Park, Eunseo Lee, Jieon Kim, Jinhyuk Kim, Gyeongmin Choo, Hyunah Kang, Taek Jeon, Byungsun Lee, Ansoo 2025-07-21T00:00:09Z 2025-07-21T00:00:09Z 2025-07-18 2025-06 0253-2964 https://pubs.kist.re.kr/handle/201004/152838 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. English 대한화학회 Biphenylyl-N-ethylethanamines induce ERK phosphorylation through 5-HT7R-Gs signaling pathway Article 10.1002/bkcs.70030 1 Bulletin of the Korean Chemical Society, v.46, no.6, pp.636 - 640 Bulletin of the Korean Chemical Society 46 6 636 640 N scie scopus kci ART003212374 001511538200001 Chemistry, Multidisciplinary Chemistry Article SEROTONIN MECHANISMS RECEPTORS Drug-like properties ERK phosphorylation Gs signaling Serotonin 5-HT7R agonists