Bulletin of the Korean Chemical Society

Korean Chemical Society (대한화학회)
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Novel 99mTc(CO)3 Complexes with WAY-100635 Moiety for the Development of 5-HT1A Receptor lmaging Agent

  • Choi, Kang-Hyuk (Radioisotope Research Division, Basic Science & Technology Department,Korea Atomic Energy Research Institute) ;
  • Pyun, Mi-Sun (Radioisotope Research Division, Basic Science & Technology Department,Korea Atomic Energy Research Institute) ;
  • Hong, Young-Don (Radioisotope Research Division, Basic Science & Technology Department,Korea Atomic Energy Research Institute) ;
  • Choi, Sun-ju (Radioisotope Research Division, Basic Science & Technology Department,Korea Atomic Energy Research Institute)
  • Published : 2009.05.20
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Abstract

The aim of this study is to develop and synthesize $5-HT_{1A}$ receptor imaging agents with WAY-100635 moiety and $^{99m}Tc(CO)_3$ core. WAY-100635 is commonly known as $5-HT_{1A}$ antagonist and its labeled compound ([$^{11}C$] WAY-100635) has been used as effective radioligand for imaging brain $5-HT_{1A}$ receptors with PET(Positron Emission Tomography). However, there are several restrictions in using a radioisotope of C-11 and requires for more effective radioisotopes and ligands. In order to produce a structure most similar to WAY-100635, WAY-100635 derivatives containing a cysteine chelator were designed and confirmed by using in silico (Hyperchem). The novel compounds (7a, 7b, 7c) were prepared in five or 7 steps with yields of 16%, 36% and 42%, respectively and radiolabeled with $[^{99m}Tc(CO)_3(H_2O)_3]^{+}$. The labeling yield was 99% for all the newly synthesized compounds. [$^{99m}Tc(CO)_3$]- WAY-100635 derivatives show a neutral charge which were confirmed by paper electrophoresis.

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References

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