1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. Adrenergic Receptor

Adrenergic Receptor

Beta Receptor

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-B0661AR
    Tamsulosin hydrochloride (Standard)
    Antagonist
    Tamsulosin (hydrochloride) (Standard) is the analytical standard of Tamsulosin hydrochloride (HY-B0661A). Tamsulosin hydrochloride ((R)-(-)-YM12617 free base) is an orally active antagonist of α1-adrenergic receptor. Tamsulosin hydrochloride induces Apoptosis. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth and inhibits inflammation in animal models.
    Tamsulosin hydrochloride (Standard)
  • HY-B0391R
    Naftopidil (Standard)
    Antagonist
    Naftopidil (Standard) is the analytical standard of Naftopidil. This product is intended for research and analytical applications. Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia.
    Naftopidil (Standard)
  • HY-10122R
    Silodosin (Standard)
    Antagonist
    Silodosin (Standard) is the analytical standard of Silodosin. This product is intended for research and analytical applications. Silodosin (KAD 3213; KMD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH.
    Silodosin (Standard)
  • HY-B0549AS
    Flavoxate-d4 (hydrochloride)
    Ligand
    Flavoxate-d4 hydrochloride (Rec-7-0040-d4) is the deuterium labeled Flavoxate hydrochloride. Flavoxate hydrochloride (Rec-7-0040; DW61) is an orally active L-type Ca2+ channel inhibitor and antispasmodic. Flavoxate hydrochloride inhibits cyclic adenosine monophosphate production by blocking voltage-dependent inward Ba2+ currents, regulating the brainstem micturition center, and stimulating G protein-coupled receptors. Consequently, Flavoxate hydrochloride induces relaxation of bladder smooth muscle and inhibits isovolumetric rhythmic contractions. Flavoxate hydrochloride effectively increases bladder capacity and alleviates symptoms of urgent urination frequency and pollakiuria caused by overactive bladder. Flavoxate hydrochloride can be used in research on overactive bladder and related voiding dysfunctions.
    Flavoxate-d<sub>4</sub> (hydrochloride)
  • HY-14561AR
    Idazoxan hydrochloride (Standard)
    Antagonist
    Idazoxan (hydrochloride) (Standard) is the analytical standard of Idazoxan (hydrochloride). This product is intended for research and analytical applications. Idazoxan hydrochloride (RX 781094 hydrochloride) is an α2-adrenoceptor antagonist and is also a imidazoline receptors (IRs) antagonist competitively antagonized the centrally induced hypotensive effect of imidazoline-like agents (IMs). Idazoxan hydrochloride also improves motor symptoms in Parkinson’s disease, L-DOPA-induced dyskinesias, and experimental Parkinsonism.
    Idazoxan hydrochloride (Standard)
  • HY-13715S
    (Rac)-Norepinephrine-d3 formate
    Agonist
    (Rac)-Norepinephrine-d3 (formate) is deuterium labeled Norepinephrine. Norepinephrine (Levarterenol; L-Noradrenaline) is a potent adrenergic receptor (AR) agonist. Norepinephrine activates α1, α2, β1 receptors.
    (Rac)-Norepinephrine-d<sub>3</sub> formate
  • HY-32329R
    Setiptiline (Standard)
    Antagonist
    Setiptiline (Standard) is the analytical standard of Setiptiline. This product is intended for research and analytical applications. Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
    Setiptiline (Standard)
  • HY-N1919R
    Ajmalicine (Standard)
    Inhibitor
    Ajmalicine (Standard) is the analytical standard of Ajmalicine. This product is intended for research and analytical applications. Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity.
    Ajmalicine (Standard)
  • HY-101656R
    Medroxalol (Standard)
    Inhibitor
    Medroxalol (Standard) is the analytical standard of Medroxalol (HY-101656). This product is intended for research and analytical applications. Medroxalol (RMI81968) is an orally active adrenergic receptor antagonist, blocks α- and β-adrenergic receptors. Medroxalol shows antihypertensive and vasodilating effects.
    Medroxalol (Standard)
  • HY-19682
    Enciprazine
    Antagonist
    Enciprazine is an orally active non-benzodiazepine anxiolytic. Enciprazine acts as an agonist of 5-HT1A receptor (5-HT1AR) and an antagonist of α1-adrenergic receptor (α1-adrenergic receptor) . Enciprazine induces drug-related electroencephalogram changes by reducing the average power of δ waves and θ waves, and increasing the average power of α waves and fast β waves. Enciprazine exhibits anti-aggressive activity, with only weak sedative and ataxic effects. Enciprazine regulates plasma corticosterone levels and activates the hypothalamic-pituitary-adrenal axis. Enciprazine can be used in research related to anxiety disorders, generalized anxiety syndrome and psychosis.
    Enciprazine
  • HY-122053
    Amidephrine hydrochloride
    Inhibitor
    Amidephrine (hydrochloride) is an adrenergic receptor (AR) agonist. Amidephrine (hydrochloride) can be used in the research of neurological diseases.
    Amidephrine hydrochloride
  • HY-135004
    SU-4029 dihydrochloride
    Antagonist
    Su-4029 is an agent that interacts with alpha receptors. It negates the blockade of norepinephrine by the reversible adrenergic blocker phentolamine but not by the irreversible blocker Dibenamine, suggesting Su-4029 acts at the same site as these blockers. Su-4029 pretreatment results in three categories of responses to pressor phenylalkylamines: irreversible blockade of amines with no or only p-hydroxylation, reversible blockade of amines with beta-carbon hydroxylation, and no blockade or augmentation of amines with m and p-hydroxylation or m or p plus beta-hydroxylation. Su-4029 may deform the alpha receptor site affected by adrenergic blocking agents.
    SU-4029 dihydrochloride
  • HY-17416R
    Guanfacine hydrochloride (Standard)
    Agonist
    Guanfacine (hydrochloride) (Standard) is the analytical standard of Guanfacine (hydrochloride). This product is intended for research and analytical applications. Guanfacine hydrochloride 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 hydrochloride (Standard)
  • HY-B1110R
    Nomifensine (Standard)
    Inhibitor
    Nomifensine (Standard) is the analytical standard of Nomifensine. This product is intended for research and analytical applications. Nomifensine ((±)-Nomifensine) is a potent norepinephrine (NE) and dopamine (DA) reuptake inhibitor. Nomifensine inhibits uptake of NE, DA and 5-HT in rat brain synaptosomes, with IC50 values of 6.6 nM, 48 nM and 830 nM, and Ki values of 4.7 nM, 26 nM and 4000 nM, respectively. Nomifensine has antidepressant and analgesic effects. Nomifensine is used in neurodegenerative diseases, compound addiction, and pain research.
    Nomifensine (Standard)
  • HY-B0371FR
    Terazosin hydrochloride (Standard)
    Antagonist
    Terazosin (hydrochloride) (Standard) is the analytical standard of Terazosin (hydrochloride). This product is intended for research and analytical applications. Terazosin hydrochloride is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin hydrochloride works by relaxing blood vessels and the opening of the bladder. Terazosin hydrochloride has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment.
    Terazosin hydrochloride (Standard)
  • HY-B1573A
    (±)-Butaclamol hydrochloride
    Antagonist
    (±)-Butaclamol hydrochloride (AY-23,028) is the antagonist for adrenergic receptor and dopamine receptor. (±)-Butaclamol hydrochloride antagonizes amphetamine or Apomorphine (HY-12723)-induced stereotyped behaviors and emesis, inhibits discriminative avoidance behavior, and induces catalepsy in rats models.
    (±)-Butaclamol hydrochloride
  • HY-106684
    Ridazolol
    Antagonist
    Ridazolol is a β-adrenergic receptor (βAR) antagonist. Ridazolol exhibits a high degree of selectivity for β-1 adrenergic receptor (β1AR) and possesses moderate intrinsic sympathomimetic activity (ISA). Ridazolol can competitively antagonize the relaxation effects induced by isoproterenol. Ridazolol is utilized in the research of cardiovascular diseases.
    Ridazolol
  • HY-100554R
    BMY 7378 (Standard)
    Antagonist
    BMY 7378 (Standard) is the analytical standard of BMY 7378 (HY-100554). This product is intended for research and analytical applications. BMY 7378 is a selective antagonist of α1D-adrenoceptor (α1D-AR). BMY 7378 binds to membranes expressing the cloned rat α1D-AR with a >100-fold higher affinity (Ki=2 nM) than binding to either the cloned rat α1A-AR (Ki=800 nM) or the hamster α1B-AR (Ki=600 nM). BMY 7378 is a 5-HT1A receptor partial agonist.
    BMY 7378 (Standard)
  • HY-19401A
    L-796568 free base
    Agonist
    L-796568 free base is a β(3)-adrenergic receptor agonist. L-796568 free base can be used for the research of obesity.
    L-796568 free base
  • HY-106554A
    Trimazosin hydrochloride hydrate
    Inhibitor
    Trimazosin hydrochloride hydrate is an orally active, quinazoline derivative which is structurally related to prazosin. Trimazosin shows hypotensive effect by selectively block α1-adrenergic receptor.
    Trimazosin hydrochloride hydrate
Cat. No. Product Name / Synonyms Application Reactivity

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