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http://dx.doi.org/10.5012/bkcs.2009.30.5.1107

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)
Publication Information
Bulletin of the Korean Chemical Society / v.30, no.5, 2009 , pp. 1107-1112 More about this Journal
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.
Keywords
WAY-100635; Central nervous system (CNS); $5-HT_{1A}$; $^{99m}Tc$Tc;
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