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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 30, Number 5
BKCSDE 30(5)
May 20, 2009 

Novel 99mTc(CO)3 Complexes with WAY-100635 Moiety
for the Development of 5-HT1A Receptor Imaging Agent
Kang Hyuk Choi, Mi Sun Pyun, Young Don Hong, Sun Ju Choi*
WAY-100635, Central nervous system (CNS), 5-HT1A, 99mTc
The aim of this study is to develop and synthesize 5-HT1A receptor imaging agents with WAY-100635 moiety and 99mTc(CO)3 core. WAY-100635 is commonly known as 5-HT1A antagonist and its labeled compound ([11C] WAY-100635) has been used as effective radioligand for imaging brain 5-HT1A 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 [99mTc(CO)3(H2O)3]+. The labeling yield was 99% for all the newly synthesized compounds. [99mTc(CO)3]- WAY-100635 derivatives show a neutral charge which were confirmed by paper electrophoresis.
1107 - 1112
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