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-15780S1
    Brexpiprazole-d8-1
    Brexpiprazole-d8-1 (OPC-34712-d8-1) is the deuterium labeled Brexpiprazole (HY-15780). Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM).
    Brexpiprazole-d<sub>8</sub>-1
  • 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-B0192A
    Alfuzosin hydrochloride
    		Antagonist 99.82%
    Alfuzosin (SL 77499-10) hydrochloride is an orally active, selective and competitive α1-adrenoceptor antagonist. Alfuzosin hydrochloride relaxes the muscles of the prostate and bladder neck, aiding in urination. Alfuzosin hydrochloride can be used in study of benign prostatic hyperplasia (BPH).
    Alfuzosin hydrochloride
  • 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-14903
    Ulimorelin
    		Antagonist
    Ulimorelin (TZP-101) is a ghrelin receptor (GRLN) agonist with an EC50 of 29 nM and a Ki of 16 nM. Ulimorelin is a prokinetic agent and causes vasorelaxation through competitive antagonist action at α1-adrenoceptors. Ulimorelin stimulates intestinal motility and is used for malnutrition.
    Ulimorelin
  • HY-12463
    Carmoterol hydrochloride
    		Agonist 98.73%
    Carmoterol hydrochloride is a highly potent, selective and long-acting β2-adrenoceptor agonist with the pEC50 of 10.19. Carmoterol has 53 times higher affinity for the β2-adrenoceptors than for the β1-adrenoceptors. Carmoterol hydrochloride can be used for the research of asthma and chronic obstructive pulmonary disease (COPD).
    Carmoterol 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-B1696
    Methyldopate
    		Agonist 98.01%
    Methyldopate is an ethyl ester proagent of α-Methyldopa (α-MD; HY-B0225). Methyldopa (L-(-)-α-Methyldopa) is an α-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopate has the potential for severe hypertension research .
    Methyldopate
  • 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
  • HY-B1587
    Carbazochrome
    		99.94%
    Carbazochrome is a capillary stabiliser and used for the research of haemorrhage. Carbazochrome is an antihemorrhagic agent.
    Carbazochrome
  • HY-14690
    Ecopipam
    		Antagonist 99.77%
    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-101656
    Medroxalol
    		Inhibitor 99.85%
    Medroxalol (RMI81968) is an orally active adrenergic receptor antagonist, blocks α- and β-adrenergic receptors. Medroxalol shows antihypertensive and vasodilating effects.
    Medroxalol
  • HY-106612
    Abanoquil
    		Antagonist 98.07%
    Abanoquil (U-K52046), an potent and selective α-1 adrenoceptor antagonist, is an anti-arrhythmic agent. Abanoquil can be used for erectile dysfunction research.
    Abanoquil
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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