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-107326A
    Bunazosin hydrochloride
    		Antagonist
    Bunazosin hydrochloride is a potent and selective α1-adrenoceptor antagonist. Bunazosin hydrochloride can be used for antihypertensive and ocular hypotensive research.
    Bunazosin hydrochloride
  • HY-167939
    (R)-Bambuterol
    (R)-Bambuterol is a β2-receptor agonist with anti-asthmatic and colitis-improving activity. (R)-Bambuterol is indicated for the treatment of asthma and chronic obstructive pulmonary disease and has the advantage of a once-daily dosing and a favorable side effect profile. (R)-Bambuterol significantly reduced disease severity in a mouse model of colitis, more effectively than (RS)-Bambuterol or (S)-Bambuterol. (R)-Bambuterol can significantly reduce the levels of inflammatory cytokines and reduce the infiltration of macrophages in mice with colitis. (R)-Bambuterol also increases β2-adrenoceptor levels and reduces the expression of IL-6, IL-17 and other related proteins in colon tissue in a dose-dependent manner.
    (R)-Bambuterol
  • HY-120519
    L-665871
    		Agonist
    L-665871 is a orally active β-adrenergic receptor agonist that can be used as a swine growth promoter.
    L-665871
  • HY-116062
    JNJ-7925476 hydrochloride
    		Inhibitor
    JNJ-7925476 (hydrochloride) is a triple monoamine uptake inhibitor with the ability to regulate neurotransmitter levels and antidepressant activity. JNJ-7925476 (hydrochloride) can be rapidly absorbed into the plasma in rats, with a higher concentration in the brain than in plasma. It can induce an increase in the levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex, and exhibits antidepressant activity in the mouse tail suspension test.
    JNJ-7925476 hydrochloride
  • HY-B0471S
    Phenylephrine-d3 hydrochloride
    		Agonist
    Phenylephrine-d3 (hydrochloride) is the deuterium labeled Phenylephrine hydrochloride. (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
    Phenylephrine-d<sub>3</sub> hydrochloride
  • HY-B0549S
    Flavoxate-d5
    		Ligand
    Flavoxate-d5 is deuterium labeled Flavoxate. Flavoxate hydrochloride (Rec-7-0040; DW61) is an orally active L-type Ca2+ channel inhibitor and antispasmodic. Flavoxate hydrochloride inhibits cyclic adenosine monophosphate production by blocking voltage-dependent inward Ba2+ currents, regulating the brainstem micturition center, and stimulating G protein-coupled receptors. Consequently, Flavoxate hydrochloride induces relaxation of bladder smooth muscle and inhibits isovolumetric rhythmic contractions. Flavoxate hydrochloride effectively increases bladder capacity and alleviates symptoms of urgent urination frequency and pollakiuria caused by overactive bladder. Flavoxate hydrochloride can be used in research on overactive bladder and related voiding dysfunctions.
    Flavoxate-d<sub>5</sub>
  • HY-135487
    Sibenadet
    		Agonist
    Sibenadet (AR-C68397AA free base) is a dual dopamine D2/β2-adrenoceptor agonist with selective β2-adrenoceptor agonism. Sibenadet inhibits capsaicin-induced plasma protein extravasation in rat trachea. Sibenadet suppresses edema from sensory nerve fiber activation by activating β2-adrenoceptor. Sibenadet is promising for research of chronic obstructive pulmonary disease (COPD).
    Sibenadet
  • HY-W707640
    Salbutamol-d4
    Salbutamol-d4 (Albuterol-d4; AH-3365-d4) is the deuterium labeled Salbutamol (HY-B1037). Salbutamol (Albuterol) is a short-acting beta-2 adrenergic receptor agonist with oral activity. Salbutamol promotes tumorigenesis of gastric cancer cells through the β2-AR/ERK/EMT pathway. Salbutamol is used to study bronchospasms caused by asthma and chronic obstructive pulmonary disease (COPD).
    Salbutamol-d<sub>4</sub>
  • HY-W556123
    Piperoxan
    		Antagonist
    Piperoxan is an α1-adrenergic receptor antagonist. Piperoxan exhibits a Ki value of 360 nM for inhibiting 3H-prazosin binding to rat brain α1-adrenoceptors. Piperoxan can be used for the research of adrenergic system-related diseases.
    Piperoxan
  • HY-106388A
    Fadolmidine hydrochloride
    		Agonist
    Fadolmidine hydrochloride is a novel, selective α2-adrenoceptor (α2-AR) agonist with EC50 values of 0.4 nM, 4.9 nM and 0.5 nM for 2A, 2B and 2C, respectively. Fadolmidine hydrochloride has been effective against various submodalities of pain such as heat pain, mechanical pain, and visceral pain. Fadolmidine hydrochloride inhibits also electrically evoked contractions in rat vas deferens.
    Fadolmidine hydrochloride
  • HY-123044
    Tedatioxetine
    		Antagonist
    Tedatioxetine (Lu AA24530) acts as a serotonin and norepinephrine (NE)-preferring triple reuptake inhibitor (TRI) and 5-HT2A, 5-HT2C, 5-HT3 and α1A-adrenergic receptor antagonist.
    Tedatioxetine
  • HY-148524
    β2AR/M-receptor agonist-1
    		Agonist
    β2AR/M-receptor agonist-1 (example 131) is a muscarinic antagonist and β2 adrenoceptor agonist (MABA). β2AR/M-receptor agonist-1 shows potency to β2 adrenoceptor with an EC50 value of 9.2 nM. β2AR/M-receptor agonist-1 also has potency to muscarinic receptor with a Ki value of 30.2 nM. β2AR/M-receptor agonist-1 shows MABA potency with an EC50 value of 4.0 nM.
    β2AR/M-receptor agonist-1
  • HY-B0983R
    Hydrocortisone 17-butyrate (Standard)
    		Agonist
    Hydrocortisone 17-butyrate (Standard) is the analytical standard of Hydrocortisone 17-butyrate. This product is intended for research and analytical applications. Hydrocortisone 17-butyrate is a non-fluorinated topical corticosteroid for use in psoriasis, eczema, and other inflammatory dermatoses. Hydrocortisone 17-butyrate inhibits granuloma formation in rats. Hydrocortisone 17-butyrate can induce vasoconstriction.
    Hydrocortisone 17-butyrate (Standard)
  • HY-178413S
    D-Mannitol-d4
    D-Mannitol-d4 (Mannitol-d4) is the deuterium labeled D-Mannitol (HY-N0378). D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β3-adrenergic receptor (β3-AR), PGC1α and PKA induced by means of white fat cells into brown fat cells. D-Mannitol is commonly used to maintain osmotic pressure between the plant cytoplasm and the culture medium and protect cells when the cell wall is weakened or even removed.
    D-Mannitol-d<sub>4</sub>
  • HY-W704363
    Pimozide-d5
    Pimozide-d5 (R6238-d5) is the deuterium labeled Pimozide (HY-12987). Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
    Pimozide-d<sub>5</sub>
  • HY-118039
    Abanoquil methylsulfate
    		Antagonist
    Abanoquil methylsulfate (UK-52046 methylsulfate) is an alpha-1 family adrenergic receptor antagonist. Abanoquil methylsulfate can be used in research on cardiovascular diseases such as arrhythmias and erectile dysfunction.
    Abanoquil methylsulfate
  • HY-B1435A
    Moxisylyte
    Moxisylyte (Thymoxamine) is a selective α1A-adrenergic receptor antagonist. Moxisylyte competitively antagonizes the activation mediated by norepinephrine. Moxisylyte relaxes penile cavernous smooth muscle and aids erectile function. Moxisylyte is applicable to research related to erectile dysfunction and multiple system atrophy.
    Moxisylyte
  • HY-W471937
    α1B-AR antagonist 1
    		Antagonist
    α1b-AR antagonist 1 (Compound Cpd1) is a selective α1B-AR antagonist. Alpha1b-ar antagonist 1 can be used in the study of cardiovascular and central nervous system diseases.
    α1B-AR antagonist 1
  • HY-121670A
    Ambenoxan hydrochloride
    Ambenoxan hydrochloride is a central nervous system-acting skeletal muscle relaxant that is effective in mice, rats, rabbits, dogs, and monkeys without loss of the righting reflex. It has no peripheral neuromuscular blocking effects and significantly reduces or eliminates decerebrate rigidity in rabbits, but does not antagonize the effects of strychnine, leptazol, or tremorine. Like other central nervous system depressants, ambenoxan prolongs sleep duration with hexobarbitone, but it has no local anesthetic effects. In anesthetized cats, the agent lowers blood pressure and reduces the pressor response to epinephrine, but has no effect on norepinephrine.
    Ambenoxan hydrochloride
  • HY-B1035A
    Levobunolol
    		Antagonist
    Levobunolol (l-Bunolol) is a non-selective β-adrenergic antagonist and vasodilator. By blocking calcium ion influx and reducing the sensitivity of vascular smooth muscle to calcium, Levobunolol effectively dilates the ciliary arteries and increases ocular blood flow, so it is widely used in research on glaucoma and ocular hypertension. Levobunolol inhibits the β-receptor signaling pathway and the expression of related proliferation markers (such as CK3, CK14, CK19, Ki67) in corneal cells. In rabbit models, Levobunolol not only does not inhibit corneal epithelial regeneration, but also accelerates the healing of mechanical injury without adverse effects. Levobunolol also inhibits histamine-induced vasoconstriction and intracellular calcium elevation, exhibiting unique vascular regulatory activity. Levobunolol protects ocular blood flow and promotes corneal repair.
    Levobunolol
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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