Novel 99mTc(CO)3 Complexes with WAY-100635 Moietyfor the Development of 5-HT1A Receptor Imaging Agent

Bulletin of the Korean chemical society

Kang Hyuk Choi¹  Mi Sun Pyun¹  Sun Ju Choi¹  Young Don Hong¹ 

关键词: WAY-100635;    Central nervous system (CNS);    5-HT1A;    99mTc;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

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.

【 授权许可】

Unknown