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-12987S1
    Pimozide-d5 N-Oxide
    		Antagonist
    Pimozide-d5 N-Oxide is the deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5[1][2].
    Pimozide-d<sub>5</sub> N-Oxide
  • HY-U00399A
    Fiduxosin hydrochloride
    		Antagonist
    Fiduxosin hydrochloride (ABT 980) is a potent α1-adrenoceptor antagonist, with Ki of 0.160 nM, 24.9 nM, and 0.920 nM for α1a-, α1b-, and α1d-adrenoceptors, respectively.
    Fiduxosin hydrochloride
  • HY-122272S
    Paroxetine-d4
    		Inhibitor
    Paroxetine-d4 (BRL29060-d4) is deuterium labeled Paroxetine. Paroxetine is an oral inhibitor that falls under the category of selective serotonin reuptake inhibitors (SSRIs). Paroxetine is also a very weak norepinephrine (NE) reuptake inhibitor, capable of inducing cell apoptosis and having anti-tumor activity. Paroxetine has antidepressant, anti-anxiety, and pain-relieving effects, and it can help improve conditions like obsessive-compulsive disorder, panic disorder, post-traumatic stress disorder, premenstrual anxiety, and chronic headaches.
    Paroxetine-d<sub>4</sub>
  • HY-14541A
    Olanzapine hydrochloride
    		Antagonist
    Olanzapine hydrochloride 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 hydrochloride is an atypical antipsychotic.
    Olanzapine hydrochloride
  • HY-132184S
    5,6-Epoxyeicosatrienoic acid-d11
    5,6-Epoxyeicosatrienoic acid-d11 (5,6-EET-d11) is deuterium labeled 5,6-Epoxyeicosatrienoic acid. 5,6-Epoxyeicosatrienoic acid (5,6-EET; (±)5,6-EpETrE) is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5,6-Epoxyeicosatrienoic acid degrades into 5,6-DiHET and 5,6-δ-lactone, which can be converted to 5,6-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5,6-Epoxyeicosatrienoic acid has been implicated in the mobilization of calcium and hormone secretion. 5,6-Epoxyeicosatrienoic acid is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50=0.54 μM), and Cav3. and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2, as measured by oxygen consumption and product formation assays when used at a concentration of 50 μM. (±)5,6-Epoxyeicosatrienoic acid is provided as a mixture of the free acid and lactone.
    5,6-Epoxyeicosatrienoic acid-d<sub>11</sub>
  • HY-116957
    Bunitrolol hydrochloride
    		Antagonist
    Bunitrolol hydrochloride is an orally active β-adrenergic blocker that has a high affinity for β-adrenergic receptors. Bunitrolol hydrochloride exerts significant β-receptor antagonist activity and has weak α1-blocking activity. Bunitrolol hydrochloride is mainly used in the study of cardiovascular diseases such as hypertension and angina pectoris, and is also used in placental transport research.
    Bunitrolol hydrochloride
  • HY-10122A
    (Rac)-Silodosin
    		Inhibitor
    (Rac)-Silodosin ((Rac)-KAD 3213) is the racemate of Silodosin (HY-10122). Silodosin is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker.
    (Rac)-Silodosin
  • HY-123059
    (Rac)-ICI-118551 hydrochloride
    		Antagonist
    (Rac)-ICI-118551 hydrochloride is a selective β2-adrenergic receptor antagonist. (Rac)-ICI-118551 hydrochloride can inhibit dendrite ramification of hippocampal neurons in a mouse model of Alzheimer's disease.
    (Rac)-ICI-118551 hydrochloride
  • HY-122212
    PF-9404C
    		Inhibitor
    PF-9404C is a potent beta-adrenergic blocker and a vasorelaxing agent. PF-9404C can be used as NO-donor. PF-9404C shows antihypertensive and cardioprotective action.
    PF-9404C
  • HY-124910
    BU-E-75
    		Antagonist
    BU-E-75 is a guanidine-type H2 receptor agonist that exhibits antagonism at postsynaptic α-adrenoceptors, which can relax the noradrenaline-precontracted vessels.
    BU-E-75
  • HY-W726390
    2-(4-(2-Hydroxy-3-(isopropyl(nitroso)amino)propoxy)phenyl)acetamide
    2-(4-(2-Hydroxy-3-(isopropyl(nitroso)amino)propoxy)phenyl)acetamide is a genotoxic derivative of Atenolol (HY-17498) that can induce DNA fragmentation in rat hepatocytes when used at concentrations ranging from 0.1 to 1 mM.
    2-(4-(2-Hydroxy-3-(isopropyl(nitroso)amino)propoxy)phenyl)acetamide
  • HY-B0528
    Octopamine
    		Agonist
    Octopamine is a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates. Octopamine can stimulate alpha2-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha2-ARs. Octopamine increased glycogenolysis, glycolysis, oxygen uptake, gluconeogenesis and the portal perfusion pressure.
    Octopamine
  • HY-12707B
    Piribedil maleate
    		Antagonist
    Piribedil maleate is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil maleate is also a α2-adrenoceptors antagonist. Piribedil maleate can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil maleate has the potential for the research of parkinson's disease, circulatory disorders, cancers.
    Piribedil maleate
  • HY-108247
    Guanethidine sesquisulfate
    Guanethidine sesquisulfate, an antihypertensive agent, is an adrenergic neurone blocking agent. Guanethidine sesquisulfate enters noradrenergic nerve terminals by the neuronal amine carrier.
    Guanethidine sesquisulfate
  • HY-B0659R
    Brimonidine (Standard)
    		Agonist
    Brimonidine (Standard) is the analytical standard of Brimonidine. This product is intended for research and analytical applications. Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist.
    Brimonidine (Standard)
  • HY-10121R
    Asenapine (Standard)
    		Inhibitor
    Asenapine (Standard) is the analytical standard of Asenapine. This product is intended for research and analytical applications. Asenapine (Org 5222), an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine can be used in the research of schizophrenia and bipolar disorder.
    Asenapine (Standard)
  • HY-13575R
    Blonanserin (Standard)
    		Antagonist
    Blonanserin (Standard) is the analytical standard of Blonanserin. This product is intended for research and analytical applications. Blonanserin (AD-5423) is a potent and orally active 5-HT2A (Ki=0.812 nM) and dopamine D2 receptor (Ki =0.142 nM) antagonist. Blonanserin is usually acts as an atypical antipsychotic agent and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension.
    Blonanserin (Standard)
  • HY-101434A
    Cetamolol hydrochloride
    		Inhibitor
    Cetamolol hydrochloride is classified as a potent β1-blocker with intrinsic sympathomimetic activity and cardioselectivity. Low and medium doses of Cetamolol and Atenolol produce a more prolonged inhibitory effect than the same doses of Propranolol and Dexpropranolol.
    Cetamolol hydrochloride
  • HY-12961AR
    Bretylium (tosylate) (Standard)
    Bretylium (tosylate) (Standard) is the analytical standard of Bretylium (tosylate). This product is intended for research and analytical applications. 0
    Bretylium (tosylate) (Standard)
  • HY-B2169R
    Melperone (Standard)
    		Antagonist
    Melperone (Standard) is the analytical standard of Melperone (HY-B2169). This product is intended for research and analytical applications. 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 (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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