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-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.
    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).
    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
  • HY-W009027
    Indoramin hydrochloride
    Indoramin (hydrochloride) is a new hypotensive agent. Indoramin (hydrochloride) is also selective for the α1A-adrenoceptor.
    Indoramin hydrochloride
  • HY-W722221
    Colterol acetate
    		Antagonist
    Colterol acetate is a selective inhibitor of β-adrenergic receptors. Colterol acetate can relax tracheal smooth muscle (primarily acting on β2 receptors), reduce subspastic contractions of tricholoma (acting on β2), and increase contractility of left ventricular papillary muscles (acting on β1).
    Colterol acetate
  • HY-136960
    β2AR antagonist 1
    		Antagonist
    β2AR antagonist 1 (Cmpd-15PA) is an antagonist of β2 adrenergic receptor (β2AR). β2AR antagonist 1 binds to the intracellular surface of the β2AR.
    β2AR antagonist 1
  • HY-106518
    Adimolol free base
    		Antagonist
    Adimolol (free base) (MEN 935 (free base)) is an antagonist of β- and α-adrenolytic receptor. Adimolol (free base) shows Kis of 5.2 x 10-7, 1.3 x 10-5 mol/L at α1 and α2 drenoceptors, respectively. Adimolol (free base) can be used for antihypertensive study.
    Adimolol free base
  • HY-A0252A
    Bupranolol hydrochloride
    Bupranolol hydrochloride is a non-selective β-adrenergic blocker with potent membrane stabilizing activity. Bupranolol hydrochloride is able to significantly modulate the contractile activity of the non-pregnant human uterus. Bupranolol hydrochloride showed significant effects on spontaneous uterine contractions in an in vitro study in patients with ovarian cancer. Bupranolol hydrochloride is similar in potency to propranolol, another β-adrenergic blocker. Bupranolol hydrochloride is rapidly and completely absorbed in vivo, and its major metabolite is carboxybupranolol.
    Bupranolol hydrochloride
  • HY-162659
    β2AR ligand 1
    β2AR ligand 1 (Compound 4) is a homobivalent bitopic ligand for β2 adrenergic receptor (β2AR) on the orthosteric binding site (OBS) and the metastable binding sites (MBS).
    β2AR ligand 1
  • HY-157502S
    Buctopamine-d9
    		Agonist
    Buctopamine-d9 is the deuterium labeled Buctopamine. Buctopamine is a β2 adrenoceptor agonist.
    Buctopamine-d<sub>9</sub>
  • HY-W777360
    Harman-13C2,15N
    		Inhibitor
    Harman-13C2,15N is 13C and 15N labeled Harmane. Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane also inhibits haloperidol and serotonin, with IC50 values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).
    Harman-<sup>13</sup>C<sub>2</sub>,<sup>15</sup>N
  • HY-106523
    Nipradolol
    		Inhibitor
    Nipradolol (KT-210; K-351) is a potent blocker of alpha-1-adrenergic receptors. Nipradolol inhibits the increase of intraocular pressure (IOP) in an albino rabbit model induced by Phenylephrine (HY-B0769). Nipradolo suppresses the noradrenaline (NA)-induced muscles contraction, also exhibits vasodilator activity on the dog coronary artery.
    Nipradolol
  • HY-100935S
    Cimaterol-d7
    		Agonist
    Cimaterol-d7 is the deuterium labeled Cimaterol. Cimaterol is a potent agonist of β-adrenergic receptors (pEC50s=8.13, 8.78, and 6.62 for human β1, β2, and β3, respectively). Cimaterol has been used in farmed animals to increase carcass mass and to alter muscle and fat deposition.
    Cimaterol-d<sub>7</sub>
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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