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-N0132R
    Synephrine (Standard)
    		Agonist
    Synephrine (Standard) is the analytical standard of Synephrine. This product is intended for research and analytical applications. Synephrine (Oxedrine), an alkaloid, is an α-adrenergic and β-adrenergic agonist derived from the Citrus aurantium. Synephrine is a sympathomimetic compound and can be used for weight loss.
    Synephrine (Standard)
  • HY-106554
    Trimazosin
    		Antagonist
    Trimazosin is an orally active, quinazoline derivative which is structurally related to prazosin. Trimazosin shows hypotensive effect by selectively block α1-adrenoceptors.
    Trimazosin
  • HY-103216A
    RWJ52353 hydrochloride
    		Agonist
    RWJ-52353 hydrochloride is an orally potent, highly selective α2D adrenergic receptor agonist (Ki: 1.5 nM) with potential analgesic effects. RWJ-52353 hydrochloride demonstrated analgesic activity in abdominal tests in rats and mice, and improved agitation in mice in the hot plate test and tail flick test. RWJ-52353 hydrochloride also regulates the organic cation transporter (OCT) subtype, inhibiting rOCT1 and rOCT2 with IC50s of 100 μM and 20 μM respectively; it also activates rOCT3, affecting [3H]-1- in cells. Methyl-4-phenylpyridinium ([3H]MPP) transport.
    RWJ52353 hydrochloride
  • HY-B0371AR
    Terazosin hydrochloride dihydrate (Standard)
    		Antagonist
    Terazosin (hydrochloride dihydrate) (Standard) is the analytical standard of Terazosin (hydrochloride dihydrate). This product is intended for research and analytical applications. Terazosin hydrochloride dihydrate is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin hydrochloride dihydrate works by relaxing blood vessels and the opening of the bladder. Terazosin hydrochloride dihydrate has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment.
    Terazosin hydrochloride dihydrate (Standard)
  • HY-B0391A
    Naftopidil dihydrochloride
    		Antagonist
    Naftopidil dihydrochloride (KT-611 dihydrochloride) is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil dihydrochloride has antiproliferative effects. Naftopidil dihydrochloride can be used for the research of prostate hyperplasia.
    Naftopidil dihydrochloride
  • HY-163363
    β-AR antagonist 2
    		Antagonist
    β-AR antagonist 2 (compound 43) is an antagonist of β-AR (IC50: 0.17 μM). β-AR-IN-1 inhibits the growth of mouse A549 xenograft tumors and shows cardioprotective efficacy against DOX-induced HF in C57 mice.
    β-AR antagonist 2
  • HY-B1296S1
    Promethazine-d4
    Promethazine-d4 is a deuterated-labeled promethazine (HY-B0781). Promethazine is an orally active H1 receptor and mAChR antagonist with antihistamine (H1), sedative, antiemetic, anticholinergic, and anti-motion sickness properties.
    Promethazine-d<sub>4</sub>
  • HY-127128
    Flestolol sulfate
    		Inhibitor
    Flestolol (ACC-9089) sulfate is a competitive, ultra-short-acting beta-adrenergic blocking agent. Flestolol sulfate shows a half-life of approximately 6.5 minutes. Flestolol sulfate has the potential for the research of chest pain.
    Flestolol sulfate
  • HY-14903
    Ulimorelin
    		Antagonist
    Ulimorelin (TZP-101) is a ghrelin receptor (GRLN) agonist with an EC50 of 29 nM and a Ki of 16 nM. Ulimorelin is a prokinetic agent and causes vasorelaxation through competitive antagonist action at α1-adrenoceptors. Ulimorelin stimulates intestinal motility and is used for malnutrition.
    Ulimorelin
  • HY-17034AR
    Dexmedetomidine hydrochloride (Standard)
    		Agonist
    Dexmedetomidine (hydrochloride) (Standard) is the analytical standard of Dexmedetomidine (hydrochloride). This product is intended for research and analytical applications. Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine hydrochloride shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine hydrochloride exhibits anxiolysis, sedation, and modest analgesia effects.
    Dexmedetomidine hydrochloride (Standard)
  • HY-B0437AS
    Sotalol-d6 hydrochloride
    		Antagonist ≥99.0%
    Sotalol-d6 (hydrochloride) is a deuterium labeled Sotalol hydrochloride. Sotalol hydrochloride is an orally active, non-selective competitive β-adrenergic receptor blocker. Sotalol hydrochloride is a potent antiarrhythmic agent that can be used for the research of pediatric arrhythmias. Sotalol hydrochloride blocks β-receptors, and potassium KCNH2 channels[1][2].
    Sotalol-d<sub>6</sub> hydrochloride
  • HY-101338
    RS-79948-197
    		Antagonist
    RS-79948-197 is a non-imidazoline α2-adrenoceptor antagonist. RS-79948-197 shows Kd values of 0.42 nM, 0.18 nM, 0.19 nM, 0.60 nM, 0.46 nM, and 0.77 nM for rat α2A, rat α2B, rat α2C, human α2A, human α2B, and human α2C, respectively.
    RS-79948-197
  • HY-101392S1
    Harmane-d2
    		Inhibitor
    Harmane-d2 is the deuterium labeled Harmane. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively)[1][2][3][4].
    Harmane-d<sub>2</sub>
  • HY-14897
    Rezatomidine
    		Agonist
    Rezatomidine (AGN-203818) is a potent and selective α2-AR agonist. Rezatomidine can be used for diabetic neuropathy and neuropathic pain research.
    Rezatomidine
  • HY-B0006S
    Carvedilol-d3
    		Inhibitor
    Carvedilol-d3 is the deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker[1]. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure[2]. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome[3].
    Carvedilol-d<sub>3</sub>
  • HY-107358A
    Lidamidine hydrochloride
    		Agonist
    Lidamidine hydrochloride (WHR-1142A) is an α2-adrenergic receptor agonist and antidiarrheal agent.
    Lidamidine hydrochloride
  • HY-155879
    (±)-N-Methylcoclaurine
    		Antagonist
    (±)-N-Methylcoclaurine is a selective α2-adrenoceptor antagonist.
    (±)-N-Methylcoclaurine
  • HY-136474
    Amidephrine
    		Agonist
    Amidephrine is a selective agonist of alpha 1-adrenoceptor. Amidephrine inhibits inhibits monopulse field contraction of the vas deferens epithelium and prostate gland.
    Amidephrine
  • HY-121578
    Agaridoxin
    		Antagonist
    Agaridoxin (GDHB) is a blocker of catecholamine and adrenergic alpha-type receptors isolated from mushrooms. Agaridoxin activates adenylyl cyclase in rat hypothalamic membrane granules in the presence of guanosyl imide diphosphate (Gpp(NH)p).
    Agaridoxin
  • HY-B0192AS1
    Alfuzosin-d7 hydrochloride
    		Antagonist
    Alfuzosin-d7 (hydrochloride) is the deuterium labeled Alfuzosin hydrochloride. Alfuzosin hydrochloride is an α1 adrenergic receptor antagonist used to treat benign prostatic hyperplasia (BPH).
    Alfuzosin-d<sub>7</sub> hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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