β2ar

BI-167107 is a high-affinity, full agonist that binds to the β2 adrenergic receptor (β2AR) with a Kd of 84 pM.

Todralazine hydrochloride (Ecarazine hydrochloride) is a β2AR blocker with antioxidant and free radical scavenging properties, making it suitable for anti-hypertensive research.

Todralazine is an anti-hypertensive agent and acts as a β2AR blocker. It also has an antioxidant and free radical scavenging activity.

β2AR/M-receptor agonist-2 is a dual-function compound acting as a muscarinic antagonist and β2 adrenoceptor agonist (MABA). It demonstrates significant activity towards the β2 adrenoceptor with an EC50 of 3.7 nM and exhibits affinity for the human cloned M3 receptor with a Ki of 0.73 nM. This potent bronchodilator holds potential for research in chronic obstructive pulmonary disease (COPD) treatment.

β2AR agonist 2 (compound 8a) is an agonist of the β2-adrenergic receptor (β2AR). It is a saturated azacyclic compound featuring a 4- to 7-membered heterocycle. The compound has a chiral structure in the -R form by incorporating a carbon with a requisite hydroxyl group, which significantly stimulates glucose uptake in skeletal muscle cells, thereby enhancing cellular glucose uptake (GU). β2AR agonist 2 is applicable in the study of type 2 diabetes (T2D).

β2AR agonist 4 (compound A19) is an effective selective agonist for the β2-adrenoceptor (β2-Adrenoceptor), exhibiting an EC50 of 3.7 pM. In a rat model with COPD, β2AR agonist 4 reduces the elevation of inflammatory factors and leukocytes, thereby improving lung function.

Compound 4, known as β2AR ligand 1, serves as a bivalent ligand for the β2-adrenergic receptor (β2AR) at both the orthosteric binding site (OBS) and the metastable binding site (MBS).

β2AR agonist 5 is a selective agonist of β2-adrenergic receptors (β2AR) that increases intracellular cAMP levels by activating Gs-coupled signaling pathways, thereby regulating bronchoconstriction and metabolism-related processes. β2AR agonist 5 can be used to study β2AR-mediated signal transduction and its functional role in respiratory or metabolic regulation.

β2AR/M-receptor agonist-1 (example 131), a muscarinic antagonist and β2 adrenoceptor agonist (MABA), exhibits dual potency towards β2 adrenoceptor and muscarinic receptor, with an EC50 value of 9.2 nM for β2 adrenoceptor and a Ki value of 30.2 nM for the muscarinic receptor, and an EC50 value of 4.0 nM highlighting its MABA activity [1].

Compound 9a (β2AR agonist 3) is a β2-adrenergic receptor (β2AR) agonist used in type 2 diabetes research [1].

β2AR antagonist 1 (Cmpd-15PA) acts as an antagonist to the β2 adrenergic receptor (β2AR). This compound binds to the intracellular surface of β2AR.

α2AR agonist 1 (compound S6a) is a morpholinopyrimidinone that serves as an agonist for the α2-adrenergic receptor (α2AR). This compound elicits a concentration-dependent relaxation in precontracted aortic rings induced by phenylephrine (pEC50=6.81). Additionally, α2AR agonist 1 elevates levels of NOx and NO in HUVEC.

α2AR agonist 2 is a selective antagonist of the α2B adrenergic receptor, with an IC50 of 1.2 µM. It can be utilized for research in inflammatory and neuropathic pain.

5-HT1A modulator 1 is a small molecule modulator, a high-affinity multi-target ligand with potent inhibitory activity against 5-HT1A receptor (IC50=2 nM), α1-adrenergic receptor (IC50=10 nM), and dopamine D2 receptor (IC50=40 nM). This compound is primarily used for research on neuropsychiatric disorders such as anxiety, depression, or schizophrenia.

PF-4348235 HCl (β2AR/M-receptor agonist-2 HCl) is a muscarinic M3 receptor antagonist (Ki: 0.73 nM) and β2 adrenergic receptor agonist (MABA, EC50: 3.7 nM). PF-4348235 HCl is also a bronchial BM213 acetate is a bronchodilator used to study cardiovascular and respiratory diseases such as chronic obstructive pulmonary disease (COPD).

A2AR-agonist-1 (N-(2-(1H-Indol-3-yl)ethyl)adenosine) is a potent A2AR and ENT1 agonist (Ki: 4.39 and 3.47 for A2AR and ENT1. It targets the Adenosine A2A Receptor and Adenosine Transporter for Neuroprotection.

cis-Urocanic acid ((E)-Urocanic acid) is a 5-HT2A receptor agonist (Kd: 4.6 nM). It is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor.

Deramciclane has high affinity for 5-HT2A and 5-HT2C receptors. It acts as an antagonist in both receptor subtypes and has inverse agonist properties for 5-HT2C receptors, but no direct stimulant agonists.

N6-(2-Phenylethyl)adenosine (N6-Phenethyladenosine) is an adenosine derivative and adenosine receptor agonist with Ki values of 11.8 nM for rat A1 receptors and 30.1 nM for human A1 receptors.

Tedatioxetine hydrobromide (Lu AA 24530 hydrobromide) is a serotonin-norepinephrine-dopamine reuptake inhibitor and an antagonist of 5-HT2A, 5-HT2C, 5-HT3, and α1A-adrenergic receptors, which can be used to treat depression and anxiety.

Abaperidone is a potent 5-HT2A receptor and dopamine D2 receptor antagonist with an IC50 of 6.2 for 5-HT2A receptors and 17 nM for dopamine D2 receptors.Abaperidone is a potentially atypical anti-psychotropic compound that reduces basal hsp70 mRNA expression in rat striatum and prefrontal cortex. expression in the striatum and prefrontal cortex of rats.

GS-6201 (CVT-6883) is a selective antagonist of the adenosine A2B receptor, demonstrating high affinity and selectivity with a Ki of 22 nM for human adenosine A2B receptors.

Furaprofen is an orally available, selective and potent HCV inhibitor with anti-inflammatory activity, inhibits carrageenan-induced paw edema in rats and inhibits cotton pellet-induced granulomas in rats at higher doses.

BL-1020 Mesylate (CYP-1020 Mesylate) is an orally available GABA A receptor agonist and D2 antagonist that decreases dopamine activity and enhances GABAA activity.BL-1020 Mesylate has been used in the study of schizophrenia, Alzheimer's disease, and bi-directional cognitive impairment.