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-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-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-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-B1435A
    Moxisylyte
    Moxisylyte (Thymoxamine) is an alpha 1-selective antagonist with activity that improves bladder emptying. Moxisylyte is used to suppress urinary difficulties in patients with multiple system atrophy (MSA) by blocking alpha 1-adrenergic receptors to reduce the amount of residual urine after urination. Moxisylyte is also used to suppress erectile dysfunction and can improve blood circulation problems caused by Raynaud's syndrome in the short term. In addition, Moxisylyte can be applied topically to the eye to reverse the mydriasis caused by phenylephrine and other sympathetic stimulants.
    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 potent and nonselective β-adrenergic receptor antagonist. Levobunolol is an ocular hypotensive agent and lowers mean intraocular pressure (IOP). Levobunolol can be used for glaucoma and superior oblique myokymia (SOM) research.
    Levobunolol
  • HY-130418
    (-)-Domesticine
    (-)-Domesticine is an anti-α-1D-adrenoceptor compound with cytotoxic activity. (-)-Domesticine showed activity in MTS cytotoxicity assays against human colon cancer cell lines HCT-116 and Caco-2. (-)-Domesticine tolerates alkoxy substituents and benzoate functional groups at the C1 position in modifications of its chemical structure. The most potent compounds of (-)-Domesticine have IC50 values in the range of 23-38 μM, similar to the known cytotoxic compound etoposide.
    (-)-Domesticine
  • HY-101061
    2-MPMDQ
    		Antagonist
    2-MPMDQ is a potent and selective α1-adrenoceptor (Ki=0.37 nM) antagonist over α2-adrenoceptor (Ki=1740 nM). 2-MPMDQ is potent anti-hypertensive agent and has the potential for hypertension research.
    2-MPMDQ
  • HY-19942
    TD-5471
    		Agonist
    TD-5471 is a potent and selective full agonist of the human β2-adrenoceptor.
    TD-5471
  • HY-W744038
    Zotepine-d6
    Zotepine-d6 is the deuterium labeled Zotepine (HY-103093). Zotepine, an antipsychotic agent, is a potent antagonist of 5-HT2A, 5-HT2C, Histamine H1, α1-adrenergic and Dopamine D2 receptors, with Kds of 2.6 nM, 3.2 nM, 3.3 nM, 7.3 nM and 8 nM, respectively. Zotepine exhibits antidepressive and anxiolytic effects in vivo.
    Zotepine-d<sub>6</sub>
  • HY-B0716S2
    Urapidil-d4
    		Antagonist
    Urapidil-d4 is the deuterium labeled Urapidil. Urapidil is an α1 adrenoreceptor antagonist and a 5-HT1A receptor agonist.
    Urapidil-d<sub>4</sub>
  • HY-106499
    Sulfinalol
    		Antagonist
    Sulfinalol is an orally active β-adrenoceptor antagonist with direct vasodilator activity.
    Sulfinalol
  • HY-13338S
    Mabuterol-d9
    		Agonist
    Mabuterol-d9 is a deuterium labeled Mabuterol. Mabuterol is an agonist of the β2-adrenergic receptor.
    Mabuterol-d<sub>9</sub>
  • HY-B0203AR
    Nebivolol hydrochloride (Standard)
    		Inhibitor
    Nebivolol (hydrochloride) (Standard) is the analytical standard of Nebivolol (hydrochloride). This product is intended for research and analytical applications. Nebivolol (R 065824) hydrochloride is an orally active beta receptor blocker and has the high beta(1)-receptor affinity.Nebivolol hydrochloride has direct vasodilator properties and adrenergic blocking characteristics. Nebivolol hydrochloride can be used for the research of kinds of diseases such as hypertension, coronary artery disease, congestive heart failure and ischemic heart disease.
    Nebivolol hydrochloride (Standard)
  • HY-165495
    Pafenolol
    		Antagonist
    Pafenolol is a selectively oral-active β1 adrenergic receptor (β1-adrenergic receptor) antagonist that effectively lowers blood pressure. Pharmacokinetic studies in rats indicate that the absorption of Pafenolol is influenced by gastrointestinal contents, with food intake reducing the bioavailability of Pafenolol in rats. Pafenolol can be used in research related to cardiovascular diseases and asthma.
    Pafenolol
  • HY-131449
    Terazosin dimer impurity dihydrochloride
    		Antagonist
    Terazosin dimer impurity dihydrochloride, a dimer of Terazosin, is an impurity of Terazosin. Terazosin is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist.
    Terazosin dimer impurity dihydrochloride
  • HY-100634R
    4-Hydroxypropranolol hydrochloride (Standard)
    		Antagonist
    4-Hydroxypropranolol (hydrochloride) (Standard) is the analytical standard of 4-Hydroxypropranolol (hydrochloride). This product is intended for research and analytical applications. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol. 4-Hydroxypropranolol hydrochlorid is of comparable potency to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties.
    4-Hydroxypropranolol hydrochloride (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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