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-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.
    (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.
    Nefazodone-d<sub>6</sub> dihydrochloride
  • HY-N6969A
    Dicentrine hydrochloride
    		Antagonist
    Dicentrine hydrochloride is a drug with anti-inflammatory and anti-cancer activity. Dicentrine hydrochloride exerts its effects by enhancing TNF-α-induced apoptosis in A549 lung adenocarcinoma cells. Dicentrine hydrochloride increases caspase-8, -9, -3 and poly(ADP-ribose) polymerase (PARP) activities. Dicentrine hydrochloride inhibits TNF-α-induced invasion and migration of A549 cells. Dicentrine hydrochloride significantly inhibited the TNF-α-activated TAK1, p38, JNK and Akt signaling pathways, and reduced the transcriptional activities of NF-κB and AP-1.
    Dicentrine hydrochloride
  • HY-W751275
    Ractopamine-13C2
    		Agonist
    Ractopamine-13C2 is the 13C-labeled Ractopamine (HY-113781). Ractopamine (LY031537 free base) is a potent and orally active β-adrenergic receptor (βAR) agonist with Kd value of ~25 nM for pig β1AR and β2AR. Ractopamine also is a mTAAR1 agonist with an EC50 of 16 μM. Ractopamine promotes muscle mass development, limits fat deposition, reduces feed consumption, increases total cellular protein synthesis, and improves growth rate and feed efficiency in finishing swine. Ractopamine can be used for researching to increase lean tissue growth and improve production efficiency in pigs.
    Ractopamine-<sup>13</sup>C<sub>2</sub>
  • 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-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-B0374S1
    Moxonidine-d7
    		Activator
    Moxonidine-d7 is deuterated labeled Moxonidine (HY-B0374). Moxonidine (BDF5895) is an orally active imidazoline type 1 receptor (I1-R) agonist. Moxonidine activates imidazoline I1 receptors and α2 adrenoceptors, affecting oxidized low-density lipoprotein uptake. Moxonidine reduces atherosclerotic lesions and lowers blood pressure. Moxonidine can be used in the study of hypertension, heart failure, and atherosclerosis.
    Moxonidine-d<sub>7</sub>
  • 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-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-129427
    DC-015
    		Antagonist
    DC-015 is a selective and orally active alpha 1-adrenoceptor antagonist on plasma lipid and vascular reactivity in hyperlipidaemic rodent model. DC-015 is a synthesized quinazoline derivative. DC-015 decreases mean arterial pressure in rats. DC-015 has antihypertensive activity.
    DC-015
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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