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-100850
    Piperoxan hydrochloride
    		Antagonist 99.66%
    Piperoxan (Benodaine) hydrochloride is an α2 adrenoceptor antagonist. Piperoxan hydrochloride is the first-generation antihistamine.
    Piperoxan hydrochloride
  • HY-14541R
    Olanzapine (Standard)
    		Antagonist
    Olanzapine (Standard) is the analytical standard of Olanzapine. This product is intended for research and analytical applications. Olanzapine (LY170053) 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 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic.
    Olanzapine (Standard)
  • HY-100634
    4-Hydroxypropranolol hydrochloride
    		Antagonist
    4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol. 4-Hydroxypropranolol hydrochlorid is of comparable potency to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties.
    4-Hydroxypropranolol hydrochloride
  • HY-148529
    Midaglizole
    		Antagonist 98.28%
    Midaglizole ((±)-DG5128 free base, DG5128 free base) is a potent α2-adrenoceptor antagonist. Midaglizole is a hypoglycemic agent. Midaglizole increases blood pressure and reduces blood glucose levels in vivo.
    Midaglizole
  • HY-B0528AS
    Octopamine-d4 hydrochloride
    		Agonist 98.28%
    Octopamine-d4 (hydrochloride) is the deuterium labeled Octopamine hydrochloride. Octopamine ((±)-p-Octopamine) hydrochloride, a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates. Octopamine hydrochloride can stimulate alpha2-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha2-ARs. Octopamine hydrochloride increased glycogenolysis, glycolysis, oxygen uptake, gluconeogenesis and the portal perfusion pressure.
    Octopamine-d<sub>4</sub> hydrochloride
  • HY-103212A
    Azepexole hydrochloride
    		Agonist
    Azepexole hydrochloride (B-HT 933 dihydrochloride; Oxazoloazepin dihydrochloride) is a selective agonist for α 2-adrenoceptor, with pKi of 8.3, 7.6, and 7.5 for α2A-, α2B- and α2C-adrenoceptor subtypes, resepctively. Azepexole dihydrochloride causes concentration-dependent inhibition of peristaltic contractions with IC50 of 78.72 nM. Azepexole hydrochloride exhibits antitussive and analgesic efficacy.
    Azepexole hydrochloride
  • HY-128515
    Metaterol
    		Agonist
    Metaterol is a beta-adrenergic receptor agonist.
    Metaterol
  • HY-12987S
    Pimozide-d4
    		Antagonist 99.2%
    Pimozide-d4 is a deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
    Pimozide-d<sub>4</sub>
  • 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-B0471S1
    Phenylephrine-2,4,6-d3 hydrochloride
    		Agonist 99.90%
    Phenylephrine-2,4,6-d3 (hydrochloride) is the deuterium labeled Phenylephrine hydrochloride. (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
    Phenylephrine-2,4,6-d<sub>3</sub> hydrochloride
  • HY-B0716S1
    Urapidil-d3
    		Antagonist 99.93%
    Urapidil-d3 is the deuterium labeled Urapidil. Urapidil is an α1 adrenoreceptor antagonist and a 5-HT1A receptor agonist.
    Urapidil-d<sub>3</sub>
  • HY-106720
    Amosulalol
    		Inhibitor 98.69%
    Amosulalol (YM 09538) is an orally active and dual inhibitor of α1/β1-Adrenergic Receptor. Amosulalol exhibits antihypertensive activity via α1-Adrenergic Receptor inhibition. Amosulalol decreases reflexogenic increases in heart rate and plasma renin activity (PRA) via β1-Adrenergic Receptor inhibition in spontaneously hypertensive rats (SHR).
    Amosulalol
  • HY-B1251
    Guanethidine
    Guanethidine sulphate was synthesized in 1959. Guanethidine is thought to lowing blood pressure by interfering with the metabolism of chemical transmitter substances in post-ganglionic sympathetic nerve fibres.
    Guanethidine
  • HY-12715S
    Yohimbine-13C,d3
    		Antagonist ≥99.0%
    Yohimbine-13C,d3 is the 13C- and deuterium labeled Yohimbine. Yohimbine is a potent and relatively nonselective alpha 2-adrenergic receptor (AR) antagonist, with IC50 of 0.6 μM.
    Yohimbine-<sup>13</sup>C,d<sub>3</sub>
  • HY-B0193AS
    Prazosin-d8 hydrochloride
    		Antagonist 99.78%
    Prazosin-d8 hydrochloride is the deuterium labeled Prazosin hydrochloride. Prazosin hydrochloride is an alpha-adrenergic blocker.
    Prazosin-d<sub>8</sub> hydrochloride
  • HY-12707S
    Piribedil-d8
    		Antagonist 99.79%
    Piribedil-d8 is the deuterium labeled Piribedil, which is an antiparkinsonian agent.
    Piribedil-d<sub>8</sub>
  • HY-153091
    BMY 14802
    		Agonist 98.96%
    BMY 14802 is a sigma-1 receptor (σ1R) antagonist, as well as an agonist at serotonin (5-HT) 1A and adrenergic alpha-1 receptors. BMY 14802 inhibits abnormal involuntary movement (AIM) in rat Parkinson's disease (PD) model, with down-regulating the expression of AIM.
    BMY 14802
  • HY-111013
    VK-II-86
    		Antagonist
    VK-II-86 is a Carvedilol (HY-B0006) analogue lacking antagonist activity at β-adrenoceptors, in hypokalaemia. VK-II-86 prevents hypokalaemia-induced ventricular arrhythmia through multi-channel effects. VK-II-86 prevents all hypokalaemia-induced changes in ion channel activity and oxidative stress.
    VK-II-86
  • HY-133116S
    4-Hydroxyatomoxetine-d3
    		98.89%
    4-Hydroxyatomoxetine-d3 is a deuterium labeled 4-Hydroxyatomoxetine. 4-Hydroxyatomoxetine is an active metabolite of Atomoxetine (Tomoxetine). 4-Hydroxyatomoxetine is metabolized by the enzyme cytochrome P450 2D6 (CYP2D6). Atomoxetine is a potent and selective noradrenal in re-uptake inhibitor.
    4-Hydroxyatomoxetine-d<sub>3</sub>
  • HY-147100
    α1A-AR Degrader 9c
    		Inhibitor
    α1A-AR Degrader 9c (compound 9c) is a potent, selective and reversible α1A-AR (Adrenergic receptor) PROTAC degrader, with a DC50 of 2.86 μM. α1A-AR Degrader 9c induces α1A-AR degradation can be attributed to proteasomal degradation. α1A-AR Degrader 9c inhibits the proliferation of PC-3 cells, with an IC50 of 6.12 μM. α1A-AR Degrader 9c shows antitumor activity, and can be used for prostate cancer research.
    α1A-AR Degrader 9c
Cat. No. Product Name / Synonyms Application Reactivity
Adrenergic Receptor Isoform Comparison

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