Eunseo Park, Jieon Lee, Jinhyuk Kim, Gyeongmin Kim, Hyunah Choo, Taek Kang, Byungsun Jeon, Ansoo Lee
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引用次数: 0
Abstract
Biphenylyl-N-ethylethanamines, novel 5-HT7R agonists synthesized from 4-chloro-3-iodobenaldehyde, activate the Gs signaling pathway. Among derivatives, compounds 4c and 4f showed potent 5-HT7R agonism, with EC50 values of 89 and 70 nM, respectively, in cAMP assays. Western blot analysis confirmed dose- and time-dependent ERK phosphorylation, with 4c and 4f inducing sustained pERK expression (14.5- and 11.4-fold at 60 min) compared to 5-HT (4.0-fold), indicating prolonged signaling. Compound 4f exhibited acceptable drug-like properties, including minimal CYP inhibition and moderate microsomal stability. These findings highlight the pharmacological potential of 4f as a 5-HT7R modulator, warranting further in vivo studies to explore its therapeutic applications.
期刊介绍:
The Bulletin of the Korean Chemical Society is an official research journal of the Korean Chemical Society. It was founded in 1980 and reaches out to the chemical community worldwide. It is strictly peer-reviewed and welcomes Accounts, Communications, Articles, and Notes written in English. The scope of the journal covers all major areas of chemistry: analytical chemistry, electrochemistry, industrial chemistry, inorganic chemistry, life-science chemistry, macromolecular chemistry, organic synthesis, non-synthetic organic chemistry, physical chemistry, and materials chemistry.