In vivo evaluation of [¹⁸F]FECIMBI-36, an agonist 5-HT_2A/2C receptor PET radioligand in nonhuman primate

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• 作者：Jaya Prabhakaran^a ; ^b ; Kiran Kumar Solingapuram Sai^c ; Francesca Zanderigo^a ; ^b ; Harry Rubin-Falcone^a ; Matthew J. Jorgensen^d ; Jay R. Kaplan^d ; Katharine I. Tooke^a ; Akiva Mintz^c ; J. John Mann^a ; ^b ; J.S. Dileep Kumar^b ; ^{kumardi@nyspi.columbia.edu}
• 关键词：5-HT ; 5-HT2A/2CR ; Agonist ; PET ; Radiotracer
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：1 January 2017
• 年：2017
• 卷：27
• 期：1
• 页码：21-23
• 全文大小：873 K
• 卷排序：27

文摘

We recently reported the radiosynthesis and in vitro evaluation of [18F]-2-(4-bromo-2,5-dimethoxyphenyl)-N-(2-(2-fluoroethoxy)benzyl)ethanamine, ([18F]FECIMBI-36) or ([18F]1), an agonist radioligand for 5HT2A/2C receptors in postmortem samples of human brain. Herein we describe the in vivo evaluation of [18F]FECIMBI-36 in vervet/African green monkeys by PET imaging. PET images show that [18F]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 [18F]FECIMBI-36 in brain may limit the use of this tracer for quantification of 5-HT2A/2C receptors by PET.