Prabhakaran Jaya, Solingapuram Sai Kiran Kumar, Zanderigo Francesca, Rubin-Falcone Harry, Jorgensen Matthew J, Kaplan Jay R, Tooke Katharine I, Mintz Akiva, Mann J John, Kumar J S Dileep
Department of Psychiatry, Columbia University Medical Center, New York, USA; Molecular Imaging and Neuropathology Division, New York State Psychiatric Institute, New York, USA.
Department of Radiology, Wake Forest School of Medicine, Winston-Salem, NC, USA.
Bioorg Med Chem Lett. 2017 Jan 1;27(1):21-23. doi: 10.1016/j.bmcl.2016.11.043. Epub 2016 Nov 16.
We recently reported the radiosynthesis and in vitro evaluation of [F]-2-(4-bromo-2,5-dimethoxyphenyl)-N-(2-(2-fluoroethoxy)benzyl)ethanamine, ([F]FECIMBI-36) or ([F]1), an agonist radioligand for 5HT receptors in postmortem samples of human brain. Herein we describe the in vivo evaluation of [F]FECIMBI-36 in vervet/African green monkeys by PET imaging. PET images show that [F]FECIMBI-36 penetrates the blood-brain barrier and a low retention of radioactivity is observed in monkey brain. Although the time activity curves indicate a somehow heterogeneous distribution of the radioligand in the brain, the low level of [F]FECIMBI-36 in brain may limit the use of this tracer for quantification of 5-HT receptors by PET.
我们最近报道了[F]-2-(4-溴-2,5-二甲氧基苯基)-N-(2-(2-氟乙氧基)苄基)乙胺（[F]FECIMBI-36或[F]1）的放射性合成及其在人脑死后样本中作为5HT受体激动剂放射性配体的体外评估。在此，我们描述了通过PET成像对黑长尾猴/非洲绿猴体内[F]FECIMBI-36的评估。PET图像显示[F]FECIMBI-36可穿透血脑屏障，并且在猴脑中观察到放射性的低滞留。尽管时间-活性曲线表明放射性配体在脑中的分布存在某种程度的异质性，但脑中[F]FECIMBI-36的低水平可能会限制该示踪剂用于通过PET定量5-HT受体。
