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-148804A
    Vemtoberant mesylate
    		Antagonist
    Vemtoberant (APD418) mesylate is a β3-adrenergic receptor (β3-AR) antagonist with a human Ki of 8.2 nM, and exhibits 400- to 600-fold selectivity over human β1-AR and β2-AR. Vemtoberant mesylate attenuates β3-AR-mediated cardiac inhibition. Vemtoberant mesylate can be used for the research of systolic heart failure.
    Vemtoberant mesylate
  • HY-101514
    β3-AR agonist 1
    		Agonist
    β3-AR agonist 1 (compound 15) is a highly potent, selective, and orally available β3-adrenergic receptor (β3-AR) agonist (EC50=18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold).
    β3-AR agonist 1
  • HY-B0532B
    Trifluoperazine dimaleate
    		Antagonist
    Trifluoperazine dimaleate, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dimaleate is a potent α1-adrenergic receptor antagonist. Trifluoperazine dimaleate is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dimaleate is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dimaleate can be used for the research of schizophrenia. Trifluoperazine dimaleate acts as a reversible inhibitor of influenza virus morphogenesis.
    Trifluoperazine dimaleate
  • HY-165456
    AGN-190851
    		Agonist
    AGN-190851 is a potent and selective agonist of α2-adrenergic receptor (α2 adrenoceptor). AGN-190851 induces dose-dependent water diuresis in rats, and inhibits vasopressin V2 receptor in a species-dependent manner in vitro, thereby suppressing cAMP production. AGN-190851 enhances the contraction of porcine myometrium. AGN 190851 can be used in studies on renal diuretic mechanisms, pharmacology of α2-adrenergic receptor subtypes, and parturition.
    AGN-190851
  • HY-15746B
    Dobutamine tartrate
    		Agonist
    Dobutamine tartrate is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine tartrate is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine tartrate can increase cardiac output and correct hypoperfusion.
    Dobutamine tartrate
  • HY-105124S
    Bufuralol-d9 hydrochloride
    Bufuralol-d9 (hydrochloride) is the deuterium labeled Bufuralol hydrochloride.
    Bufuralol-d<sub>9</sub> hydrochloride
  • HY-116790BS
    (±)-Penbutolol-d9
    (±)-Penbutolol-d9 is the deuterium labeled (±)-Penbutolol.
    (±)-Penbutolol-d<sub>9</sub>
  • HY-A0019S
    Paliperidone-d4
    		Antagonist
    Paliperidone-d4 is the deuterium labeled Paliperidone. Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia.
    Paliperidone-d<sub>4</sub>
  • HY-B0573CS
    (R)-Propranolol-d7
    (R)-Propranolol-d7 is the deuterium labeled (R)-Propranolol.
    (R)-Propranolol-d<sub>7</sub>
  • HY-B1272AS1
    Desipramine-d3
    Desipramine-d3 is the deuterium labeled Desipramine (HY-B1272A). Desipramine is a first-generation tricyclic antidepressant. Desipramine selectively binds to norepinephrine transporter and blocks neuronal norepinephrine reuptake. Desipramine activates MAPK signaling via ERK1/2, JNK, and p38, represses NF-κB and AP-1 activity, and induces apoptosis via ROS elevation, mitochondrial membrane potential reduction, and intracellular calcium increase. Desipramine also shows anyi-inflammatory activity, inhibiting TNF-α production. Desipramine can be used for the research of hepatocellular cancer, inflammation, and neurological diseases.
    Desipramine-d<sub>3</sub>
  • HY-17503S2
    (S)-Metoprolol-d7
    		Inhibitor
    (S)-Metoprolol-d7 is the deuterium labeled Metoprolol. Metoprolol (Toprol) is a selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension[1][2].
    (S)-Metoprolol-d<sub>7</sub>
  • HY-17498AS
    (S)-Atenolol-d7
    (S)-Atenolol-d7 is the deuterium labeled (S)-Atenolol.
    (S)-Atenolol-d<sub>7</sub>
  • HY-B0431AS
    Phenoxybenzamine-d5 hydrochloride
    		Antagonist
    Phenoxybenzamine-d5 (hydrochloride) is the deuterium labeled Phenoxybenzamine hydrochloride. Phenoxybenzamine hydrochloride is a nonselective, irreversible, orally active α-adrenoceptor antagonist that is commonly used for the research of hypertension, specifically caused by pheochromocytoma. Phenoxybenzamine hydrochloride also shows antitumor activity[1][2][3].
    Phenoxybenzamine-d<sub>5</sub> hydrochloride
  • HY-110223
    Atomoxetine-d3 hydrochloride
    		Inhibitor
    Atomoxetine-d3 hydrochloride is the deuterium labeled Atomoxetine hydrochloride. Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5, 77 and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively).
    Atomoxetine-d3 hydrochloride
  • HY-B0192AS
    Alfuzosin-d3 hydrochloride
    		Antagonist 99.15%
    Alfuzosin-d3 hydrochloride is the deuterium labeled Alfuzosin hydrochloride. Alfuzosin hydrochloride is an α1 adrenergic receptor antagonist used to treat benign prostatic hyperplasia (BPH).
    Alfuzosin-d<sub>3<sub> hydrochloride
  • HY-17503S1
    (R)-Metoprolol-d7
    		Inhibitor
    (R)-Metoprolol-d7 is the deuterium labeled Metoprolol. Metoprolol (Toprol) is a selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension[1][2].
    (R)-Metoprolol-d<sub>7</sub>
  • HY-B1110S
    Nomifensine-d3 maleate
    		Inhibitor
    Nomifensine-d3 ((±)-Nomifensine-d3) maleate is the deuterium labeled Nomifensine maleate (HY-B1110A). Nomifensine ((±)-Nomifensine) maleate is a potent norepinephrine (NE) and dopamine (DA) reuptake inhibitor. Nomifensine maleate 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 maleate has antidepressant and analgesic effects. Nomifensine maleate is used in neurodegenerative diseases, compound addiction, and pain research.
    Nomifensine-d<sub>3</sub> maleate
  • HY-18610S
    Diclofensine-d3 (hydrochloride)
    		Inhibitor
    Diclofensine-d3 (Ro-8-4650-d3) hydrochloride is the deuterium labeled Diclofensine hydrochloride. Diclofensine hydrochloride is an orally active neuronal monoamine uptake inhibitor. Diclofensine hydrochloride blocks the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3 and 3.7 nM, respectively. Diclofensine hydrochloride potentiates norepinephrine-induced hypertension and attenuates Tyramine (HY-W007606)-induced hypertension. Diclofensine hydrochloride produces psychostimulant and mood-elevating effects without causing sudden disappearance or withdrawal reactions. Diclofensine hydrochloride can be used in the research of moderate to severe depression.
    Diclofensine-d<sub>3</sub> (hydrochloride)
  • HY-118335S
    Prazobind-d8
    Prazobind-d8 (SZL 49-d8) is the deuterium labeled Prazobind (HY-118335). Prazobind, a prazosin analog, is an irreversible α1-adrenoceptor antagonist. Prazobind competes for alpha 1-adrenoceptor binding sites with a similar potency (IC50 of 1 nM) in tissues enriched in both the alpha 1A (hippocampus) and alpha 1B (liver) subtypes. Prazobind partially inhibits the contractions of circular muscles, longitudinal muscles and smooth muscles of the spleen. Prazobind can be used for the study of blood pressure.
    Prazobind-d<sub>8</sub>
  • HY-12721S
    Clonidine-d4 hydrochloride
    		Agonist
    Clonidine-d4 (hydrochloride) is the deuterium labeled Clonidine. Clonidine hydrochloride is an alpha 2-adrenergic agonist.
    Clonidine-d<sub>4</sub> hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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