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-B0194AS
    Tizanidine-d4 hydrochloride
    		Agonist
    Tizanidine-d4 hydrochloride is deuterium labeled Tizanidine hydrochloride (HY-B0194A). Tizanidine hydrochloride, a skeletal muscle relaxant, is an orally effective central α2-adrenoceptor agonist (IC50 = 6.9 nmol). Tizanidine hydrochloride primarily exerts muscle relaxation effects by inhibiting the release of excitatory amino acids (glutamate and aspartate) from the presynaptic terminals of spinal cord interneurons. Tizanidine hydrochloride has anti-injury activity and can inhibit gastrointestinal (GI) transport. Tizanidine hydrochloride can inhibit the proliferation, migration, and invasion of lung cancer cells and induce cell apoptosis by upregulating Nischarin and inhibiting the AKT and Wnt3a/β-catenin signaling pathways. Tizanidine hydrochloride can be used to treat spasticity caused by diseases such as multiple sclerosis (MS), stroke, and spinal cord injury (SCI).
    Tizanidine-d<sub>4</sub> hydrochloride
  • HY-106933A
    Dabelotine methanesulfonate
    		Activator
    Dabelotine (methanesulfonate) is a cognitive enhancer. Dabelotine (methanesulfonate) can be used for Alzheimer disease (AD) research.
    Dabelotine methanesulfonate
  • HY-14539A
    Clozapine hydrochloride
    		Inhibitor
    Clozapine hydrochloride (HF 1854 hydrochloride) is an antipsychotic used for the research of schizophrenia. Clozapine hydrochloride has high affinity for a number of neuroreceptors. Clozapine hydrochloride is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine hydrochloride inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively. Clozapine hydrochloride is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM).
    Clozapine hydrochloride
  • HY-17416AS
    Guanfacine-13C,15N3
    Guanfacine-13C,15N3 is the 13C and 15N labeled Guanfacine. 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>13</sup>C,<sup>15</sup>N<sub>3</sub>
  • HY-A0019BS
    (R)-9-Hydroxy Risperidone-d4
    (R)-9-Hydroxy Risperidone-d4 is the deuterium labeled (R)-9-Hydroxy Risperidone.
    (R)-9-Hydroxy Risperidone-d<sub>4</sub>
  • HY-116379
    RS-100329
    		Antagonist
    RS-100329 is an α1-adrenergic receptor (α1-AR) antagonist that effectively inhibits α1-adrenergic receptor-mediated contractions of lower urinary tract tissues in vitro and in vivo. RS-100329 can be used in the research of symptoms related to benign prostatic hyperplasia.
    RS-100329
  • HY-122272S2
    Paroxetine-d6-1
    		Inhibitor
    Paroxetine-d6-1 is a deuterated labeled Paroxetine. Paroxetine, a phenylpiperidine derivative, is a potent and selective serotonin reuptake inhibitor (SSRI). Paroxetine is a very weak inhibitor of norepinephrine (NE) uptake but it is still more potent at this site than the other SSRIs.
    Paroxetine-d<sub>6</sub>-1
  • HY-W909149
    TAAR1 agonist 3
    		Agonist
    TAAR1 agonist 3 is a trace amine-associated receptor 1 (TAAR1) agonist (pEC50=7.6). TAAR1 agonist 3 is also a full agonist of the α2A receptor (pEC50=6). TAAR1 agonist 3 can be used in the study of neuropsychiatric diseases.
    TAAR1 agonist 3
  • HY-W742256
    N-Nitroso nebivolol (mixture of diastereomers)
    		Control
    N-Nitroso nebivolol (mixture of diastereomers) is a nitrosamine and mutagenic.
    N-Nitroso nebivolol (mixture of diastereomers)
  • HY-121166
    Levobetaxolol
    		Antagonist
    Levobetaxolol is a potent and high affinity β-adrenergic antagonist with IC50 values of 33.2, 2970, 709 nM for guinea pig atrial β1, tracheal β2 and rat colonic β3 receptors, respectively. Levobetaxolol reduces IOP (intraocular pressure). Levobetaxolol exhibits a micromolar affinity for L-type Ca21-channels. Levobetaxolol decreases the effects of ischaemia/reperfusion injury in rats. Levobetaxolol has the potential for the research of glaucoma.
    Levobetaxolol
  • HY-101337A
    Imiloxan hydrochloride
    		Antagonist 98.47%
    Imiloxan hydrochloride is a potent and selective alpha 2B-adrenoceptor antagonist. Imiloxan hydrochloride has the potential for acute kidney injury research.
    Imiloxan hydrochloride
  • HY-B1098A
    Hydroxyamphetamine hydrobromide
    Hydroxyamphetamine (4-Hydroxyamphetamine) hydrobromide is a sympathomimetic agent, stimulates the sympathetic nervous system. Hydroxyamphetamine hydrobromide can be used in eye drops to dilate the pupil.
    Hydroxyamphetamine hydrobromide
  • HY-B0010AS
    Formoterol-d3
    		Agonist
    Formoterol-d3 is deuterium labeled Arformoterol. Arformoterol ((R,R)-Formoterol), the (R,R)-enantiomer of Formoterol, is a long-acting β2-adrenergic receptor (β2-AR) agonist, with a Kd of 2.9 nM. Arformoterol can be used for the research of chronic obstructive pulmonary disease (COPD).
    Formoterol-d<sub>3</sub>
  • HY-B1001
    Todralazine
    		Inhibitor
    Todralazine (Ecarazine) is an anti-hypertensive agent, acts as a β2AR blocker, with antioxidant and free radical scavenging activity.
    Todralazine
  • HY-W742404
    Bopindolol-d9
    Bopindolol-d9 ((±)-Bopindolol-d9) is the deuterium labeled Bopindolol (HY-B1562). Bopindolol ((±)-Bopindolol) is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol is a proagent of Pindolol (HY-B0982). Bopindolol can be used for essential and renovascular hypertension research.
    Bopindolol-d<sub>9</sub>
  • HY-106361
    Flerobuterol
    		Agonist
    Flerobuterol is a beta-adrenoceptor agonist with antidepressant activity. Flerobuterol enhances serotonergic neurotransmission.
    Flerobuterol
  • HY-A0077AS
    Perphenazine-d8 dihydrochloride
    		Inhibitor ≥98.0%
    Perphenazine-d8 (dihydrochloride) is the deuterium labeled Perphenazine, which is a typical antipsychotic agent(5-HT, Dopamine receptor ligand).
    Perphenazine-d<sub>8</sub> dihydrochloride
  • HY-W741706
    Butopamine hydrochloride
    Butopamine hydrochloride is an orally active inotropic compound. Butopamine hydrochloride increases heart rate more than Dobutamine (HY-15746A).
    Butopamine hydrochloride
  • HY-B0452R
    Ritodrine hydrochloride (Standard)
    		Agonist
    Ritodrine (hydrochloride) (Standard) is the analytical standard of Ritodrine (hydrochloride). This product is intended for research and analytical applications. Ritodrine (DU21220) hydrochloride is a potent and orally active β-adrenergic agonist. Ritodrine hydrochloride decreases preterm delivery and uterine contraction. Ritodrine hydrochloride has the potential for the research of preterm labor.
    Ritodrine hydrochloride (Standard)
  • HY-B1392S
    Esmolol-d7 hydrochloride
    		Inhibitor
    Esmolol-d7 hydrochloride is the deuterium labeled Esmolol hydrochloride (HY-B1392). Esmolol hydrochloride is an ultra-short-acting cardioselective β1-adrenergic blocker. Esmolol hydrochloride exerts its antiarrhythmic effect by activating Neurokinin 1 Receptoraldose reductase) and the production of advanced glycation end products and promoting fibroblast migration. Esmolol hydrochloride can be used to study cardiac diseases such as arrhythmias and diabetic foot ulcers.
    Esmolol-d<sub>7</sub> hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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