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제112회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Synthesis and biological evaluation of tetrahydrothieno[2,3-c]pyridine derivatives as mGluR1/5 negative allosteric modulators

등록일
2013년 9월 5일 13시 48분 19초
접수번호
1372
발표코드
MEDI.P-956 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
10월 16일 (수요일) 16:00~19:00
발표형식
포스터
발표분야
의약화학
저자 및
공동저자
남민아, 배애님1,*, 백두종2,*
상명대학교 자연과학대 화학과, Korea
1한국과학기술연구원(KIST) 생체과학연구본부, Korea
2상명대학교 화학과, Korea
Glutamate (L-glutamic acid), the major excitatory transmitter in the mammalian central nervous system (CNS), exerts its effects through both ionotropic and metabotropic glutamate receptors, thereby generating the fast excitatory synaptic responses at the majority of CNS synapses and involved in pathologies of many brain diseases. While ionotropic glutamate receptors are ligand-gated ion channels responsible for mediation of glutamate fast transmission, the metabotropic glutamate receptors (mGlus) belong to family C of the Gprotein- coupled receptors (GPCRs) and modulate the strength of synaptic transmission and they are divided into three groups with eight subtypes on the basis of their sequence homology, pharmacology, and signal transduction mechanism. Group 1 consists of the mGluR1 and mGluR5, which are predominantly identified in post-synapses in the brain region, including the hippocampus, cerebellum, thalamic nuclei, and spinal cord. Recently studies show that selective mGluR5 antagonists may play a role in the treatment of neuropathic pain and other brain diseases. In this study, we report the synthesis and biological evaluation of novel tetrahydrothieno[2,3-c]pyridine derivatives as mGluR5 antagonists for treatment of neuropathic pain.

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