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제125회 대한화학회 학술발표회 및 총회 Synthesis and biological evaluation of novel 5-HT7R ligands with biaryl moiety

2020년 2월 5일 14시 37분 12초
MEDI.P-695 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
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Medicinal Chemistry
저자 및
Jieon Lee, Hyunah Choo1,*
Division of Bio-Medical Science & Technology, University of Science & Technology, Korea
1Center for neuro medicine, Korea Institute of Science and Technology, Korea
Serotonin, 5-hydroxytryptamine (5-HT) has been the subject of intense research efforts because of its responsibility for multiple physiological functions. In the central nervous system (CNS), 5-HT is involved in multiple functions, including cognition, memory processes, modulation of circadian rhythm, and mood. All of these physiological processes are mediated through a variety of receptors that are classified on the basis of structural, functional, and pharmacological criteria. Among the 5-HT receptors (5-HTRs), the 5-HT7 receptor (5-HT7R) was the last to be discovered in 1993. Autoradiographic and immunohistochemisry studies showed that 5-HT7R is distributed within the CNS with high to moderate concentration in limbic areas, such as the thalamus, hypothalamus, hippocampus, and amygdala, in the raphe and cortical regions. The presence of 5-HT7R in the CNS tends to indicate that it is involved in important roles such as circadian rhythm, sleep, learning and memory as well as several diseases such as migraine, sleep disturbance, and depression. 5-HT7R belongs to the family of G protein coupled receptors(GPCRs) and is shown to be positively coupled to adenylate cyclase (AC) through activation of Gs-proteins, resulting in an extracellular increase of cAMP, and displays a high constitutive AC activity. Herein, we designed and synthesized 5-HT7R novel ligands with biaryl core structure of which biological evaluations are also performed. The results will be presented in details.