub> hydrochloride
  • HY-B0475R
    Xylometazoline hydrochloride (Standard)
    		Agonist
    Xylometazoline (hydrochloride) (Standard) is the analytical standard of Xylometazoline (hydrochloride). This product is intended for research and analytical applications. Xylometazoline hydrochloride is an α-adrenergic receptor agonist (Ki=0.05-1.7 μM). Xylometazoline hydrochloride can constrict nasal blood vessels and increase nasal airflow. Xylometazoline hydrochloride can be used in nose stuffiness and runny nose research.
    Xylometazoline hydrochloride (Standard)
  • HY-14541S2
    Olanzapine-d8
    		Antagonist
    Olanzapine-d8 is a deuterated labeled Olanzapine. Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic.
    Olanzapine-d<sub>8</sub>
  • HY-17497
    Acebutolol
    		Antagonist
    Acebutolol is an orally active β1 adrenergic receptor (β1AR) antagonist. Acebutolol is used for hypertension, angina pectoris and cardiac arrhythmias research.
    Acebutolol
  • HY-120829
    Bisoprolol fumarate
    		Inhibitor
    Bisoprolol fumarate is a potent, selective and orally active β1-adrenergic receptor blocker with little activity on β2-receptor. Bisoprolol fumarate has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.
    Bisoprolol fumarate
  • HY-106079
    Fezolamine
    		Inhibitor
    Fezolamine is an orally active non-tricyclic compound , and shows antidepressant activity.
    Fezolamine
  • HY-P4456
    (Des-His6)-ACTH (1-24) (human, bovine, rat)
    (Des-His6)-ACTH (1-24) (human, bovine, rat) is an analogue of Adrenocorticotropic hormone (ACTH; HY-106373). ACTH is a polypeptide tropic hormone produced by the anterior pituitary gland, regulating cortisol and androgen production.
    (Des-His6)-ACTH (1-24) (human, bovine, rat)
  • HY-13338A
    (S)-Mabuterol
    		Agonist
    (S)-Mabuterol is a selective β2 adrenoreceptor agonist that demonstrates blood pressure reduction and increased heart rate and contractile force in animal models.
    (S)-Mabuterol
  • HY-B1562B
    Bopindolol (malonate)
    		Antagonist
    Bopindolol ((±)-Bopindolol) malonate is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol malonate is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol malonate has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol malonate is a proagent of Pindolol (HY-B0982). Bopindolol malonate can be used for essential and renovascular hypertension research.
    Bopindolol (malonate)
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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