at 2 receptor

AT2 receptorligand-1 (compound 14) is a potent ligand for the angiotensin AT2 receptor, with a Ki value of 4.9 nM. It exhibits high stability in microsomes containing sulfonamide ligands.

A2B receptor antagonist 1 (EXAMPLE 9B) is a potent A2B adenosine receptor antagonist.

Sigma-1 receptor antagonist 2 is a more potent and selective antagonist of the sigma-1 receptor (σ1 R, Ki = 3.88 nM) compared to the sigma-2 receptor (Ki = 1288 nM).

AMPA receptor modulator-2 (Example 134) is an AMPA receptor modulator with a pIC50 of 10.1 for TARPγ2 dependent AMPA receptor[1]. pIC50 = -lgIC50. [1]. BERRY CYNTHIA G B (US), et al. AZABENZIMIDAZOLES AND THEIR USE AS AMPA RECEPTOR MODULATORS. Patent. WO2016176460.

A2A receptor antagonist 1 (CPI-444 analog) is an inhibitor of the adenosine A2A receptor and A1 receptor with Ki values of 4 nM and 264 nM, respectively.

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.

A2B receptor antagonist 2 hydrochloride is an antagonist of adenosine receptor A2B (Ki = 2.30 μM for rA1, 6.8 μM for rA2A, 3.44 μM for hA2B).

GABA receptor antagonist 2 (Compound IId) is a GABA receptor blocker with an LC50 of 0.0735 μg/mL against Plutella xylostella (P. xylostella). This compound exhibits significant insecticidal activity against P. xylostella and its resistant strains, as well as against Spodoptera frugiperda and Chilo suppressalis. GABA receptor antagonist 2 can bind to the GABA receptor at the Drosophila RdlG335 site and is useful for managing resistant pest populations.

CCK-B Receptor Antagonist 2 is a potent and orally active antagonist of Gastrin/CCK-B (IC50: 0.43 nM). It also inhibits gastrin/CCK-A activity (IC50: 1.82 μM).

GLP-1 receptor agonist 2 is a glucagon-like peptide-1 receptor (GLP-1R) agonist.

Glucagon receptor antagonist -2 is a highly effective glucagon receptor antagonist.

Sigma-2 receptor antagonist 1 is an antagonist of the sigma-2 (σ-2) receptor.

CB1/2 receptor-1 (compound 5.3) serves as an agonist for CB1/2 receptors and is utilized in angiogenesis research.

P2X7 receptor antagonist-5 (compound 13a) is a potent, orally active, and long-lasting antagonist of the P2X7 receptor.

5-HT2A receptor agonist-6 (compound 47) is a selective agonist of the 5-HT2A receptor with a pEC50 value of 6.58.

CB2 receptor agonist 9 (Compound 33) is an orally active agonist of cannabinoid receptor 2 (CB2 receptor) with an EC50 of 16.2 nM. It inhibits the expression of TNF-α, IL-1β, and IL-6, demonstrating anti-inflammatory activity in a DSS-induced acute colitis model in mice.

CB2 receptor agonist 8 (Compound 17) is an agonist of the cannabinoid receptor 2 (CB2 receptor). It shows cytotoxicity in U87, RPMI 8226, HL-60, and L929 cells with IC50 values of 91.03, 16.29, 23.51, and 564.6 μM, respectively. CB2 receptor agonist 8 activates caspase 3/7, increases the expression of pro-apoptotic genes BAX, BAD, BIM, and the tumor suppressor gene p53, and induces apoptosis in U87 cells. Additionally, it inhibits the migration of U87 cells.

5-HT2A receptor agonist-5 (compound I-3) is a potent 5-HT2A agonist with a Ki value of 0.017 µM and exhibits antidepressant activity.

5-HT2A receptor agonist-7 (517) functions as a modulator of the 5-HT2A receptor, with an EC50 value of less than 100 nM.

5-HT2A receptor agonist-8 (compound 8) is a potent 5-HT2A receptor agonist with an EC50 of 0.6784 nM. It is suitable for research related to depression and bipolar disorder.

5-HT2A receptor agonist-9 is a β-arrestin-biased agonist of the 5-HT2A receptor. It may be utilized in research related to neurological conditions such as depression and psychedelia.

Orexin 2 Receptor Agonist 3 is an orally active and brain-penetrant agonist of the orexin receptor 2 (OX2) with an EC50 value of 2.5 nM. This compound increases wakefulness in both orexin/ataxin-3 NT1 mouse models and healthy Beagle dogs. It is applicable for research related to narcolepsy.

CB2receptor antagonist 3 (compound (S)-1) is an inverse agonist of the cannabinoid receptor CB2R, with a binding affinity (Kd) of 39 nM. This compound serves as a tool for synthesizing various CB2R probes.

CB2 receptor antagonist 4 is a selective inverse agonist for the CB2 receptor with a Kd value of 39 nM.