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-17453S1
    Salmeterol-13C6 xinafoate
    		Agonist
    Salmeterol-13C6 (xinafoate) is the 13C6 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-<sup>13</sup>C<sub>6</sub> xinafoate
  • HY-17416AS1
    Guanfacine-15N13,13C2
    		Agonist
    Guanfacine-15N3,13C2 is 15N and 13C labeled Guanfacine (HY-17416A). Guanfacine is an orally active noradrenergic α2A agonist and has high selective for the α2A receptor subtype. Guanfacine has effects in producing hypotension and sedation. Guanfacine can be used for the research of a variety of prefrontal cortex (PFC) cognitive disorders, including tourette's syndrome and attention deficit hyperactivity disorder (ADHD).
    Guanfacine-<sup>15</sup>N<sup>13</sup>,<sup>13</sup>C<sub>2</sub>
  • HY-B1696A
    Methyldopate hydrochloride
    		Agonist
    Methyldopate hydrochloride is an ethyl ester hydrochloride proagent of α-Methyldopa (α-MD; HY-B0225). Methyldopa (L-(-)-α-Methyldopa) is an α-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopate hydrochloride has the potential for severe hypertension research.
    Methyldopate hydrochloride
  • HY-101435
    Centpropazine
    		Antagonist
    Centpropazine (CNPZ) is a brain-penetrant and non-selective antagonist of serotonin (5-HT1/5-HT2) and adrenergic (α1) receptors. Centpropazine functions by modulating monoamine neurotransmission, particularly reducing serotonin and norepinephrine reuptake, to exert antidepressant effects. Centpropazine is promising for research of depression.
    Centpropazine
  • HY-W153897R
    N-Methyltyramine (Standard)
    		Antagonist
    N-Methyltyramine (Standard) is the analytical standard of N-Methyltyramine. This product is intended for research and analytical applications. N-Methyltyramine is a protoalkaloid that can be isolated from various plant species. N-Methyltyramine is an α2-adrenoreceptor antagonist. N-Methyltyramine enhances appetite and digestion of foods by stimulating gastrin and pancreatic secretions. N-Methyltyramine can relax mouse small intestinal smooth muscle and inhibits small intestinal propulsion.
    N-Methyltyramine (Standard)
  • HY-117046A
    AVN-101 hydrochloride
    		Inhibitor 99.59%
    AVN-101 hydrochloride is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56  nM, and 1.17  nM, respectively). AVN-101 hydrochloride also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 hydrochloride can be studied in such diseases as general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis.
    AVN-101 hydrochloride
  • HY-100141
    Ancarolol
    		Inhibitor
    Ancarolol is a beta-adrenergic blocking agent.
    Ancarolol
  • HY-13788B
    LY 344864 hydrochloride
    		Agonist
    LY 344864 hydrochloride is a selective, orally active 5-HT1F receptor agonist with a Ki of 6 nM. LY 344864 hydrochloride is a full agonist producing an effect similar in magnitude to serotonin itself. LY 344864 hydrochloride can cross the blood brain barrier to some extent.
    LY 344864 hydrochloride
  • HY-15394S
    (Rac)-Rotigotine-d7 hydrochloride
    		Antagonist
    (Rac)-Rotigotine-d7 (hydrochloride) is deuterium labeled (Rac)-Rotigotine (hydrochloride). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
    (Rac)-Rotigotine-d<sub>7</sub> hydrochloride
  • HY-121588
    IMTPPE
    		Inhibitor
    IMTPPE is an inhibitor of the androgen receptor (AR) in C4-2 prostate cancer cells, inhibiting its transcriptional activity and protein levels. IMTPPE inhibited the proliferation of AR-positive prostate cancer cells but had no effect on AR-negative prostate cancer cells. IMTPPE also inhibited the growth of enzalutamide-resistant 22Rv1 xenograft tumors.
    IMTPPE
  • HY-122300C
    Oxaprotiline hydrochloride
    		Inhibitor
    Oxaprotiline hydrochloride is a potent norepinephrine (NA) uptake inhibitor. Oxaprotiline hydrochloride has antidepressant activity.
    Oxaprotiline hydrochloride
  • HY-157796
    β2AR agonist 4
    		Agonist
    β2AR agonist 4 (compound A19) is a potent and selective β2-Adrenoceptor agonist with an EC50 of 3.7 pM. β2AR agonist 4 suppresses the inflammatory cytokines and leukocytes upregulation and improves lung function in COPD rat model.
    β2AR agonist 4
  • HY-167698
    Dibenamine
    		Antagonist
    Dibenamine is an alpha-adrenergic antagonist that exhibits the ability to block both basal and histamine-stimulated gastric acid secretion, making it therapeutically relevant in conditions involving excessive gastric acid production.
    Dibenamine
  • HY-101345
    AH 11110A
    		Antagonist
    AH 11110A is an α1B-adrenoceptor antagonist, but it can't effectively distinguish between the different subtypes of alpha(1) adrenoceptors (A, B, and D), nor can it clearly differentiate between alpha(1) and alpha(2) adrenoceptors.
    AH 11110A
  • HY-14539S3
    Clozapine-d3
    		Inhibitor
    Clozapine-d3 (HF 1854-d3) is deuterium labeled Clozapine. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM).
    Clozapine-d<sub>3</sub>
  • HY-W707407
    Bisoprolol-d7
    		Inhibitor
    Bisoprolol-d7 is deuterium labeled Bisoprolol. Bisoprolol is a potent, selective and orally active β1-adrenergic receptor blocker with little activity on β2-receptor. Bisoprolol has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.
    Bisoprolol-d<sub>7</sub>
  • HY-176060
    Platelet aggregation-IN-3
    		Ligand
    Platelet aggregation-IN-3 (Compound 5) is a ligand for H2 histamine receptors, α2(A,C)-adrenergic receptors (α2-AR), and 5-HT2(B,C) serotonin receptors. Platelet aggregation-IN-3 can inhibit platelet aggregation induced by ADP and collagen and can also modulate tumour cell-induced platelet aggregation (TCIPA). Platelet aggregation-IN-3 is promising for research of antiplatelet therapy in cardiovascular diseases and the prevention of cancer-related thrombosis and tumour metastasis.
    Platelet aggregation-IN-3
  • HY-119485
    Dilevalol
    		Agonist
    Dilevalol ((+)-Labetalol) is a novel agonist of ß2-receptor that can be used to suppress hypertension during pregnancy.
    Dilevalol
  • HY-14302S1
    Salmeterol-d5
    		Agonist
    Salmeterol-d5 is a deuterated labeled Salmeterol. Salmeterol (GR33343X) 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>5</sub>
  • HY-112071A
    Prenalterol hydrochloride
    		Agonist
    Prenalterol hydrochloride is a partial adrenal agonist with functional β1-receptor specificity and positive inotropic effects. Prenalterol hydrochloride is effective in suppressing acute heart failure, low output syndrome after myocardial infarction, shock, and reducing orthostatic hypotension in Shy-Drager syndrome.
    Prenalterol hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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