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Synthesis and Evaluation of 4-(4-phenoxy-4-phenylbutyl)piperazines for T-type Ca2+ channel blockers

등록일
2009년 8월 14일 16시 35분 52초
접수번호
1305
발표코드
38P208포 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
금 <발표Ⅳ>
발표형식
포스터
발표분야
의약화학
저자 및
공동저자
김익수, 이숙자, 이주현1, 금교창2, 강순방3, 김유승3
한국외국어대학교 화학과, Korea
1고려대학교 화학과, Korea
2한국과학기술연구원 케모인포메틱스연구센터, Korea
3한국과학기술연구원 생화학물질연구센터, Korea
T-type Ca2+ channels are a type of voltage-dependent calcium channel and widely expressed in neurons. T-type Ca2+ channels have attracted much attention since they are able to be novel therapeutic targets such as hypertensions, absence epilepsy, neuropathic pains, sleep disorder, and obesity. It is recently reported that T-type Ca2+ channel show subtype-specific and region-specific role in the pain pathway. In order to develop T-type Ca2+ channel blockers with higher potency and selectivity we have prepared a series of new 4-(4-phenoxy-4-phenylbutyl)piperazine derivatives by using Mitsunobu reaction and N-alkylation protocol. Their inhibitory activities on T-type Ca2+ channel were evaluated by in vitro assay with α1G and α1H clones using FDSS screening system. Their activity, subtype selectivity, and structure-activity relationship (SAR) on T-type Ca2+ channels will be presented.

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