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-W702712
    3-Hydroxy xylazine
    		Control
    3-Hydroxy xylazine is a metabolite of the α2-adrenergic receptor agonist Xylazine.
    3-Hydroxy xylazine
  • HY-101393A
    CGP 12177 hydrochloride
    		Modulator 99.69%
    CGP 12177 ((±)-CGP 12177) hydrochloride is a β Adrenergic Receptor Ligand. CGP 12177 hydrochloride is a high affinity antagonist of β1- and β2-AR. CGP 12177 hydrochloride is also shown to interact, with a lower affinity, with the β3-AR and to exhibit a partial agonist activity on rodent and human β3-AR. CGP 12177 hydrochloride exhibits partial agonist properties for α1-AR in rat pulmonary artery.
    CGP 12177 hydrochloride
  • HY-135026
    DL-Norepinephrine tartrate
    		Modulator
    DL-Norepinephrine tartrate is a neurotransmitter, which targets adrenergic receptors, and causes large-amplitude sleep-like electrical activity in the neocortex and suppresses electroencephalography (EEG) activity in the hippocampus. DL-Norepinephrine tartrate results in head shake, difficulty walking, and frequent posture changes in rats model.
    DL-Norepinephrine tartrate
  • 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-162677
    MT-1207
    		Antagonist 99.96%
    MT-1207 is an orally active and selective adrenergic α1 and 5-HT2A receptor antagonist. MT-1207 shows IC50<0.1 nM, 0.15 nM, 1.40 nM and 0.27 nM for α1A, α1B, α1D and 5-HT2A, respectively. MT-1207 achieves an effective blood pressure (BP) reduction in the 2K2C rat model without damaging renal function. MT-1207 is a potent multitarget inhibitor with the potential for vasodilatation research.
    MT-1207
  • HY-137447A
    Pirepemat fumarate
    		Antagonist 98.26%
    Pirepemat (IRL752) fumarate is a corticalpreferring catecholamine- and cognition-promoting agent. Pirepemat fumarate is used for the study of Parkinson's disease.
    Pirepemat fumarate
  • HY-114814
    ORM-10921 free base
    		Antagonist 98.08%
    ORM-10921 free base is a selective α-2C adrenergic receptor antagonist with a Ki of 1.4 nM. ORM-10921 free base displays potent antidepressant and antipsychotic-like effects.
    ORM-10921 free base
  • HY-B0573BS
    Propranolol-d7
    		Antagonist ≥99.0%
    Propranolol-d7 is the deuterium labeled Propranolol. Propranolol 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 inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
    Propranolol-d<sub>7</sub>
  • HY-100490B
    Rilmenidine phosphate
    		Agonist ≥98.0%
    Rilmenidine phosphate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate is an alpha 2-adrenoceptor agonist. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
    Rilmenidine phosphate
  • HY-P3557
    Mibenratide
    		Antagonist 99.77%
    Mibenratide, a small cyclic peptide, is an adrenergic β1 receptor antagonist. Mibenratide can be used for heart failure research.
    Mibenratide
  • HY-171978A
    LM-189 free base
    		Agonist 99.45%
    LM-189 free base, a G protein alpha subunit I (Gαi)-biased agonist, is a Gαi-biased ligand of β2-adrenergic receptor (β2AR). LM-189 free base stabilizes a distinct conformation in TM6 and increases the dynamics of ICL2. LM-189 free base can be used to develop the Gαi-biased β2AR agonists.
    LM-189 free base
  • 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-155879
    (±)-N-Methylcoclaurine
    		Antagonist ≥98.0%
    (±)-N-Methylcoclaurine is a selective α2-adrenoceptor antagonist.
    (±)-N-Methylcoclaurine
  • HY-136474
    Amidephrine
    		Agonist
    Amidephrine is a selective agonist of alpha 1-adrenoceptor. Amidephrine inhibits inhibits monopulse field contraction of the vas deferens epithelium and prostate gland.
    Amidephrine
  • HY-B1615S
    Clenbuterol-d9
    		Agonist 99.86%
    Clenbuterol-d9 is the deuterium labeled Clenbuterol. Clenbuterol (NAB-365) is a β2-adrenergic receptor agonist with an EC50 of 31.9 nM.
    Clenbuterol-d<sub>9</sub>
  • HY-A0275
    Amezinium methylsulfate
    		Activator 99.72%
    Amezinium metilsulfate has multiple mechanisms, including stimulation of alpha and beta-1 receptors and inhibition ofnoradrenaline and tyramine uptake.
    Amezinium methylsulfate
  • HY-B1506
    Acepromazine
    		Antagonist
    Acepromazine (Acetopromazine) is a phenothiazine tranquilizeran and alpha-adrenoceptor antagonist.
    Acepromazine
  • HY-B1037S
    Salbutamol-d3
    		Agonist 98.59%
    Salbutamol-d3 (Albuterol-d3) is the deuterium labeled Salbutamol (HY-B1037). Salbutamol (Albuterol) is an orally active short-acting β2-adrenergic receptor agonist. Salbutamol promotes tumorigenesis in gastric cancer cells through the β2-AR/ERK/EMT pathway. Salbutamol can relax bronchial smooth muscle and is used to study bronchospasm induced by asthma and chronic obstructive pulmonary disease.
    Salbutamol-d<sub>3</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-B0573S
    Propranolol-d7 hydrochloride
    		Antagonist 98.47%
    Propranolol-d7 (hydrochloride) is a 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 the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
    Propranolol-d<sub>7</sub> hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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