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-W009027
    Indoramin hydrochloride
    Indoramin (hydrochloride) is a new hypotensive agent. Indoramin (hydrochloride) is also selective for the α1A-adrenoceptor.
    Indoramin hydrochloride
  • HY-W722221
    Colterol acetate
    Antagonist
    Colterol acetate is a selective inhibitor of β-adrenergic receptors. Colterol acetate can relax tracheal smooth muscle (primarily acting on β2 receptors), reduce subspastic contractions of tricholoma (acting on β2), and increase contractility of left ventricular papillary muscles (acting on β1).
    Colterol acetate
  • HY-136960
    β2AR antagonist 1
    Antagonist
    β2AR antagonist 1 (Cmpd-15PA) is an antagonist of β2 adrenergic receptor (β2AR). β2AR antagonist 1 binds to the intracellular surface of the β2AR.
    β2AR antagonist 1
  • HY-106518
    Adimolol free base
    Antagonist
    Adimolol (free base) (MEN 935 (free base)) is an antagonist of β- and α-adrenolytic receptor. Adimolol (free base) shows Kis of 5.2 x 10-7, 1.3 x 10-5 mol/L at α1 and α2 drenoceptors, respectively. Adimolol (free base) can be used for antihypertensive study.
    Adimolol free base
  • HY-176333
    Nebivolol O-β-D-glucuronide
    Antagonist
    Nebivolol O-β-D-glucuronide is a derivative of Nebivolol (HY-B0203). Nebivolol is an orally active beta receptor blocker and has the high beta(1)-receptor affinity. Nebivolol has direct vasodilator properties and adrenergic blocking characteristics. Nebivolol can be used for the research of kinds of diseases such as hypertension, coronary artery disease, congestive heart failure and ischemic heart disease.
    Nebivolol O-β-D-glucuronide
  • HY-A0252A
    Bupranolol hydrochloride
    Bupranolol hydrochloride is a non-selective β-adrenergic blocker with potent membrane stabilizing activity. Bupranolol hydrochloride is able to significantly modulate the contractile activity of the non-pregnant human uterus. Bupranolol hydrochloride showed significant effects on spontaneous uterine contractions in an in vitro study in patients with ovarian cancer. Bupranolol hydrochloride is similar in potency to propranolol, another β-adrenergic blocker. Bupranolol hydrochloride is rapidly and completely absorbed in vivo, and its major metabolite is carboxybupranolol.
    Bupranolol hydrochloride
  • HY-162659
    β2AR ligand 1
    β2AR ligand 1 (Compound 4) is a homobivalent bitopic ligand for β2 adrenergic receptor (β2AR) on the orthosteric binding site (OBS) and the metastable binding sites (MBS).
    β2AR ligand 1
  • HY-157502S
    Buctopamine-d9
    Agonist
    Buctopamine-d9 is the deuterium labeled Buctopamine. Buctopamine is a β2 adrenoceptor agonist.
    Buctopamine-d<sub>9</sub>
  • HY-W777360
    Harman-13C2,15N
    Inhibitor
    Harman-13C2,15N is 13C and 15N labeled Harmane. Harmane is a benzodiazepine receptor inhibitor (IC50=7 μM), with IC50 values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane also inhibits haloperidol and serotonin, with IC50 values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC50=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).
    Harman-<sup>13</sup>C<sub>2</sub>,<sup>15</sup>N
  • HY-106523
    Nipradolol
    Inhibitor
    Nipradolol (KT-210; K-351) is a potent blocker of alpha-1-adrenergic receptors. Nipradolol inhibits the increase of intraocular pressure (IOP) in an albino rabbit model induced by Phenylephrine (HY-B0769). Nipradolo suppresses the noradrenaline (NA)-induced muscles contraction, also exhibits vasodilator activity on the dog coronary artery.
    Nipradolol
  • HY-100935S
    Cimaterol-d7
    Agonist
    Cimaterol-d7 is the deuterium labeled Cimaterol. Cimaterol is a potent agonist of β-adrenergic receptors (pEC50s=8.13, 8.78, and 6.62 for human β1, β2, and β3, respectively). Cimaterol has been used in farmed animals to increase carcass mass and to alter muscle and fat deposition.
    Cimaterol-d<sub>7</sub>
  • HY-W777156
    Carazolol-d6 hydrochloride
    Carazolol-d6 (hydrochloride) is deuterium labeled Carazolol hydrochloride (HY-W517264). Carazolol hydrochloride is a highly potent antagonist of β12 adrenoceptor. Carazolol hydrochloride is also a potent, selective β3-adrenoceptor agonist. Carazolol hydrochloride can be used in the research of hypertension.
    Carazolol-d<sub>6</sub> hydrochloride
  • HY-B0006BS
    (S)-Carvedilol-d4
    Inhibitor
    (S)-Carvedilol-d4 is deuterium labeled (S)-Carvedilol. (S)-Carvedilol, the S-enantiomer of Carvedilol, is a non-selective β/α-1 blocker. (S)-Carvedilol exerts protection against the vascular or cardiac toxicity of Doxorubicin (DOX).
    (S)-Carvedilol-d<sub>4</sub>
  • HY-108901R
    Formoterol hemifumarate hydrate (Standard)
    Agonist
    Formoterol (hemifumarate hydrate) (Standard) is the analytical standard of Formoterol (hemifumarate hydrate). This product is intended for research and analytical applications. Formoterol hemifumarate hydrate is a selective, long-acting beta 2-adrenoceptor agonist. Formoterol is a bronchodilator used for the research of the asthma and chronic obstructive pulmonary disease (COPD). Formoterol hemifumarate hydrate induces mitochondrial biogenesis and promotes cognitive recovery after traumatic brain injury.
    Formoterol hemifumarate hydrate (Standard)
  • HY-P1582
    ACTH (1-14)
    Activator
    ACTH (1-14) is a fragment of adrenocorticotrophin, which regulates cortisol and androgen production.
    ACTH (1-14)
  • HY-U00237B
    L-771688 hydrochloride
    Antagonist
    L-771688 hydrochloride is a potent and highly selective α1A-adrenoceptor antagonist (Kd=43-90 pM). L-771688 hydrochloride is effective against cloned human, rat and dog α1A-adrenergic receptors. L-771688 exhibits high affinity (Ki ≤ 1 nM) and over 500-fold selectivity over the α1B and α1D isoforms. L-771688 potently antagonizes norepinephrine-induced responses at these receptors. Inhibits contractions induced by phenylephrine or A-61603 in rat, dog, human and monkey models.
    L-771688 hydrochloride
  • HY-13715BR
    Norepinephrine bitartrate monohydrate (Standard)
    Agonist
    Norepinephrine (bitartrate monohydrate) (Standard) is the analytical standard of Norepinephrine (bitartrate monohydrate). This product is intended for research and analytical applications. Norepinephrine (Levarterenol; L-Noradrenaline) bitartrate monohydrate is a potent adrenergic receptor (AR) agonist. Norepinephrine activates α1, α2, β1 receptors.
    Norepinephrine bitartrate monohydrate (Standard)
  • HY-12707A
    Piribedil dihydrochloride
    Antagonist
    Piribedil dihydrochloride is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil dihydrochloride is also a α2-adrenoceptors antagonist. Piribedil dihydrochloride can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil dihydrochloride has the potential for the research of parkinson's disease, circulatory disorders, cancers.
    Piribedil dihydrochloride
  • HY-119873
    Celiprolol
    Antagonist
    Celiprolol (REV 5320) is a potent, cardioselective and orally active β1-andrenoceptor r antagonist with partial β2 agonist activity, with Ki values of 0.14-8.3 μM. Celiprolol has antihypertensive and antianginal activity, and can be used for the research of cardiovascular disease such as high blood pressure.
    Celiprolol
  • HY-B2195
    Aldioxa
    Antagonist
    Aidioxa has the ability to improve delayed gastric emptying in rats. It can partially improve delayed gastric emptying caused by clonidine or restraint stress. The allyltoin part of Aidioxa restores gastric emptying activity by antagonizing α-2 adrenergic receptors. Its aluminum hydroxide part is involved in restoring gastric compliance. Aidioxa can improve both delayed gastric emptying and impaired gastric compliance, both of which play an important role in functional dyspepsia (FD). Aidioxa is a candidate agent for inhibiting FD.
    Aldioxa
Cat. No. Product Name / Synonyms Application Reactivity

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