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-126635R
    Mafoprazine (Standard)
    		Antagonist
    Mafoprazine (Standard) is the analytical standard of Mafoprazine. This product is intended for research and analytical applications. 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 (Standard)
  • HY-13458A
    Droxidopa hydrochloride
    Droxidopa (L-DOPS) hydrochloride is a potent, orally active norepinephrine precursor. Droxidopa hydrochloride increases standing blood pressure, ameliorates symptoms of orthostatic hypotension and improves standing ability. Droxidopa hydrochloride has the potential for the research of neurogenic orthostatic hypotension (nOH) and alternative ADHD (attention deficit hyperactivity disorder).
    Droxidopa hydrochloride
  • HY-148526
    β2AR/M3-receptor agonist-1
    		Agonist
    β2AR/M3-receptor agonist-1 (example 9) is a potent β2AR and M3 receptor agonist. β2AR/M3-receptor agonist-1 shows M3 receptor affinity with a pIC50 value of 9.3. β2AR/M3-receptor agonist-1 has the potential for the research of respiratory tract disorders.
    β2AR/M3-receptor agonist-1
  • HY-100935R
    Cimaterol (Standard)
    		Agonist
    Cimaterol (Standard) is the analytical standard of Cimaterol. This product is intended for research and analytical applications. Cimaterol (CL 263780) is a β-adrenergic agonist on energy metabolism in ob/ob mice. The Kd for Cimaterol binding to the L6 β-receptor is 26 nM which is compatible with its EC50 for the stimulation of protein synthesis (approx 5 nM).
    Cimaterol (Standard)
  • HY-136935
    Alloyohimbine
    		Antagonist
    Alloyohimbine, an alkaloid, is a selective α2-adrenoceptor antagonist with K Dα1, K Dα2 of 0.28 μM and 0.006 μM, respectively.
    Alloyohimbine
  • HY-122221
    KUM 32
    		Inhibitor
    KUM 32 is a potent antagonist of epinephrine-induced platelet aggregation. KUM 32 is an adenylate cyclase activity inhibitor. KUM 32 binds to the alpha 2 adrenergic receptor of human platelets.
    KUM 32
  • HY-100490S
    Rilmenidine-d4
    		Agonist
    Rilmenidine-d4 is the deuterium labeled Rilmenidine. Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells.
    Rilmenidine-d<sub>4</sub>
  • HY-119795
    Zometapine
    Zometapine (CI-781) is a pyrazolodiazepine derivative. Zometapine can be used in antidepressant research.
    Zometapine
  • HY-107327S
    Carazolol-d7
    		≥99.0%
    Carazolol-d7 is the deuterium labeled Carazolol (HY-107327). Carazolol is a highly potent antagonist of β1/β2 adrenoceptor. Carazolol is also a potent, selective β3-adrenoceptor agonist. Carazolol can be used in the research of hypertension.
    Carazolol-d<sub>7</sub>
  • HY-123322
    PF-184298
    PF-184298 is a dual serotonin/noradrenaline reuptake inhibitor with IC50 of 6 nM and 21 nM, respectively.
    PF-184298
  • HY-121783
    BE2254
    		Antagonist
    BE2254 is a compound with antipyretic and metabolic activity, which has the activity of regulating the febrile response and metabolism. BE2254 can reduce the metabolic and febrile activity induced by lipopolysaccharide in febrile rabbits, suggesting that it may regulate body temperature by acting on the α1-adrenergic receptor mechanism.
    BE2254
  • HY-116790B
    (±)-Penbutolol
    		Antagonist
    (±)-Penbutolol ((Rac)-Penbutolol) is the racemic mixture of Penbutolol. (±)-Penbutolol is an orally active β-adrenergic receptor antagonist. (±)-Penbutolol antagonizes exercise-induced tachycardia, reduces the increase in peak expiratory flow rate (PEFR) caused by exercise, and decreases resting plasma renin activity (PRA). (±)-Penbutolol reaches peak plasma concentration 1 hour after oral administration, with a half-life of 4.5 hours, and is converted into an active metabolite in the body. (±)-Penbutolol can be used in cardiovascular-related disease research.
    (±)-Penbutolol
  • HY-103216
    RWJ52353
    RWJ52353 is a selective, orally active ligand for α2D adrenoceptor, which binds α2D, α2A, α2B and α1 receptors, with Kis of 1.5, 254, 621 and 443 nM. RWJ52353 exhibits analgesic efficacy in mouse abdominal irritation test (MAIT), with an ED50 of 15.1 mg/kg.
    RWJ52353
  • HY-107010A
    Esprolol hydrochloride
    		Antagonist
    Esprolol hydrochloride is an orally active and potent β-adrenergic receptor antagonist. Esprolol hydrochloride undergoes rapid metabolism by blood and tissue esterases to form an active metabolite, amoxolol. Esprolol hydrochloride is promising for research of exertional angina.
    Esprolol hydrochloride
  • HY-P5846
    Muscarinic toxin 3
    		Antagonist
    Muscarinic toxin 3 (MT3) is a potent and non-competitive mAChR and adrenoceptors antagonist with pIC50s of 6.71, 8.79, 8.86, 7.57, 8.13, 8.49, <6.5, 7.29 against M1, M4, α1A, α1B, α1D,α2A,α2B and α2C receptors, respectively. Muscarinic toxin 3 displays prominent adrenoceptor activity.
    Muscarinic toxin 3
  • HY-15376
    Besipirdine
    		Antagonist
    Besipirdine is a non-receptor-dependent cholinomimetic agent with noradrenergic activity. Besipirdine inhibits voltage-dependent sodium and potassium channels.
    Besipirdine
  • HY-17380S
    (S)-Timolol-d9 maleate
    		Antagonist
    (S)-Timolol-d9 (maleate) is deuterium labeled (S)-Timolol (Maleate). (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-d<sub>9</sub> maleate
  • HY-B1396S1
    Nefazodone-d6 dihydrochloride
    		Antagonist
    Nefazodone-d6 (dihydrochloride) is deuterium labeled Nefazodone (hydrochloride). Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity.
    Nefazodone-d<sub>6</sub> dihydrochloride
  • HY-N6969A
    Dicentrine hydrochloride
    		Antagonist
    Dicentrine hydrochloride is a drug with anti-inflammatory and anti-cancer activity. Dicentrine hydrochloride exerts its effects by enhancing TNF-α-induced apoptosis in A549 lung adenocarcinoma cells. Dicentrine hydrochloride increases caspase-8, -9, -3 and poly(ADP-ribose) polymerase (PARP) activities. Dicentrine hydrochloride inhibits TNF-α-induced invasion and migration of A549 cells. Dicentrine hydrochloride significantly inhibited the TNF-α-activated TAK1, p38, JNK and Akt signaling pathways, and reduced the transcriptional activities of NF-κB and AP-1.
    Dicentrine hydrochloride
  • HY-B0391B
    Naftopidil hydrochloride
    		Antagonist
    Naftopidil hydrochloride (KT-611 hydrochloride) 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 hydrochloride has antiproliferative effects. Naftopidil hydrochloride can be used for the research of prostate hyperplasia.
    Naftopidil hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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