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-B1486
    Oxprenolol hydrochloride
    		Antagonist 99.86%
    Oxprenolol hydrochloride (Ba 39089) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle.
    Oxprenolol hydrochloride
  • HY-B0781
    Promethazine hydrochloride
    		99.85%
    Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors.
    Promethazine hydrochloride
  • HY-B1276
    Metaproterenol hemisulfate
    		Agonist 99.44%
    Metaproterenol hemisulfate (Orciprenaline hemisulfate) is a direct-acting sympathomimetic and a β2-adrenergic receptor (β2AR) agonist with an IC50 of 68 nM. Metaproterenol hemisulfate also has anti-inflammatory activity.
    Metaproterenol hemisulfate
  • HY-101327A
    Xamoterol hemifumarate
    		Agonist ≥99.0%
    Xamoterol (Corwin; ICI 118587) hemifumarate is an orally active and selective β1-adrenoceptor partial agonist. Xamoterol hemifumarate acts as agonist at low sympathetic tone, antagonist at high sympathetic tone, with context-dependent cardiovascular effects including modulated heart rate, blood pressure, and cardiac output. Xamoterol hemifumarate can be used for the research of heart failure, postural hypotension, and ischemic heart disease.
    Xamoterol hemifumarate
  • HY-132184
    5,6-Epoxyeicosatrienoic acid
    		99.9%
    5,6-Epoxyeicosatrienoic acid (5,6-EET; (±)5,6-EpETrE) is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5,6-Epoxyeicosatrienoic acid degrades into 5,6-DiHET and 5,6-δ-lactone, which can be converted to 5,6-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5,6-Epoxyeicosatrienoic acid has been implicated in the mobilization of calcium and hormone secretion. 5,6-Epoxyeicosatrienoic acid is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50=0.54 μM), and Cav3. and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2.
    5,6-Epoxyeicosatrienoic acid
  • HY-17495A
    Carteolol hydrochloride
    		Antagonist 99.96%
    Carteolol hydrochloride (OPC-1085 hydrochloride) is a non-selective beta blocker used to treat glaucoma.
    Carteolol hydrochloride
  • HY-B0371A
    Terazosin hydrochloride dihydrate
    		Antagonist 99.92%
    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
  • HY-B1110
    Nomifensine
    		Inhibitor 98.93%
    Nomifensine ((±)-Nomifensine) is a potent norepinephrine (NE) and dopamine (DA) reuptake inhibitor. Nomifensine inhibits uptake of NE, DA and 5-HT in rat brain synaptosomes, with IC50 values of 6.6 nM, 48 nM and 830 nM, and Ki values of 4.7 nM, 26 nM and 4000 nM, respectively. Nomifensine has antidepressant and analgesic effects. Nomifensine is used in neurodegenerative diseases, compound addiction, and pain research.
    Nomifensine
  • HY-101366
    A-61603
    		Agonist 99.34%
    A-61603 is a selective α1A/α1a-adrenergic receptor agonist with Ki of 8.89 nM for rat submaxillary gland α1A, Ki of 30.5 nM for cloned bovine α1a. A-61603 potentiates Ca2+ transients with EC50 of 6.9 nM. A-61603 stimulates phosphoinositide hydrolysis, induces contractile responses in vas deferens, prostate strips, and spleen strips, and exhibits low activity in aortic rings. A-61603 can be used for research on adrenergic function.
    A-61603
  • HY-17549
    Adrafinil
    		Agonist 99.85%
    Adrafinil (CRL 40028) is an orally active vigilance promoting agent. Adrafinil enhances central noradrenergic transmission, improves spontaneous activity, exploratory behavior, discriminative learning ability and response motivation, but impairs visuospatial working memory. Adrafinil antagonizes Prazosin (HY-B0193)-induced hypoactivity and hypothermia, exerts anticonvulsant effects, and induces sustained enhancement of high-frequency electrocortical activity. Adrafinil can be used for research on decreased alertness and specific cognitive deficits.
    Adrafinil
  • HY-B1392
    Esmolol hydrochloride
    		Inhibitor 99.69%
    Esmolol hydrochloride is an ultra-short-acting cardioselective β1-adrenergic blocker. Esmolol hydrochloride exerts its antiarrhythmic effect by activating Neurokinin 1 Receptor. Esmolol hydrochloride attenuates post resuscitation myocardial dysfunction. Esmolol hydrochloride improves diabetic wound healing by inhibiting aldose reductase and the production of advanced glycation end products and promoting fibroblast migration. Esmolol hydrochloride can be used to study cardiac diseases such as arrhythmias and diabetic foot ulcers.
    Esmolol hydrochloride
  • HY-108353
    Isoprenaline
    		Agonist 98.93%
    Isoprenaline is a non-selective, orally active β-adrenergic receptor agonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma.
    Isoprenaline
  • HY-14301A
    Olodaterol hydrochloride
    		Agonist 99.70%
    Olodaterol (BI1744) hydrochloride is a selective, long acting β2-adrenoceptor (β2-AR) agonist (EC50=0.1 nM and pKi= 9.14 for human β2-adrenoceptor, respectively). Olodaterol can be used for chronic obstructive pulmonary disease (COPD) and pulmonary fibrosis.
    Olodaterol hydrochloride
  • HY-A0066A
    Tolazoline hydrochloride
    		Antagonist 99.93%
    Tolazoline hydrochloride (Imidaline hydrochloride) is an α-adrenergic receptor antagonist. Tolazoline hydrochloride inhibits Noradrenaline (HY-13715)-induced cell contraction, modulates vascular resistance, increases arterial pressure, and reverses bradycardia and tachypnea. Tolazoline hydrochloride can be used to study erectile dysfunction, α2-adrenergic receptor agonist-related poisoning, and skin vascular disease research.
    Tolazoline hydrochloride
  • HY-14299A
    Indacaterol maleate
    		Agonist 99.82%
    Indacaterol maleate (QAB149) is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol maleate inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol maleate can also be used in cardiovascular disease research.
    Indacaterol maleate
  • HY-B1506A
    Acepromazine maleate
    		Antagonist 99.48%
    Acepromazine (Acetopromazine) maleate is a phenothiazine tranquilizer and is alpha-adrenoceptor antagonist.
    Acepromazine maleate
  • HY-B1154
    Penbutolol sulfate
    		Antagonist 98.89%
    Penbutolol sulfate ((-)-Terbuclomine) is a potent β-adrenoceptor and 5-HT receptor antagonist with Ki of 11.6 nM and 11.9 nM for 5-HT in rat cornu ammonis 1 (CA1) and human CA3.
    Penbutolol sulfate
  • HY-B1396
    Nefazodone hydrochloride
    		Antagonist 99.94%
    Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity.
    Nefazodone hydrochloride
  • HY-123012
    Lubabegron
    		Modulator 98.40%
    Lubabegron is a potent modulator of β-adrenergic receptor (β-AR). Lubabegron demonstrates antagonistic behavior at the β1 and β 2 receptor subtypes and agonistic behavior at the β 3 receptor subtype in cattle. Lubabegron reduces NH3 gas emissions from an animal or its waste. Lubabegron is available as an animal supplement.
    Lubabegron
  • HY-103197
    2-Methoxyidazoxan monohydrochloride
    		Antagonist 98.62%
    2-Methoxyidazoxan monohydrochloride (RX821002 hydrochloride) is a highly selective alpha 2-adrenoceptor antagonist with little or no imidazoline antagonist effect. RX 821002 has markedly higher affinity for (guinea-pig) alpha 2D-adrenoceptors (pKd 9.7) than for (rabbit) alpha 2A-adrenoceptors (pKd 8.2).
    2-Methoxyidazoxan monohydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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