σ2 receptor

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).

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

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.

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.

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.

CB2receptor agonist 6 (compound 70) is a CB2R agonist with an EC50 of 162 nM. It has IC50 values of 4.83 μM for CB1R and 0.88 μM for CB2R. As a neuroprotective agent, CB2receptor agonist 6 is useful for research in neurological disorders.

Sigma-2 Receptor ligand 1 (Compound 7i) is a highly selective ligand for the Sigma-2 receptor, with a Ki of 40 nM. It shows potential for Alzheimer's disease research.

EP2 receptor antagonist-3 is a selective antagonist of the EP2 receptor, with an IC50 of 8 nM determined in the hEP2 SPA assay and an IC50 of 50 nM in the hEP2 cAMP assay. It enhances macrophage-mediated clearance of Amyloid-β plaques. In CD-1 mice, it shows moderate clearance and good exposure, and exhibits good central nervous system (CNS) exposure in both mice and rats. EP2 receptor antagonist-3 is applicable for research in Alzheimer's disease.

GP 2A is a selective agonist of CB2 receptor.

Orexin 2 Receptor Agonist (OX2R) is an effective (EC50: 23 nM) and OX2R-selective (OX1R/OX2R EC50 ratio: 70) agonist.

Orexin 2 Receptor Agonist 2 (ORA-2) is a specific agonist for the orexin 2 receptor.

Edg-2 receptor inhibitor 1 (SAR-100842) is an Edg-2 receptor inhibitor extracted (IC50: <0.1 μM).

Dopamine D2 receptor agonist-2 (Dopamine D2 Receptor) is a ligand targeting the dopamine D2 receptor.

Hexyl resorcinol derivative 29 is a CB2 selective competitive antagonist/reverse agonist demonstrating notable potency. Meanwhile, Olivanol and 5-(2-methyloctane-2-yl) resorcinol derivatives 23 and 24 exhibit substantial antinociceptive effects. Notably, compound 24 activates both cannabinoid and TRPV1 receptors.

EP2 receptor antagonist-1 is a reversible, potent, agonist-dependent variant of the prostaglandin EP2 receptor antagonist.EP2 receptor antagonist-1 exhibits anti-inflammatory activity.

Vasopressin V2 receptor antagonist 1 (Compound 4g) is a vasopressin V2 receptor (V2R) antagonist with a Ki of 3.8 nM, used in the treatment of autosomal dominant polycystic kidney disease (ADPKD).

Compound 39, also known as CB2 receptor antagonist 2, is a potent CB2 antagonist exhibiting an IC50 of 0.33 μM. It engages in strong interactions with residues L17, W6.48, V6.51, and C7.42 [1].

Compound 17, a dopamine D4 receptor ligand, exhibits high potency and selectivity with IC 50 values of 0.057 nM for D4, and >1000, 220, and 270 nM for D2, 5-HT1A, and α1 receptors, respectively [1].

Vasopressin V2 receptor antagonist 2 (Compound 33) is an arginine vasopressin V2 receptor (V2R) antagonist with a Ki of 6.2 nM. It effectively reduces cAMP levels, thereby inhibiting the growth of renal cysts.

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

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.