Adrenergic Receptor

Bometolol Hydrochloride is a beta-adrenergic blocking compound used for the treatment of cardiovascular disease.

Ersentilide, a benzamide derivative, functions as both a β1-adrenergic receptor antagonist and an Ikr blocker. It has demonstrated efficacy in animal models of cardiac arrhythmias.

Aclidinium, a dual-action compound, serves as a long-acting muscarinic antagonist and a β2-adrenoceptor (β2-AR) agonist, exhibiting bronchodilator properties. It effectively reduces lung hyperinflation, enhances lung function, and prolongs exercise endurance time. This compound is commonly utilized in studies focusing on chronic obstructive pulmonary disease (COPD).

<p>Metrazoline (o-Methyl-tracizoline) acts as a ligand for adrenergic receptors (low affinity) and imidazoline I2 receptors.</p>

L-654284 is an α2-adrenergic receptor antagonist characterized by its notable selectivity. It competes with 3H-clonidine and 3H-rauwolscine for binding in vitro, exhibiting Ki values of 0.8 nM and 1.1 nM, respectively. L-654284 effectively blocks the pre-ejaculatory effects of clonidine in isolated rat vas deferens, with a pA2 value of 9.1. The compound demonstrates significant selectivity for α2 over α1 adrenergic receptors, with a Ki value of 110 nM against 3H-prazosin binding. In vivo, L-654284 significantly increases the turnover of norepinephrine in the rat cerebral cortex, indicating its activity in blocking α2-adrenergic receptors within the central nervous system.

(Rac)-Nebivolol, a racemic β1-adrenergic blocker (IC50=0.8 nM), has vasodilatory properties and mitigates ethanol-induced cardiac harm.

LK-11, an alkaloid derivative, inhibits the passive uptake of norepinephrine (NA) by synaptic vesicles in the thalamus, similarly to cocaine.

Mafoprazine, a phenylpiperazine derivative, exhibits varying affinities for neuronal receptors, primarily exerting its antipsychotic effects through blocking D2 receptors and enhancing α-adrenergic activity. It also increases the activity of dopamine metabolites.

RU 52583 is an alpha 2-adrenergic receptor antagonist.

Vibegron (MK-4618) is an effective and selective Beta 3 adrenergic receptor agonist, used to treat overactive bladder (OAB).

SAR-150640, a selective β3-adrenergic receptor agonist, prevents an increase in MMP activity and production observed after LPS stimulation or in cases of chorioamnionitis.

PF-9404C: S-S diastereoisomer, beta-blocker with vasodilation, boosts cyclic GMP in rat aorta cells from 3 to 53 pmol/mg protein.

Carazolol (BM 51052) hydrochloride is a potent antagonist of β1/β2-adrenoceptors and also serves as a powerful and selective agonist of β3-adrenoceptors. It is utilized in research focusing on hypertension.

Anti-MRSA agent 19 (Compound 1) is an antibiotic that exhibits activity against Staphylococcus aureus. It is active against 40 clinical isolates from the CDC, representing diverse bacterial species with various resistance factors, including resistance to vancomycin, aminoglycoside/tetracycline, and oxazolidinone (median MIC=4 μg/mL).

AA 497, a beta-2 agonist, causes relaxation and suppresses Ca spike frequency.

2,3-MDMA hydrochloride is an inhibitor of the noradrenalin transporter and serotonin transporter, with IC50 values of 6.2 μM and 82 μM, respectively.

Meluadrine, a potent agonist of the β2 adrenergic receptor, is one of the metabolites of Tulobuterol [1].

DCB-3503, a tylophorine analog, may treat cancer and suppress immunity by blocking protein synthesis and modulating HSC70's ATPase activity.

TAAR1 agonist 3 is a potent agonist of Trace Amine-Associated Receptor 1 (TAAR1) with a pEC50 value of 7.6. Additionally, it acts as a full agonist at the α2AR with a pEC50 of 6. TAAR1 agonist 3 is utilized in the research of neuropsychiatric disorders.

(S)-Bucindolol is an enantiomer of bucindolol, specifically a β1-adrenergic receptor antagonist. It is primarily utilized in research related to heart failure.

HOKU-81is a new bronchodilator and is one of the metabolites of tulobuterol.

<p>Picumeterol(GR 114297A) is a potent and selective β2 adrenergic receptor agonist. In vitro and in vivo trials, Picumeterol produced long-lasting airway smooth muscle relaxation. Picumeterol is a pure R enantiomer that can be used to improve lung function and reduce airway hyperreactivity in patients with asthma.</p>

1-(2,4-Dichlorophenyl)-2-(1H-imidazol-1-yl)ethanol is a useful organic compound for research related to life sciences. The catalog number is T65156 and the CAS number is 24155-42-8.

SKF 89748 is an agonists of alpha 1-adrenoceptor.

4-Hydroxyatomoxetine, an active metabolite of Atomoxetine, is metabolized by CYP2D6. Atomoxetine is a noradrenaline reuptake inhibitor.

4-Hydroxypropranolol hydrochloride is an active metabolite of Propranolol, with a potency comparable to Propranolol. It inhibits β1- and β2-adrenergic receptors (pA2s: 8.24 and 8.26).

N-methyl-2-AI (hydrochloride) is a useful organic compound for research related to life sciences. The catalog number is T66396 and the CAS number is 10408-85-2.

SB251023 is an agonist of β3-adrenoceptor.