[18F]FEAC and [18F]FEDAC: Two novel positron emission tomography ligands for peripheral-type benzodiazepine receptor in the brain

Kazuhiko Yanamoto; Katsushi Kumata; Tomoteru Yamasaki; Chika Odawara; Kazunori Kawamura; Joji Yui; Akiko Hatori; Kazutoshi Suzuki; Ming-Rong Zhang

doi:10.1016/j.bmcl.2009.01.093

[18F]FEAC and [18F]FEDAC: Two novel positron emission tomography ligands for peripheral-type benzodiazepine receptor in the brain

Bioorg Med Chem Lett. 2009 Mar 15;19(6):1707-10. doi: 10.1016/j.bmcl.2009.01.093. Epub 2009 Jan 31.

Authors

Kazuhiko Yanamoto¹, Katsushi Kumata, Tomoteru Yamasaki, Chika Odawara, Kazunori Kawamura, Joji Yui, Akiko Hatori, Kazutoshi Suzuki, Ming-Rong Zhang

Affiliation

¹ Department of Molecular Probes, Molecular Imaging Center, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba 263-8555, Japan.

PMID: 19217778
DOI: 10.1016/j.bmcl.2009.01.093

Abstract

[(18)F]FEAC ([(18)F]4a) and [(18)F]FEDAC ([(18)F]4b) were developed as two novel positron emission tomography (PET) ligands for peripheral-type benzodiazepine receptor (PBR). [(18)F]4a and [(18)F]4b were synthesized by fluoroethylation of precursors 8a and 8b with [(18)F]FCH(2)CH(2)Br ([(18)F]9), respectively. Small-animal PET scan for a neuroinflammatory rat model showed that the two radioligands had high uptakes of radioactivity in the kainic acid-infused striatum, a brain region where PBR density was increased.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Brain / drug effects
Brain / metabolism
Chemistry, Pharmaceutical / methods*
Drug Design
Fluorine Radioisotopes / pharmacology*
Humans
Inflammation
Ligands
Male
Models, Chemical
Positron-Emission Tomography / instrumentation*
Positron-Emission Tomography / methods
Radiopharmaceuticals / chemical synthesis*
Radiopharmaceuticals / pharmacology*
Rats
Rats, Sprague-Dawley
Receptors, GABA-A / metabolism*

Substances

Fluorine Radioisotopes
Ligands
Radiopharmaceuticals
Receptors, GABA-A