Kawamura Kazunori, Elsinga Philip H, Kobayashi Tadayuki, Ishii Shin-ichi, Wang Wei-Fang, Matsuno Kiyoshi, Vaalburg Willem, Ishiwata Kiichi
Positron Medical Center, Tokyo Metropolitan Institute of Gerontology, Tokyo, Japan.
Nucl Med Biol. 2003 Apr;30(3):273-84. doi: 10.1016/s0969-8051(02)00439-0.
We prepared sigma(1)-receptor selective 1-([4-methoxy-(11)C]-3,4-dimethoxyphenethyl)-4-(3-phenylpropyl)piperazine ([(11)C]SA4503) and its fluorinated analog 1-([4-methoxy-(11)C]3,4-dimethoxyphenethyl)-4-[3-(4-fluorophenyl)propyl]piperazine ([(11)C]SA5845), and their [(11)C]ethoxy and [(18)F]fluoroethoxy analogs, and evaluated their potential for positron emission tomography studies. [(11)C]SA4503 is most selective for sigma(1) receptors, and the other five showed affinities for sigma(1) and sigma(2) receptors with a different extent. All radioligands showed the receptor-specific binding in the brain, and visualized similar regional brain distributions by ex vivo autoradiography. The [(11)C]ethoxy analogs were relatively labile for metabolism.
我们制备了西格玛-1受体选择性的1-([4-甲氧基-(11)C]-3,4-二甲氧基苯乙胺)-4-(3-苯丙基)哌嗪([(11)C]SA4503)及其氟化类似物1-([4-甲氧基-(11)C]3,4-二甲氧基苯乙胺)-4-[3-(4-氟苯基)丙基]哌嗪([(11)C]SA5845)，以及它们的[(11)C]乙氧基和[(18)F]氟乙氧基类似物，并评估了它们在正电子发射断层扫描研究中的潜力。[(11)C]SA4503对西格玛-1受体具有最高选择性，其他五种对西格玛-1和西格玛-2受体具有不同程度的亲和力。所有放射性配体在脑中均显示出受体特异性结合，并通过离体放射自显影显示出相似的脑区分布。[(11)C]乙氧基类似物代谢相对不稳定。
