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-B1231R
    Heptaminol hydrochloride (Standard)
    Heptaminol (hydrochloride) (Standard) is the analytical standard of Heptaminol (hydrochloride). This product is intended for research and analytical applications. Heptaminol (RP-2831) hydrochloride is a vasoconstrictor used in the study of hypotension, especially orthostatic hypotension. Heptaminol is also a skin cancer proliferation inhibitor that inhibits immune inflammation induced by the tumor promoting factor 12-O-tetradecanoylphorbol-13-acetate (TPA) in an NO-dependent manner. Heptaminol also acts as a sympathomimetic amine, exerting indirect sympathetic effects. Heptaminol is also an antagonist of catecholamine release and uptake and can increase intracellular free calcium levels.
    Heptaminol hydrochloride (Standard)
  • HY-B0802AR
    Terbutaline (Standard)
    		Agonist
    Benactyzine hydrochloride (Standard) is the analytical standard of Benactyzine hydrochloride. This product is intended for research and analytical applications. Benactyzine hydrochloride is a competitive BChE inhibitor with a Ki of 0.01 mM. Benactyzine hydrochloride is an anticholinergic drug. Benactyzine hydrochloride has the potential for organophosphate poisoning research.
    Terbutaline (Standard)
  • HY-103109
    Melperone hydrochloride
    		Antagonist
    Melperone hydrochloride is a butyrophenone with atypical antipsychotic properties. Melperone hydrochloride 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 hydrochloride 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 hydrochloride is also a CYP2D6 inhibitor. Melperone hydrochloride can be used for the study of schizophrenia, and agitation in the elderly.
    Melperone hydrochloride
  • HY-106444
    Fipamezole
    		Antagonist
    Fipamezole (MPV 1730; JP-1730) is a potent and orally active α2-adrenergic receptor antagonist with Ki values of 9.2 nM, 17 nM, and 55 nM for human α2A, α2B, and α2C, receptors, respectively. Fipamezole is an anti-dyskinetic agent, and can be used for the study of Parkinson's disease.
    Fipamezole
  • HY-W263279
    (E)-Guanabenz
    		Agonist
    (E)-Guanabenz ((E)-Wy-8678) is an orally active central α2-adrenoceptor agonist. (E)-Guanabenz has antihypertensive activity, acts via stimulating central α2-adrenoceptors, and reducing net sympathetic outflow into the periphery. (E)-Guanabenz also directly binds to and inhibits GADD34, and has neuroprotective activity. (E)-Guanabenz can be used for researching hypertension and Parkinson disease.
    (E)-Guanabenz
  • HY-123008
    Reproterol hydrochloride
    		Agonist
    Reproterol hydrochloride is a dual-acting beta2-adrenoceptor agonist and phosphodiesterase inhibitor. Reproterol hydrochloride is more potent than albuterol and feterol in stimulating cAMP production in human monocytes, demonstrating its potential in enhancing airway function. Furthermore, Reproterol significantly inhibited the production of LTB4, indicating its anti-inflammatory properties. Reproterol hydrochloride may have inhibitory effects in respiratory diseases such as asthma and COPD.
    Reproterol hydrochloride
  • HY-B1111S1
    Amitraz-d3
    		Agonist
    Amitraz-d3 is the deuterium labeled Amitraz. Amitraz is a non-systemic acaricide and insecticide, with alpha-adrenergic agonist activity, interaction with octopamine receptors of the central nervous system and inhibition of monoamine oxidases and prostaglandin synthesis.
    Amitraz-d<sub>3</sub>
  • HY-163694
    ADRA2A antagonist 1
    		Antagonist
    ADRA2A antagonist 1 (compd 4n) is a potent and selective ADRA2A antagonist with an IC50 of 18 nM. ADRA2A antagonist 1 can be used for inflammation and sepsis research.
    ADRA2A antagonist 1
  • HY-B1270R
    Isoxsuprine hydrochloride (Standard)
    		Agonist
    Isoxsuprine hydrochloride (Standard) is the analytical standard of Isoxsuprine hydrochloride. This product is intended for research and analytical applications. Isoxsuprine hydrochloride is a beta-adrenergic receptor agonist with Kis of 13.65 μΜ and 3.48 μΜ for myometrial and placcntal beta-adrenergic receptor, respectively. Isoxsuprine hydrochloride is also a NMDA receptor antagonist.
    Isoxsuprine hydrochloride (Standard)
  • HY-B0006S2
    Carvedilol-d5
    		Inhibitor
    Carvedilol-d5 is deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome.
    Carvedilol-d<sub>5</sub>
  • HY-13458S1
    Droxidopa-13C2,15N hydrochloride
    Droxidopa-13C2,15N (hydrochloride) is deuterium labeled Droxidopa. Droxidopa(L-DOPS), the mixture of Droxidopa (w/w80%) and Pharmaceutical starch (w/w20%), acts as a proagent to the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline); Droxidopa(L-DOPS) is capable of crossing the protective blood-brain barrier.
    Droxidopa-<sup>13</sup>C<sub>2</sub>,<sup>15</sup>N hydrochloride
  • HY-119006
    L-640,033
    		Agonist
    L-640,033 is a potent agonist of β-adrenergic. L-640,033 play an important role in lipid metabolism, and growth.
    L-640,033
  • HY-135895
    Detomidine carboxylic acid
    		Agonist
    Detomidine carboxylic acid is the major urinary metabolite of Detomidine. Detomidine is a synthetic α2-adrenergic agonist. Detomidine also has cardiac and respiratory effects and an antidiuretic action.
    Detomidine carboxylic acid
  • HY-A0007R
    Rotigotine Hydrochloride (Standard)
    		Antagonist
    Rotigotine (Hydrochloride) (Standard) is the analytical standard of Rotigotine (Hydrochloride). This product is intended for research and analytical applications. Rotigotine Hydrochloride (N-0923 Hydrochloride) is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Ki of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
    Rotigotine Hydrochloride (Standard)
  • HY-136693
    L-654284
    L-654284 is an α2-adrenergic receptor antagonist with significant selectivity. L-654284 competes with the binding of 3H-clonidine and 3H-rauwolscine in vitro and shows Ki values of 0.8 nM and 1.1 nM, respectively. L-654284 can block the protrusion effect of clonidine in isolated vas deferens in rats, with a pA2 value of 9.1. L-654284 exhibits remarkable selectivity for α2 and α1 adrenergic receptors, and exhibits a Ki of 110 nM in inhibiting 3H-prazosin binding. L-654284 can significantly increase the turnover rate of norepinephrine in rat cerebral cortex in vivo, showing α2-adrenergic receptor blocking activity in the central nervous system.
    L-654284
  • HY-100255
    Tiodazosin
    		Antagonist
    Tiodazosin is a potent competitive postsynaptic alpha adrenergic receptor antagonist.
    Tiodazosin
  • HY-P1442
    AdTx1
    		Antagonist
    AdTx1 is a selective α1A-adrenoceptor antagonist (Ki: 0.35 nM). AdTx1 can be used for research of benign prostatic hyperplasia.
    AdTx1
  • HY-106769
    Fluparoxan
    		Antagonist 99.66%
    Fluparoxan is an orally active, selective and competitive alpha 2-adrenoceptor antagonist. Fluparoxan is an anti-depressant agent.
    Fluparoxan
  • HY-158194
    α2C adrenoceptor agonist 1
    		Agonist
    α2C adrenoceptor agonist 1 (Compound A) is an orally active, highly selective, and non-central nervous system penetrating agonist for the α2C-adrenoceptor, with EC50 and Ki values of 108 nM and 12 nM, respectively. α2C adrenoceptor agonist 1 can be used in the study of nasal congestion.
    α2C adrenoceptor agonist 1
  • HY-17380R
    (S)-Timolol maleate (Standard)
    		Antagonist
    (S)-Timolol (maleate) (Standard) is the analytical standard of (S)-Timolol (maleate). This product is intended for research and analytical applications. (S)-Timolol Maleate (L-714,465 Maleate) is a non-cardioselective hydrophilic β-adrenoceptor blocker. (S)-Timolol Maleate is widely used as standard medication for intraocular pressure (glaucoma) by preventing the production of aqueous humor. (S)-Timolol Maleate can be used for hypertension, angina pectoris and myocardial infarction.
    (S)-Timolol maleate (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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