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-103216
    RWJ52353
    RWJ52353 is a selective, orally active ligand for α2D adrenoceptor, which binds α2D, α2A, α2B and α1 receptors, with Kis of 1.5, 254, 621 and 443 nM. RWJ52353 exhibits analgesic efficacy in mouse abdominal irritation test (MAIT), with an ED50 of 15.1 mg/kg.
    RWJ52353
  • HY-B1276R
    Metaproterenol hemisulfate (Standard)
    		Agonist
    Metaproterenol (hemisulfate) (Standard) is the analytical standard of Metaproterenol (hemisulfate). This product is intended for research and analytical applications. 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 (Standard)
  • HY-P5846
    Muscarinic toxin 3
    		Antagonist
    Muscarinic toxin 3 (MT3) is a potent and non-competitive mAChR and adrenoceptors antagonist with pIC50s of 6.71, 8.79, 8.86, 7.57, 8.13, 8.49, <6.5, 7.29 against M1, M4, α1A, α1B, α1D,α2A,α2B and α2C receptors, respectively. Muscarinic toxin 3 displays prominent adrenoceptor activity.
    Muscarinic toxin 3
  • HY-15376
    Besipirdine
    		Antagonist
    Besipirdine is a non-receptor-dependent cholinomimetic agent with noradrenergic activity. Besipirdine inhibits voltage-dependent sodium and potassium channels.
    Besipirdine
  • HY-17380S
    (S)-Timolol-d9 maleate
    		Antagonist
    (S)-Timolol-d9 (maleate) is deuterium labeled (S)-Timolol (Maleate). (S)-Timolol Maleate (L-714,465 Maleate) is a non-cardioselective hydrophilic β-adrenoceptor blocker. (S)-Timolol Maleate is widely used as standard medication for intraocular pressure (glaucoma) by preventing the production of aqueous humor. (S)-Timolol Maleate can be used for hypertension, angina pectoris and myocardial infarction[1][2][3].
    (S)-Timolol-d<sub>9</sub> maleate
  • HY-B1396S1
    Nefazodone-d6 dihydrochloride
    		Antagonist
    Nefazodone-d6 (dihydrochloride) is deuterium labeled Nefazodone (hydrochloride). 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[1][2].
    Nefazodone-d<sub>6</sub> dihydrochloride
  • HY-B0391B
    Naftopidil hydrochloride
    		Antagonist
    Naftopidil hydrochloride (KT-611 hydrochloride) 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 hydrochloride has antiproliferative effects. Naftopidil hydrochloride can be used for the research of prostate hyperplasia.
    Naftopidil hydrochloride
  • 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-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-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[1].
    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[1][2][3].
    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[1][2].
    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-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-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[1]. 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[2][3].
    Phenoxybenzamine-d<sub>5</sub>
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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