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제125회 대한화학회 학술발표회 및 총회 Synthesis and biological activity of biphenyl derivatives as 5-HT7R ligands

2020년 2월 5일 14시 38분 20초
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Medicinal Chemistry
저자 및
Doyoung Kim, Hyunah Choo1,*
Chemistry, Sogang University, Korea
1Neoro-Medicine, Korea Institute of Science and Technology, Korea
In recent study, it has been suggested that serotonin (5-hydroxytryptamine, 5-HT) is correlated with mental diseases including anxiety, mood disorder, depression, and schizophrenia. As a monoamine neurotransmitter, basically serotonin activates serotonin receptors (5-HTRs) and has extensive effects on the brain. All serotonin receptors (5-HT1R ~ 5-HT7R) belong to G protein-coupled receptors (GPCRs) family except 5-HT3R, which is a ligand-gated ion channel. Among them, 5-HT7R, the most recently discovered receptor, has been cloned from various species such as rodent, rabbit and human. It is localized in human brain, particularly hypothalamus, thalamus, raphe nuclei, cerebral cortex, and hippocampus. On the basis of its distribution in the central nervous system (CNS), 5-HT7R has been closely linked with multiple functions for instance regulation of sleep, mood, pain, and circadian rhythm. It has been reported that 5-HT7R activates adenylyl cyclase (AC) signaling resulting in conversion of ATP to cAMP via coupling to Gs which mediates a variety of cellular reactions and is associated with β-arrestin signaling pathway as well. So we conducted functional assay for Gs mediated cAMP production (cAMP assay) and β-arrestin recruitment (Tango assay). Herein, we designed and synthesized 5-HT7R ligands with biphenyl moiety of which biological evaluation was also performed. The results will be presented in detail.