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Synthesis and Small Animal Brain PET Study of a Serotonin Receptor Radiotracer, 18F-Mefway

세로토닌 5-HT1A수용체 방사성 추적자 18F-Mefway의 합성과 소동물 뇌 PET 연구

  • 안성민 (가천의과대학교 방사선학과) ;
  • 홍태기 (한서대학교 화학과) ;
  • 유영훈 (연세대학교 강남세브란스병원 핵의학과) ;
  • 최재용 (연세대학교 강남세브란스병원 핵의학과) ;
  • 김성철 (가천의과대학교 방사선학과)
  • Published : 2009.11.28

Abstract

$^{18}F$-mefway has been developed as radioligand for serotonin receptor 5-$HT_{1A}$. The object of this study was to obtain the mefway precursor with the higher yield than previous method and to identify whether $^{18}F$-mefway can bind to 5-$HT_{1A}$ or not. from microPET imaging of small animal brain. Precursor was prepared by a modification of the reported procedure then [$^{18}F$] labeling was performed by adding $^{18}F$ ion at $130^{\circ}C$ in the hot cell for 30min. After purification of reaction mixture using alumina Sep-pak and HPLC, microPET images of small animal brain were determined. The chemical yield of precursor was increased from 9% to 34% using oxalyl chloride and LAH/diethylether. We synthesized a precursor which was successfully labeled with no-carrier-added $^{18}F$-by new synthetic route. This research suggest that $^{18}F$-mefway will be used a radiopharmaceutical for evaluation of central nerve system disorder as imaging a gent for 5-$HT_{1A}$ receptor.

세로토닌 수용체 5-$HT_{1A}$에 대한 방사성추적자로 알려진 $^{18}F$-mefway를 개선된 방법으로 합성하고, 소 동물 뇌 microPET 연구를 통해서 이 수용체에 선택적으로 결합하는 지를 확인하려고 한다. 기존 합성 방법을 수정하여 전구체를 합성하고, $[^{18}F]^-$$130^{\circ}C$에서 30분간 교반하여 $^{18}F$-mefway를 합성하여, Solid phase extraction(SPE)과 HPLC를 이용해 정제한 다음, 소동물 뇌의 microPET 다이나믹 영상을 얻었다. Oxalyl chloride와 LAH/diethyl ether을 사용해서 기존 합성수율 9%에서 34%로 $^{18}F$-mefway 전구체를 향상된 수율로 합성할 수 있는 개선된 방법을 확립하였다. 이렇게 합성된 $^{18}F$-mefway는 세로토닌 5-$HT_{1A}$수용체 영상용 방사성 의약품으로서 신경정신질환 연구에 이용될 수 있을 것으로 사료된다.

Keywords

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