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-111326A
    Naphazoline nitrate
    		Agonist ≥98.0%
    Naphazoline (Naphthazoline) nitrate is an α-adrenergic receptor agonist. Naphazoline nitrate reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline nitrate reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF. Naphazoline nitrate can be used for non-bacterial conjunctivitis research.
    Naphazoline nitrate
  • HY-N1919
    Ajmalicine
    		Inhibitor 99.39%
    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
  • HY-105124A
    Bufuralol hydrochloride
    		Antagonist ≥99.0%
    Bufuralol (Ro 3-4787) hydrochloride is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity. Bufuralol hydrochloride is a CYP2D6 probe substrate.
    Bufuralol hydrochloride
  • HY-111191
    ONO-2952
    		99.51%
    ONO-2952 is a potent, selective and orally active translocator protein 18 kDa (TSPO) antagonist with Ki of 0.33-9.30 nM for rat and human TSPO. ONO-2952 is more selective for TSPO than other receptors, transporters, ion channels and enzymes. ONO-2952 exerts its anti-stress effects through inhibition of excessive activation of noradrenergic system in the brain without the amnesic effect. ONO-2952 has the potential for irritable bowel syndrome treatment.
    ONO-2952
  • HY-B1416A
    Efaroxan hydrochloride
    		Antagonist 99.94%
    Efaroxan hydrochloride is a potent, selective and orally active α2-adrenoceptor antagonist, with antidiabetic activity. Efaroxan hydrochloride is a selective I1-Imidazoline receptor antagonist. Efaroxan hydrochloride can be used for the research of cardiovascular disease.
    Efaroxan hydrochloride
  • HY-109075A
    Tasipimidine sulfate
    		Inhibitor 99.46%
    Tasipimidine sulfate is an orally active and selective α2A-adrenoceptor agonist with a pEC50 of 7.57 against human α2A-adrenoceptor. Tasipimidine sulfate can be used for situational anxiety and fear research.
    Tasipimidine sulfate
  • HY-148825
    NP10679
    		Inhibitor 99.42%
    NP10679 is a selective, pH dependent GluN2B subunit-specific N-methyl-D-aspartate (NMDA) receptor inhibitor with high oral bioavailability and good brain penetration. NP10679 inhibits GluN2B with IC50s of 23 and 142 nM at pH 6.9 and 7.6, respectively. NP10679 is a histamine H1 antagonist and a hERG channel inhibitor with IC50s of 73 and 620 nM, respectively. NP10679 is a reversible inhibitor of human liver CYP enzymes.
    NP10679
  • HY-133116
    4-Hydroxyatomoxetine
    4-Hydroxyatomoxetine is an active metabolite of Atomoxetine. 4-Hydroxyatomoxetine is metabolized by the enzyme cytochrome P450 2D6 (CYP2D6). Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5 nM, 77 nM and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively).
    4-Hydroxyatomoxetine
  • HY-B1696
    Methyldopate
    		Agonist 98.01%
    Methyldopate is an ethyl ester proagent of α-Methyldopa (α-MD; HY-B0225). Methyldopa (L-(-)-α-Methyldopa) is an α-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopate has the potential for severe hypertension research .
    Methyldopate
  • HY-13338
    Mabuterol
    		Agonist 99.96%
    Mabuterol is a selective and orally active beta-2 adrenergic receptor (ADRB2) agonist. Mabuterol inhibits the proliferation and suppresses the increase of intracellular Ca2+ induced by PDGF-BB. Mabuterol suppresses the protein expressions of Drp-1, cyclinD1 and PCNA and enhanced the expression of Mfn-2 induced by PDGF-BB.
    Mabuterol
  • HY-101656
    Medroxalol
    		Inhibitor 99.66%
    Medroxalol (RMI81968) is an orally active adrenergic receptor antagonist, blocks α- and β-adrenergic receptors. Medroxalol shows antihypertensive and vasodilating effects.
    Medroxalol
  • HY-101366
    A-61603
    		Agonist ≥99.0%
    A-61603 is a selective α1A-adrenergic receptor agonist. A-61603 increases the frequency of spontaneous Ca2+ transients in rat ventricular myocytes in vitro.
    A-61603
  • HY-14541S
    Olanzapine-d3
    		Antagonist 99.09%
    Olanzapine-d3 is the deuterium labeled Olanzapine. Olanzapine 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 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic[1][2].
    Olanzapine-d<sub>3</sub>
  • HY-100606
    l-Pindolol
    		Agonist 99.89%
    l-Pindolol ((-)-pindolol) is a reversible, competitive and orally active 5-HT1A/1B antagonist. l-Pindolol is a partial β-adrenoceptor agonist. l-Pindolol can be used for the research of neurological disease.
    l-Pindolol
  • HY-12706
    Spiroxatrine
    		Antagonist 99.18%
    Spiroxatrine (R 5188) is a selective, dual antagonist of 5-HT1α and α2-adrenergic, with the Ki values of 3.94, 224000, 118.5 nM for 5-HT1α, 5-HT1β and 5-HT2, respectively. Spiroxatrine (R 5188) has a sedative effect.
    Spiroxatrine
  • HY-B0556A
    Tetrahydrozoline hydrochloride
    		Agonist 99.88%
    Tetrahydrozoline hydrochloride (Tetryzoline hydrochloride), a derivative of imidazoline, is an α-adrenergic agonist that causes vasoconstriction. Tetrahydrozoline hydrochloride is widely used for the research of nasal congestion and conjunctival congestion.
    Tetrahydrozoline hydrochloride
  • HY-N3298
    Meranzin
    		Modulator ≥98.0%
    Meranzin is an absorbed bioactive compound from the Traditional Chinese Medicine (TCM) Chaihu-Shugan-San (CSS). Meranzin, isolated from leaves of Murraya exotica L., regulates the shared alpha 2-adrenoceptor and involves the AMPA-ERK1/2–BDNF signaling pathway. Meranzin has the potential for the prevention of the comorbidity of atherosclerosis and depression.
    Meranzin
  • HY-12716A
    BRL-44408 maleate
    		Antagonist ≥99.0%
    BRL-44408 maleate is an α2A-adrenoceptor antagonist (Ki: 8.5 nM). BRL-44408 maleate has antidepressant and analgesic activity. BRL-44408 also improves cecal ligation puncture (CLP)-induced acute lung injury.
    BRL-44408 maleate
  • HY-B0371D
    (S)-Terazosin
    		Antagonist 99.90%
    (S)-Terazosin is an active S-enantiomer of Terazosin. (S)-Terazosin is a potent and high-affinity α-adrenoceptor antagonist with Ki values of 3.91 nM, 0.79 nM and 1.16 nM for α1a, α1b and α1d-adrenoceptor, respectively. (S)-Terazosin also has high-affinity for α2a, α2B and α2c-adrenoceptor with Ki values of 729 nM, 3.5 nM and 46.4 nM, respectively.
    (S)-Terazosin
  • HY-103207
    Amibegron hydrochloride
    		Agonist ≥99.0%
    Amibegron hydrochloride is a selective β3-adrenoceptor agonist, with an EC50 of 3.5 nM for β-adrenoceptor in rat colon; Amibegron hydrochloride has anxiolytic and antidepressant activity.
    Amibegron hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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