2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. Adrenergic Receptor
  5. Adrenergic Receptor Inhibitor

Adrenergic Receptor Inhibitor

Adrenergic Receptor Isoform Comparison

Adrenergic Receptor Inhibitors (207):

Cat. No. Product Name Effect Purity
  • HY-101392
    Harmane
    		Inhibitor 99.91%
    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 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).
  • HY-B0381
    Betaxolol
    		Inhibitor 99.82%
    Betaxolol is a selective beta1 adrenergic receptor blocker that can be used for the research of hypertension and glaucoma.
  • HY-B0702
    Nicergoline
    		Inhibitor 99.06%
    Nicergoline, an ergoline derivative ester of bromonicotinic acid, is a potent, selective and orally active antagonist of α1A-adrenoceptor. Nicergoline has vasodilator effects. Nicergoline also has ameliorative effects on cognitive function in mouse models of Alzheimer's disease.
  • HY-16736A
    Centanafadine hydrochloride
    		Inhibitor 99.93%
    Centanafadine (hydrochloride) is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively.
  • HY-10121
    Asenapine
    		Inhibitor 99.62%
    Asenapine (Org 5222), an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine can be used in the research of schizophrenia and bipolar disorder.
  • HY-B0381A
    Betaxolol hydrochloride
    		Inhibitor 99.30%
    Betaxolol Hydrochloride is a selective beta1 adrenergic receptor blocker that can be used for the research of hypertension and glaucoma.
  • HY-12717A
    Phentolamine hydrochloride
    		Inhibitor 99.87%
    Phentolamine hydrochloride is an orally active adrenergic α receptor-blocking agent.
  • HY-B1392
    Esmolol hydrochloride
    		Inhibitor 99.92%
    Esmolol hydrochloride is a beta adrenergic receptor blocker.
  • HY-B1110A
    Nomifensine maleate
    		Inhibitor 98.79%
    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 shows low or ineffective binding activity to dopamine D2, α1-adrenergic, 5-HT2, and muscarinic receptors. Nomifensine maleate has antidepressive effects.
  • HY-100490A
    Rilmenidine hemifumarate
    		Inhibitor 99.82%
    Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an alpha 2-adrenoceptor agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine hemifumarate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
  • 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.
  • HY-12390
    Lofepramine
    		Inhibitor ≥99.0%
    Lofepramine (Lopramine) is a modified tricyclic and orally active antidepressant. Lofepramine inhibits the uptake of Noradrenaline (NA) (HY-13715) and 5-hydroxytryptamine (5-HT) with IC50s of 2.7 μM and 11 μM, respectively. Lofepramine exerts its antidepressant activity by promoting noradrenergic neurotransmission. Lofepramine also enhances serotonergic neurotransmission by inhibiting neuronal uptake of 5-HT and tryptophan pyrrolase. Lofepramine exhibits significant anxiolytic properties. .
  • HY-B0006B
    (S)-Carvedilol
    		Inhibitor 99.64%
    (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).
  • 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.
  • HY-P1376A
    G-Protein antagonist peptide TFA
    		Inhibitor 98.91%
    G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis.
  • HY-129029
    Bisoprolol
    		Inhibitor 99.78%
    Bisoprolol is a potent, selective and orally active β1-adrenergic receptor blocker with little activity on β2-receptor. Bisoprolol has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.
  • HY-120170
    BMS-466442
    		Inhibitor 98.99%
    BMS-466442 is a potent and selective inhibitor of asc-1 (alanine serine cysteine transporter-1), with an IC50 of 11 nM. BMS-466442 inhibits [3H] D-serine uptake into rat brain synaptosomes, with an IC50 of 400 nM. BMS-466442 can be used for schizophrenia research.
  • HY-W376701
    Guanadrel
    		Inhibitor ≥98.0%
    Guanadrel is an orally active postganglionic adrenergic inhibitor of spiroketal. Guanadre can be used in anti-hypertensive studies.
  • HY-14539R
    Clozapine (Standard)
    		Inhibitor 99.98%
    Clozapine (Standard) is the analytical standard of Clozapine. This product is intended for research and analytical applications. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM).
  • HY-B0006A
    Carvedilol phosphate hemihydrate
    		Inhibitor 99.94%
    Carvedilol phosphate hemihydrate (BM 14190 phosphate hemihydrate) is a non-selective β/α-1 blocker. Carvedilol phosphate hemihydrate inhibits lipid peroxidation with an IC50 of 5 μM. Carvedilol phosphate hemihydrate is a multiple action antihypertensive agent with potential use in angina and congestive heart failure. Carvedilol phosphate hemihydrate is an autophagy inducer that inhibits the NLRP3 inflammasome.