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-106769C
    Fluparoxan hydrochloride
    		Antagonist
    Fluparoxan hydrochloride is an orally active, selective and competitive alpha 2-adrenoceptor antagonist. Fluparoxan hydrochloride is an anti-depressant agent.
    Fluparoxan hydrochloride
  • 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-15413
    Edivoxetine
    		Inhibitor
    Edivoxetine (LY 2216684) is a potent and selective norepinephrine reuptake inhibitor. Edivoxetine can be used for the study of major depressive disorder (MDD) and attention-deficit/hyperactivity disorder (ADHD).
    Edivoxetine
  • HY-106973
    Nolomirole
    		Agonist
    Nolomirole (CHF 1035) is an orally active and selective DA2 dopaminergic receptor/α2-adrenoceptor agonist. Nolomirole attenuates the heart failure signs in the Monocrotaline (HY-N0750)-induced congestive heart failure model. Nolomirole increases cardiac output.
    Nolomirole
  • 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-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-N0378AGL
    D-Mannitol, M200 (GMP Like)
    D-Mannitol, M200 (GMP Like) (Mannitol, M200 (GMP Like)) is the GMP Like class D-Mannitol that can be used as pharmaceutical excipients. 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, M200 (GMP Like)
  • HY-107847
    2-(2-Methoxyphenoxy)ethylamine hydrochloride
    		Antagonist ≥98.0%
    2-(2-Methoxyphenoxy)ethylamine hydrochloride (Compound 2b) is a mixed agonist/antagonist. 2-(2-Methoxyphenoxy)ethylamine hydrochloride is a5-HT1A receptor partial agonist and a α1-adrenergic receptor antagonist. 2-(2-Methoxyphenoxy)ethylamine hydrochloride can be used for neurological diseases research, such as anxiety, depression and psychosis.
    2-(2-Methoxyphenoxy)ethylamine hydrochloride
  • 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).
    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-107358A
    Lidamidine hydrochloride
    		Agonist
    Lidamidine hydrochloride (WHR-1142A) is an α2-adrenergic receptor agonist and antidiarrheal agent.
    Lidamidine hydrochloride
  • 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
  • HY-122300B
    R-(-)-Oxaprotiline
    R-(-)-Oxaprotiline (Levoprotiline) is an antidepressant with anticholinergic and sympathostimulatory activities. R-(-)-Oxaprotiline exhibits different abilities to block norepinephrine uptake and anticholinergic activity compared to its enantiomer C 49802 B-Ba. R-(-)-Oxaprotiline in human studies shows physiological effects consistent with those in animals. Administration of R-(-)-Oxaprotiline results in a modest increase in heart rate and arterial blood pressure. Salivation is inhibited with R-(-)-Oxaprotiline, consistent with its anticholinergic properties. R-(-)-Oxaprotiline has similar effects to the established antidepressant compound Levoprotiline and has a shorter onset of action.
    R-(-)-Oxaprotiline
  • HY-14790
    Esreboxetine
    Esreboxetine ((S,S)-Reboxetine) is a selective norepinephrine reuptake inhibitor with activity in increasing urethral resistance. Esreboxetine has been reported to be effective in patients with stress urinary incontinence in a Phase IIa clinical study, achieving this effect by increasing urethral closure. The mechanism of action of esreboxetine involves inhibition of norepinephrine transporters in the central and peripheral nervous systems. The peripheral selectivity of esreboxetine helps it significantly increase urethral resistance without penetrating the brain.
    Esreboxetine
  • HY-118335
    Prazobind
    		Inhibitor
    Prazobind (SZL 49), a prazosin analog, is a selective α1-adrenoceptor antagonist. Prazobind competes for alpha 1-adrenoceptor binding sites with a similar potency (IC50 of 1 nM) in tissues enriched in both the alpha 1A (hippocampus) and alpha 1B (liver) subtypes. Prazobind can be used for the study of blood pressure.
    Prazobind
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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