[18F]FEAC and [18F]FEDAC: Two novel positron emission tomography ligands for peripheral-type benzodiazepine receptor in the brain.
[(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.
Yanamoto
Kazuhiko
K
Department of Molecular Probes, Molecular Imaging Center, National Institute of Radiological Sciences, 4-9-1 Anagawa, Inage-ku, Chiba 263-8555, Japan.
Kumata
Katsushi
K
Yamasaki
Tomoteru
T
Odawara
Chika
C
Kawamura
Kazunori
K
Yui
Joji
J
Hatori
Akiko
A
Suzuki
Kazutoshi
K
Zhang
Ming-Rong
MR
D000818:Animals; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D005462:Fluorine Radioisotopes / Q000494:pharmacology*; D006801:Humans; D007249:Inflammation; D008024:Ligands; D008297:Male; D008956:Models, Chemical; D049268:Positron-Emission Tomography / Q000295:instrumentation* / Q000379:methods; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D011963:Receptors, GABA-A / Q000378:metabolism*
D005462:Fluorine Radioisotopes; D008024:Ligands; D019275:Radiopharmaceuticals; D011963:Receptors, GABA-A