psb-kd 477

R-(+)-EU-1180-453 是一种新型 GluN2C D 选择性 NMDAR 阳性变构调节剂，可用于研究神经系统疾病。

PSB-KD477 is an Agonist of the Cannabinoid-Activated Orphan G-Protein-Coupled Receptor GPR18. PSB-KD477 displayed significantly higher potency and efficacy than THC, determined in a GPR18-dependent β-arrestin recruitment assay, and were found to be selective versus the CB-sensitive receptors CB1, CB2, and GPR55. Structure-activity relationships were steep, and indole substitution was crucial for biological activity. These first selective agonists, which are structurally distinct from the lipidic agonist(s), will allow target validation studies and may eventually contribute to the deorphanization of GPR18.