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  • 02월 26일 17시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제115회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Synthesis of 99mTc(CO)3 labeled 2-(4-chloro)phenyl-imidazo[1,2-a]pyridine analog (99mTc-CB256)

등록일
2015년 2월 12일 13시 47분 42초
접수번호
0866
발표코드
MEDI.O-2 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
금 10시 : 20분
발표형식
구두발표
발표분야
의약화학 - Oral Presentation for Young Medicinal Chemists
저자 및
공동저자
최지영, 이병철1,*
서울대학교 융합과학기술대학원 방사선융합의생명전공, Korea
1분당서울대학교병원 핵의학과, Korea

The 18 kDa translocator protein (TSPO) is a mitochondrial protein associated with a wide number of biological processes including cell proliferation, apoptosis, steroidogenesis, and immunomodulation. In this work, we synthesized 99mTc-CB256 as a new TSPO-selective SPECT imaging agent and performed TSPO-positive tumor cell binding assay. Re-CB256 and 99mTc-CB256 were synthesized as described in Fig 1. 99mTc-CB256 was synthesized in 75~85% of radiochemical yield (d.c.) with over 98% of radiochemical purity. The chemical identity of 99mTc-CB256 was confirmed by comparing retention time of 99mTc-CB256 (22.5 min) with that of Re-CB256 (22 min), including NMR and HRMS. The obtained 99mTc-CB256 was shown to be highly stable (>99%) in human serum for 4 h and had a relatively low lipophilicity (log D = 2.15 ± 0.02). In vitro time dependent tumor cell binding uptake of 99mTc-CB256 was shown 10.26 ± 0.23 and 7.88 ± 0.23 %ID in C6 and U87-MG cells at 60 min, respectively. Our in vitro data indicated that 99mTc-CB256 can be considered as a new TSPO-positive cancer imaging agent and provides the foundation for further in vivo biological evaluation in tumor xenograft.


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