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N ‐(Biphenyl‐3‐ylmethyl)ethanamines as G protein‐biased agonists of 5‐HT 7 R
Kim Doyoung,Lee Jieon,Kwag Rina,Kim Hyunbin,Oh Hyunji,문봉진,Kim Hak Joong,Seong Jihye,Jeon Byungsun,Kang Taek,Choo Hyunah 대한화학회 2022 Bulletin of the Korean Chemical Society Vol.43 No.1
There has been much attention to biased ligands of G protein-coupled receptors (GPCRs) for potential pharmacological benefits. Recently, we reported N- ((6-chloro-2’-methoxy-[1,1’-biphenyl]-3-yl)methyl)ethanamine 1 as G proteinbiased agonist of 5-HT7R, which could be used as a chemical probe for the study on treatment discovery of autism spectrum disorder. Herein, we describe the synthesis of derivatives of the compound 1 and their biological evaluations in both G protein and β-arrestin signaling pathway. Total 16 compounds were synthesized and evaluated, and the compounds 3c, 3f, 3i, and 3p could be called as G protein-biased agonists like the compound 1. Among the four compounds, the compound 3c was the best in efficacy with an Emax value of 73% and the compound 3f was the most potent agonist with an EC50 value of 0.094 μM.