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-B0371S
    Terazosin-d8
    		Antagonist
    Terazosin-d8 is deuterium labeled Terazosin. Terazosin is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin works by relaxing blood vessels and the opening of the bladder. Terazosin has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment.
    Terazosin-d<sub>8</sub>
  • 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-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-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>
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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