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-122215
    Tilisolol hydrochloride
    Tilisolol hydrochloride (N-696) is a non-selective β-adrenergic antagonist with vasodilatory and hypotensive activities. Tilisolol hydrochloride exerts its effects in canine coronary arteries by opening ATP-sensitive K+ channels. Tilisolol hydrochloride exhibits concentration-dependent relaxation in KCl-precontracted rat thoracic aorta. Tilisolol hydrochloride reduces diastolic blood pressure in a dose-dependent manner and slightly increases heart rate in spinal cord stimulated rats.
    Tilisolol hydrochloride
  • HY-139727A
    S(-)-Bisoprolol fumarate
    S(-)-Bisoprolol fumarate is a S(-)-enantiomer of Bisoprolol fumarate. Bisoprolol fumarate is a potent, selective and orally active β1-adrenergic receptor blocker. Bisoprolol has little activity on β2-receptor and has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.
    S(-)-Bisoprolol fumarate
  • HY-G0008
    O-Desmethyl Mebeverine alcohol
    O-Desmethyl Mebeverine alcohol is a metabolite of Mebeverine, which is a potent α1 repector inhibitor, causing relaxation of the gastrointestinal tract.
    O-Desmethyl Mebeverine alcohol
  • HY-126635
    Mafoprazine
    Antagonist
    Mafoprazine is a phenylpiperazine derivative with variable affinities for neuronal receptors. It may exert its antipsychotic effects primarily through D2 receptor blockade and α-adrenergic activity, and may increase the activity of dopamine metabolites.
    Mafoprazine
  • HY-126635
    Mafoprazine
    Agonist
    Mafoprazine is a phenylpiperazine derivative with variable affinities for neuronal receptors. It may exert its antipsychotic effects primarily through D2 receptor blockade and α-adrenergic activity, and may increase the activity of dopamine metabolites.
    Mafoprazine
  • HY-122364
    Bucumolol hydrochloride
    Antagonist
    Bucumolol hydrochloride is a β-adrenergic receptor antagonist that can slow heart rate (negative chronotropic effect) and reduce cardiac contractility (negative inotropic effect). Bucumolol hydrochloride has antiarrhythmic and local anesthetic activity and can be used in the study of cardiovascular diseases.
    Bucumolol hydrochloride
  • HY-B0203BS2
    (Rac)-Nebivolol-d2,15N
    Antagonist
    (Rac)-Nebivolol-d2,15N is 15N and deuterated labeled (Rac)-Nebivolol (HY-B0203B). (Rac)-Nebivolol ((Rac)-R 065824) is a racemic isomer of Nebivolol. Nebivolol is a selective β1-adrenergic receptor antagonist with an IC50 value of 0.8 nM. Nebivolol can prevent up-regulation of Nox2/NADPH oxidase and lipoperoxidation in the early stages of ethanol-induced cardiac toxicity. Vasodilatory activity.
    (Rac)-Nebivolol-d<sub>2</sub>,<sup>15</sup>N
  • HY-W748758
    (Z)-Thiothixene-d8
    (Z)-Thiothixene-d8 (NSC 108165-d8; Navan-d8; Navane-d8) is the deuterium labeled Thiothixene (HY-A0139). Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.
    (Z)-Thiothixene-d<sub>8</sub>
  • HY-B0556B
    Tetrahydrozoline nitrate
    Agonist
    Tetrahydrozoline (Tetryzoline) nitrate , a derivative of imidazoline, is an α-adrenergic agonist that causes vasoconstriction. Tetrahydrozoline is widely used for the research of nasal congestion and conjunctival congestion.
    Tetrahydrozoline nitrate
  • HY-W753523
    Clorprenaline-d7 hydrochloride
    Clorprenaline-d7 hydrochloride is the deuterium labeled Clorprenaline hydrochloride (HY-B1347). Clorprenaline hydrochloride is a β2-adrenergic receptor agonist that is implicated in bronchial expansion. Clorprenaline has the potential for asthma research.
    Clorprenaline-d<sub>7</sub> hydrochloride
  • HY-B0076S
    Bisoprolol-d7 hemifumarate
    Inhibitor
    Bisoprolol-d7 (hemifumarate) is the deuterium labeled Bisoprolol hemifumarate. Bisoprolol hemifumarate is a selective type β1 adrenergic receptor blocker.
    Bisoprolol-d<sub>7</sub> hemifumarate
  • HY-119868
    Butaxamine
    Antagonist
    Butaxamine (Butoxamin) is a potent, selective and orally active β2-adrenoceptor antagonist. Butaxamine shows antiosteoporotic activity.
    Butaxamine
  • HY-B1481B
    Isoetharine hydrochloride
    Agonist
    Isoetharine hydrochloride is selective, short-acting and orally active β-agonist which is widely used as a bronchodilator in the research of inhalation research.
    Isoetharine hydrochloride
  • HY-19225A
    Ensaculin free base
    Antagonist
    Ensaculin free base (KA-672) is a NMDA antagonist and have high affinities to serotonergic 5-HT1A and 5-HT7 receptors, adrenergic α1, and dopaminergic D2 and D3 receptors. Ensaculin free base is a memory-enhancing agent. Ensaculin free base has the potential as an antidementia agent acting on various transmitter systems.
    Ensaculin free base
  • HY-129029R
    Bisoprolol (Standard)
    Inhibitor
    Bisoprolol (Standard) is the analytical standard of Bisoprolol. This product is intended for research and analytical applications. 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 (Standard)
  • HY-B0436R
    Salbutamol hemisulfate (Standard)
    Agonist
    Salbutamol (Albuterol) hemisulfate (Standard) is the analytical standard of Salbutamol hemisulfate (HY-B0436). This product is intended for research and analytical applications. Salbutamol (Albuterol) hemisulfate is an orally active short-acting β2-adrenergic receptor agonist. Salbutamol hemisulfate promotes tumorigenesis in gastric cancer cells through the β2-AR/ERK/EMT pathway. Salbutamol hemisulfate can relax bronchial smooth muscle and is used to study bronchospasm induced by asthma and chronic obstructive pulmonary disease.
    Salbutamol hemisulfate (Standard)
  • HY-120325
    DHMPA
    Inhibitor
    DHMPA is an effective depletor of norepinephrine content of the heart, brain and spleen in mouse and rat. DHMPA has antihypertensive effects.
    DHMPA
  • HY-103202A
    SNAP5089
    SNAP5089 is a selective α1A-adrenoceptor antagonist with over 1700-fold selectivity for the α1A subtype, which may have implications for the treatment of hypertension and benign prostatic hypertrophy. SNAP5089 demonstrates significant receptor affinity compared to other clinical drugs, emphasizing its potential therapeutic advantages. SNAP5089's high affinity aligns with its suitability for conditions where precise α1A modulation is desirable.
    SNAP5089
  • HY-148527
    LAS190792
    Agonist
    LAS190792 (AZD8999) is a potent muscarinic antagonist and β2-adrenoceptor agonist with pIC50 8.9, 8.8, 8.8, 9.2, 8.2, 7.5, 9.1, 5.6 for M1, M2, M3, M4, M5, β1, β2, β3, respectively. LAS190792 can be used as a bronchodilator.
    LAS190792
  • HY-129682
    LY125180
    Inhibitor
    LY125180 is a serotonin uptake inhibitor. LY125180 competitively inhibits the uptake of serotonin and norepinephrine by cortical synaptosomes and of dopamine by striatal synaptosomes, with Ki values of 0.06 μM, 2.2 μM and 2.5 μM respectively.
    LY125180
Cat. No. Product Name / Synonyms Application Reactivity

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