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-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-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-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-100490
    Rilmenidine
    		Agonist ≥99.0%
    Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells.
    Rilmenidine
  • HY-B0010D
    Arformoterol tartrate
    		Agonist 99.63%
    Arformoterol ((R,R)-Formoterol) tartrate, the (R,R)-enantiomer of Formoterol, is a long-acting β2-adrenergic receptor (β2-AR) agonist, with a Kd of 2.9 nM. Arformoterol tartrate can be used for the research of chronic obstructive pulmonary disease (COPD).
    Arformoterol tartrate
  • HY-B0162AS
    Ivabradine-d6 hydrochloride
    		Inhibitor
    Ivabradine-d6 (hydrochloride) is the deuterium labeled Ivabradine hydrochloride. Ivabradine hydrochloride is a new If inhibitor with IC50 of 2.9 μM, and used as a pure heart rate lowering agent.
    Ivabradine-d<sub>6</sub> hydrochloride
  • HY-108300
    Oxyfedrine hydrochloride
    		Agonist 99.92%
    Oxyfedrine hydrochloride, a vasodilator, is an orally active β-adrenoreceptor agonist. Oxyfedrine decreases the tonicity of coronary vessels. Oxyfedrine hydrochloride can be used in the research of cardiovascular disease.
    Oxyfedrine hydrochloride
  • HY-15780S
    Brexpiprazole-d8
    		Antagonist ≥99.0%
    Brexpiprazole-d8 (OPC-34712-d8) 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>
  • HY-14539S2
    Clozapine-d4
    		Inhibitor 99.82%
    Clozapine-d4 is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors.
    Clozapine-d<sub>4</sub>
  • HY-100672B
    (2R)-SR59230A
    		Antagonist 99.88%
    (2R)-SR59230A is the isomer of SR59230A (HY-100672), and can be used as an experimental control. SR59230A is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist with IC50s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively.
    (2R)-SR59230A
  • 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-B0556A
    Tetrahydrozoline hydrochloride
    		Agonist 99.88%
    Tetrahydrozoline hydrochloride (Tetryzoline hydrochloride), a derivative of imidazoline, is an α-adrenergic agonist that causes vasoconstriction. Tetrahydrozoline hydrochloride is widely used for the research of nasal congestion and conjunctival congestion.
    Tetrahydrozoline hydrochloride
  • HY-B0371B
    (R)-Terazosin
    		Antagonist 99.76%
    (R)-Terazosin is an active R-enantiomer of Terazosin. (R)-Terazosin is a potent α1-adrenoceptor antagonist with Ki values of 6.51 nM, 1.01 nM and 1.97 nM for α1a, α1b and α1d-adrenoceptor, respectively.
    (R)-Terazosin
  • HY-N1163
    Tetrahydroalstonine
    		Antagonist 99.84%
    Tetrahydroalstonine ((-)-Tetrahydroalstonine) is an indole alkaloid and a selective α₂-adrenergic receptor antagonist. Tetrahydroalstonine exhibits certain neuroprotective effects. Tetrahydroalstonine can regulate autophagy-lysosomal function by activating the Akt/mTOR pathway, significantly reducing OGD/R-induced primary cortical neuronal injury.
    Tetrahydroalstonine
  • HY-50291
    HOKU-81
    		Activator
    HOKU-81 (4-Hydroxytulobuterol) is one of the metabolites of Tulobuterol (HY-B1810). HOKU-81 is a potent and selective β2-adrenoceptor stimulant. HOKU-81 has bronchodilating effect.
    HOKU-81
  • HY-100704
    Procaterol hydrochloride
    		Agonist 99.88%
    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
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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