Cliffe I A
Department of Chemistry, Vernalis Research, Oakdene Court, 613 Reading Road, Winnersh, Workingham RG41 5UA, United Kingdom.
Nucl Med Biol. 2000 Jul;27(5):441-7. doi: 10.1016/s0969-8051(00)00109-8.
Abstract. An outline is given of the developments that led to the identification of [O-methyl-(11)C]WAY-100635 (4) as the first useful PET ligand for imaging serotonin(1A) (5-HT(1A)) receptors in the living human brain. Recent attempts to develop 5-HT(1A) receptor radioligands superior to 4 are reviewed, and [carbonyl-(11)C]WAY-100635 (6) has been shown to be the best currently available radioligand for human studies. Of other (11)C-radiolabelled compounds, O-methyl-(11)C-CPC-222 (9), DWAY (8), and [(11)C]NAD-299 (14) all demonstrate specific binding to 5-HT(1A) receptors in animals and warrant further expedited studies in humans. The trans-fluorocyclohexane, 12, and fluorobenzene, [(18)F]p-MPPF 13, are highlighted as examples of promising (18)F-labelled ligands.
摘要。本文概述了促使[O-甲基-(11)C]WAY-100635（4）被鉴定为用于活体人类大脑中5-羟色胺（1A）（5-HT(1A)）受体成像的首个实用正电子发射断层扫描（PET）配体的研究进展。综述了近期开发比4更优的5-HT(1A)受体放射性配体的尝试，且已证明[羰基-(11)C]WAY-100635（6）是目前可用于人体研究的最佳放射性配体。在其他(11)C标记的化合物中，O-甲基-(11)C-CPC-222（9）、DWAY（8）和[(11)C]NAD-299（14）在动物体内均显示出与5-HT(1A)受体的特异性结合，值得在人体中进一步加快研究。反式氟代环己烷12和氟苯[(18)F]p-MPPF 13被重点介绍，作为有前景的(18)F标记配体的示例。
