뇌혈류 영상용 방사성의약품 PRODD의 $^{99m}Tc$ 표지 및 생체내분포

$^{99m}Tc$ Labeling and Biodistribution of PRODD as a Cerebral Blood Flow Imaging Radiopharmaceutical

  • 정수욱 (서울대학교병원 핵의학과) ;
  • 정재민 (서울대학교병원 핵의학과) ;
  • 이동수 (서울대학교병원 핵의학과) ;
  • 조정혁 (한국과학기술연구원 응용과학부) ;
  • 오승준 (한국과학기술연구원 응용과학부) ;
  • 정준기 (서울대학교병원 핵의학과) ;
  • 이명철 (서울대학교병원 핵의학과) ;
  • 고창순 (서울대학교병원 핵의학과)
  • Chung, Soo-Wook (Department of Nuclear Medicine, Seoul National University Hospital) ;
  • Jeong, Jae-Min (Department of Nuclear Medicine, Seoul National University Hospital) ;
  • Lee, Dong-Soo (Department of Nuclear Medicine, Seoul National University Hospital) ;
  • Cho, Jung-Hyuck (Division of Applied Science, Korea Institute of Science and Technology) ;
  • Oh, Seung-Joon (Division of Applied Science, Korea Institute of Science and Technology) ;
  • Chung, June-Key (Department of Nuclear Medicine, Seoul National University Hospital) ;
  • Lee, Myung-Chul (Department of Nuclear Medicine, Seoul National University Hospital) ;
  • Koh, Chang-Soon (Department of Nuclear Medicine, Seoul National University Hospital)
  • 발행 : 1995.09.25

초록

$^{99m}Tc$ labeled PnAO(propylene amine oxime) derivatives have been widely studied as brain perfusion agents. We synthesized and characterized a PnAO derivative, (RR/SS/ meso)-4,8-diaza-3,9-dimethylundecane-2, 10-dione bisoxime(PRODD). Proton-NMR spectroscopy and thin layer chromatography(silica gel) were performed for its characterization. PRODD was labeled with $^{99m}Tc$ using stannous chloride as reducing agent. The labeling efficiency was determined to be about 85%. Brain uptakes of $4.16{\pm}0.42$ %ID/g and $3.24{\pm}0.13$ %ID/g were found after 10min and 30min after intravenous injection. Brain-to-blood ratios were 1.17 and 0.75 at 10 and 30 minutes, which were lower than 1.3 and 1.9 of the ratios with commercial ${\pm}$-HMPAO. Autoradiographs of rat brain sections showed the gray matter to white matter ratios of $1.13{\pm}0.10$ at 30 min after intravenous injection, which was lower than $1.94{\pm}0.19$ of commercial $^{99m}Tc$-HMPAO. With the above findings, we concluded that the lipophilic $^{99m}Tc$-PRODD complex was able to cross the blood-brain barrier, however the complex showed lower uptake than $^{99m}Tc$-HMPAO in mouse or rat brains. We could suggest possibility that PRODD could be used as another $^{99m}Tc$ chelator.

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