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-113833
    N-Methylindan-2-amine hydrochloride
    		99.94%
    N-Methylindan-2-amine hydrochloride (compound 3b) is an N-alkylated congener of phenylethylamine that increases hot plate reaction time in mice without inducing dopaminergic effects. N-Methylindan-2-amine hydrochloride can be used to study central noradrenergic mechanisms.
    N-Methylindan-2-amine hydrochloride
  • HY-B2169
    Melperone
    		Antagonist 99.84%
    Melperone is a butyrophenone with atypical antipsychotic properties. Melperone is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values ​​of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone is also a CYP2D6 inhibitor. Melperone can be used for the study of schizophrenia, and agitation in the elderly.
    Melperone
  • HY-100704
    Procaterol hydrochloride
    		Agonist 99.99%
    Procaterol hydrochloride is a selective intermediate-acting β2 adrenoreceptor agonist with an EC50 of 12.9 μM. Procaterol hydrochloride can inhibit inflammation both in vivo and in vitro.
    Procaterol hydrochloride
  • HY-W011733
    Tulobuterol hydrochloride
    		Agonist 99.83%
    Tulobuterol hydrochloride (C-78) is a long-acting β2-adrenoceptor agonist, which reduces the frequency of exacerbations of chronic obstructive pulmonary disease and bronchial asthma. Tulobuterol hydrochloride is also a sympathomimetic agent used as a transdermal patch, increases normal diaphragm muscle strength. Tulobuterol hydrochloride inhibit rhinovirus replication and modulate airway inflammation.
    Tulobuterol hydrochloride
  • HY-W795507
    Cyanopindolol
    		Antagonist 99.24%
    Cyanopindolol is an β3-adrenoceptor antagonist. Cyanopindolol is a potent and selective antagonist at the presynaptic serotonin autoreceptor in the rat brain cortex. Cyanopindolol has binding affinity for 5-HT1A and 5-HT1B receptor (Ki: 2.1 and 3 nM respectively).
    Cyanopindolol
  • HY-101355A
    CGP 20712 dihydrochloride
    		Antagonist 99.4%
    CGP 20712 dihydrochloride is a highly selective β1-adrenoceptor antagonist with an IC50 of 0.7 nM. CGP 20712 dihydrochloride exhibits ~10,000-fold selectivity over β2-adrenoceptors.
    CGP 20712 dihydrochloride
  • HY-100699
    Clenproperol
    		Agonist 99.44%
    Clenproperol is a β2-adrenergic agonist.
    Clenproperol
  • HY-B0484
    Buflomedil hydrochloride
    		Antagonist 99.81%
    Buflomedil hydrochloride, a vasodilator agent, is an orally active α1A-adrenoceptor antagonist with Kis of 4.06 µM and 6.84 µM for α1A-AR and α1B-AR, respectively. Buflomedil hydrochloride can be used for the study of peripheral circulatory disorders.
    Buflomedil hydrochloride
  • HY-B1052
    Lofexidine hydrochloride
    		Agonist 99.94%
    Lofexidine (hydrochloride) is a selective α2-receptor agonist, commonly used to alleviate the physical symptoms of heroin and other types of opioid withdrawal.
    Lofexidine hydrochloride
  • HY-14541S
    Olanzapine-d3
    		Antagonist 99.09%
    Olanzapine-d3 is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic.
    Olanzapine-d<sub>3</sub>
  • HY-148804
    Vemtoberant
    		Antagonist 99.08%
    Vemtoberant is an β3 Adrenergic Receptor antagonist. Vemtoberant can be used for research of β3 adrenergic receptor-mediated disorder, such as, heart failure.
    Vemtoberant
  • HY-116790A
    (+)-Penbutolol
    		Antagonist
    (+)-Penbutolol is a β-adrenoceptor antagonist, with an IC50 of 0.74 μM. (+)-Penbutolol is an optical isomer of l-penbutolol with Na+ channel-blocking action.
    (+)-Penbutolol
  • HY-100952
    Nifenalol hydrochloride
    		Antagonist 99.93%
    Nifenalol hydrochloride is a β-adrenergic receptor antagonist. Nifenalol hydrochloride induces the Early Afterdepolarization (EAD) effect. EAD is a phenomenon in cardiac electrophysiology that usually occurs during an action potential in ventricular muscle cells and can lead to arrhythmia. The EAD effect of Nifenalol hydrochloride can be blocked by Tetrodotoxin. Nifenalol hydrochloride is used in the study of conditions such as irregular heartbeat or high blood pressure.
    Nifenalol hydrochloride
  • HY-B1001A
    Todralazine hydrochloride
    		Inhibitor 99.87%
    Todralazine hydrochloride (Ecarazine hydrochloride) is an anti-hypertensive agent, acts as a β2AR blocker, with antioxidant and free radical scavenging activity.
    Todralazine hydrochloride
  • HY-B0573S1
    Propranolol-d7 (ring-d7)
    		Antagonist 99.80%
    Propranolol-d7 (ring-d7) is the deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
    Propranolol-d<sub>7</sub> (ring-d<sub>7</sub>)
  • HY-14541R
    Olanzapine (Standard)
    		Antagonist
    Olanzapine (Standard) is the analytical standard of Olanzapine. This product is intended for research and analytical applications. Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic.
    Olanzapine (Standard)
  • HY-133116
    4-Hydroxyatomoxetine
    4-Hydroxyatomoxetine is an active metabolite of Atomoxetine. 4-Hydroxyatomoxetine is metabolized by the enzyme cytochrome P450 2D6 (CYP2D6). Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5 nM, 77 nM and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively).
    4-Hydroxyatomoxetine
  • HY-13338
    Mabuterol
    		Agonist 99.96%
    Mabuterol is a selective and orally active beta-2 adrenergic receptor (ADRB2) agonist. Mabuterol inhibits the proliferation and suppresses the increase of intracellular Ca2+ induced by PDGF-BB. Mabuterol suppresses the protein expressions of Drp-1, cyclinD1 and PCNA and enhanced the expression of Mfn-2 induced by PDGF-BB.
    Mabuterol
  • HY-A0144
    Etilefrine
    		Agonist
    Etilefrine is a sympathetic nerve agonist and AMPK activator that selectively targets α1/β1 adrenergic receptors. Etilefrine stimulates α1 adrenergic receptors, leading to contraction of vascular smooth muscle and increased peripheral resistance. Etilefrine also stimulates β1 receptors to enhance myocardial contractility and increase heart rate, thereby increasing blood pressure and improving cardiac output. Etilefrine also bidirectionally regulates the AMPK/Akt pathway and modulates the phosphorylation levels. Etilefrine can be used in cardiovascular research, such as postural hypotension, chylothorax, and improving low cardiac output.
    Etilefrine
  • HY-128380
    Dibenamine hydrochloride
    		Antagonist 99.32%
    Dibenamine hydrochloride is a competitive and irreversible adrenergic blocking agent and is known to modify the pharmacological effects of epinephrine. Dibenamine hydrochloride cause a significant increase in the rate of destruction of I-epinephrine in the mouse.
    Dibenamine hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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