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-14690
    Ecopipam
    		Antagonist
    Ecopipam (SCH 39166) is a potent, selective and orally active antagonist of dopamine D1/D5 receptor, with Kis of 1.2 nM and 2.0 nM, respectively. Ecopipam shows more than 40-flod selectivity over D2, D4, 5-HT, and α2a receptor (Ki=0.98, 5.52, 0.08, and 0.73 μM, respectively). Ecopipam can be used for the research of schizophrenia and obesity.
    Ecopipam
  • HY-116982
    BMY 7378 free base
    		Antagonist
    BMY 7378 (free base) is a selective antagonist of α1D-adrenoceptor (α1D-AR). BMY 7378 (free base) binds to membranes expressing the cloned rat α1D-AR with a >100-fold higher affinity (Ki=2 nM) than binding to either the cloned rat α1A-AR (Ki=800 nM) or the hamster α1B-AR (Ki=600 nM). BMY 7378 (free base) is a 5-HT1A receptor partial agonist.
    BMY 7378 free base
  • HY-101392R
    Harmane (Standard)
    		Inhibitor
    Harmane (Standard) is the analytical standard of Harmane. This product is intended for research and analytical applications. 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 exhibits comutagenic effect.
    Harmane (Standard)
  • HY-105537
    Ro 70‐0004
    		Antagonist
    Ro 70-0004 (RS-100975) is a selective alpha1A-adrenoceptor antagonist with a pKi of 8.9. Ro 70‐0004 can be used in the study of prostatic hyperplasia.
    Ro 70‐0004
  • HY-111124
    Paroxetine-d2
    Paroxetine-d2 (CTP 347) is a deuterium labeled Paroxetine (HY-122272). Paroxetine is an oral inhibitor that falls under the category of selective serotonin reuptake inhibitors (SSRIs). Paroxetine is also a very weak norepinephrine (NE) reuptake inhibitor, capable of inducing cell apoptosis and having anti-tumor activity. Paroxetine has antidepressant, anti-anxiety, and pain-relieving effects, and it can help improve conditions like obsessive-compulsive disorder, panic disorder, post-traumatic stress disorder, premenstrual anxiety, and chronic headaches.
    Paroxetine-d<sub>2</sub>
  • HY-B0532AR
    Trifluoperazine dihydrochloride (Standard)
    		Antagonist
    Trifluoperazine (dihydrochloride) (Standard) is the analytical standard of Trifluoperazine (dihydrochloride). This product is intended for research and analytical applications. Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis.
    Trifluoperazine dihydrochloride (Standard)
  • HY-14690S
    Ecopipam-d4
    Ecopipam-d4 is deuterium labeled Ecopipam.
    Ecopipam-d<sub>4</sub>
  • HY-17453S
    Salmeterol-d3 xinafoate
    		Agonist
    Salmeterol-d3 (xinafoate) is the deuterium labeled Salmeterol xinafoate. Salmeterol (GR 33343X) xinafoate is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively.
    Salmeterol-d<sub>3</sub> xinafoate
  • HY-119802S
    Practolol-d7
    		Antagonist
    Practolol-d7 is the deuterium labeled Practolol. Practolol is a potent and selective β1-adrenergic receptor antagonist. Practolol can be used for the research of cardiac arrhythmias.
    Practolol-d<sub>7</sub>
  • HY-100704A
    (Rac)-Procaterol hydrochloride
    		Agonist
    (Rac)-Procaterol hydrochloride is a selective, orally active agonist at β2-adrenoceptor. (Rac)-Procaterol hydrochloride is used as a bronchodilator.
    (Rac)-Procaterol hydrochloride
  • HY-B0352S2
    Mirtazapine-d4
    		Antagonist
    Mirtazapine-d4 is deuterium labeled Mirtazapine. Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively.
    Mirtazapine-d<sub>4</sub>
  • HY-B0192S1
    Alfuzosin-13C,d3
    		Antagonist
    Alfuzosin-13C,d3 is the 13C- and deuterium labeled Alfuzosin.
    Alfuzosin-<sup>13</sup>C,d<sub>3</sub>
  • HY-14296
    PF-610355
    		Agonist
    PF-610355 is a long-acting inhaled β2-adrenoreceptor agonist, with an EC50 of 0.26 nM. PF-610355 has the potential for the study of asthma and COPD.
    PF-610355
  • HY-14297
    Milveterol
    Milveterol is a long-acting β(2)-adrenoceptor agonist with high binding activity. Milveterol exhibits high potency in vitro and a prolonged duration of action in a guinea pig bronchoprotection model. Milveterol has been structurally optimized to show enhanced binding potency compared to its parent monomer.
    Milveterol
  • HY-19401
    L-796568
    		Agonist
    L-796568 is a β(3)-adrenergic receptor agonist. L-796568 can be used for the research of obesity.
    L-796568
  • HY-14915
    Bedoradrine
    Bedoradrine is a highly selective β2-adrenergic agonist with activity in suppressing asthma and chronic obstructive pulmonary disease (COPD). Bedoradrine is administered by intravenous infusion and is specifically indicated for the suppression of acute asthma attacks. Bedoradrine has shown good safety and preliminary efficacy in clinical trials, especially in patients with stable moderate to severe asthma. The results of Bedoradrine studies have shown that it can provide clinical benefits without increasing clinical risks, especially for patients who are unable to use inhalation or nebulization suppression.
    Bedoradrine
  • HY-112658
    p-Iodoclonidine hydrochloride
    		Agonist
    p-Iodoclonidine hydrochloride is a partial agonist of α2-adrenergic receptor. p-Iodoclonidine hydrochloride also has minimal agonist activity in inhibiting adenylate cyclase in platelet membranes, and potentiates ADP induced platelet aggregation with an EC50 of 1.5 μM.
    p-Iodoclonidine hydrochloride
  • HY-B0431S
    Phenoxybenzamine-d5
    Phenoxybenzamine-d5 is the deuterium labeled Phenoxybenzamine. Phenoxybenzamine is a nonselective, irreversible, orally active α-adrenoceptor antagonist that is commonly used for the research of hypertension, specifically caused by pheochromocytoma. Phenoxybenzamine also shows antitumor activity.
    Phenoxybenzamine-d<sub>5</sub>
  • HY-117158
    SKF 89748
    		Agonist
    SKF 89748 is an α1-adrenergic receptor agonist with the activity of inhibiting food and water intake. SKF 89748 inhibits food and water intake in adult male rats with an ED50 of 0.37mg/kg for inhibiting food intake.
    SKF 89748
  • HY-101320A
    ZD-7114 hydrochloride
    		Agonist
    ZD-7114 hydrochloride is a potent and selective agonist of β3-adrenergic. ZD-7114 hydrochloride is a selective thermogenic agent in vivo. ZD-7114 hydrochloride can be used in study obesity and diabetes.
    ZD-7114 hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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