Bulletin of the Korean Chemical Society

Korean Chemical Society (대한화학회)
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99mTc(CO)3-Labeled Histidine-Arylpiperazines as Potential Radiotracers for a Neuroreceptor Targeting

  • Choi, Kang-hyuk (Radioisotope R&D LAB, HANARO Application Research, Korea Atomic Energy Research Institute) ;
  • Hong, Young-Don (Radioisotope R&D LAB, HANARO Application Research, Korea Atomic Energy Research Institute) ;
  • Choi, Ok-Ja (Radioisotope R&D LAB, HANARO Application Research, Korea Atomic Energy Research Institute) ;
  • Choi, Sun-Ju (Radioisotope R&D LAB, HANARO Application Research, Korea Atomic Energy Research Institute)
  • Published : 2006.08.20
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Abstract

In order to develop radiopharmaceuticals for targeting a serotonin receptor such as $5-HT_{1A}$, histidine-$C_n$-arylpiperazines (AP) (C = alkyl, n = 2, 3, 4) were prepared in five steps with yields of 25%, 37% and 51%, respectively, and radiolabeled with the $[^{99m}Tc(CO)_3(H_2O)+3]^+$. The $^{99m}Tc(CO)_3$-Histidine-Cn-APs were prepared with a high yield (>99%) and characterized as a tridentate complex with a neutral charge to pass through the blood-brain barrier (BBB). The rhenium complexes with $Re(CO)_3$ were also synthesised and comparative experiments were achieved to evaluate the nature of the $^{99m}Tc$ complexes.

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