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  • 09월 06일 15시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제112회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Development of M1 selective muscarinic acetylcholine receptor agonists with cyclic oxime moiety

등록일
2013년 9월 5일 16시 35분 29초
접수번호
1435
발표코드
MEDI.P-960 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
10월 16일 (수요일) 16:00~19:00
발표형식
포스터
발표분야
의약화학
저자 및
공동저자
석대환, 임혜원1, 강순방, 금교창2,*
한국과학기술연구원(KIST) 뇌의약연구단, Korea
1한국과학기술연구원(KIST) 의과학연구센터, Korea
2한국과학기술연구원(KIST) 뇌의학연구단, Korea
Muscarinic acetylcholine receptors (mAChRs) mediate the metabotropic action of the neurotransmitter acetylcholine (ACh) in the peripheral and central nervous system, and consist of five muscarinic receptor subtypes, M1―M5. The M1 receptor subtype of them is abundant in cerebral cortex and hippocampus of central nervous system (CNS), and has been considered as potential therapeutic target for the treatment of cognitive dysfunction and impairment observed in Alzheimer′s disease (AD) and schizophrenia patients. Our efforts have been focused on developing novel M1 selective mAChR agonists with low side effects for the treatment of AD. We designed and synthesized new analogs that have (1) N-methyltetrahydropyridine moiety, (2) cyclic oxime moiety and (3) various substituents at 5 position of isoxazoline ring. We assayed the analogs in HEK293 cells transiently transfected with each human mAchR, and found an M1 selective compound and further examined the effect of the compound on ERK1/2 phosphorylation.

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