Premium
Novel peripheral benzodiazepine receptor ligand [ 11 C]DAA1106 for PET: An imaging tool for glial cells in the brain
Author(s) -
Maeda Jun,
Suhara Tetsuya,
Zhang MingRong,
Okauchi Takashi,
Yasuno Fumihiko,
Ikoma Yoko,
Inaji Motoki,
Nagai Yuji,
Takano Akihiro,
Obayashi Shigeru,
Suzuki Kazutoshi
Publication year - 2004
Publication title -
synapse
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.809
H-Index - 106
eISSN - 1098-2396
pISSN - 0887-4476
DOI - 10.1002/syn.20027
Subject(s) - in vivo , choroid plexus , ligand (biochemistry) , olfactory bulb , chemistry , cerebellum , hippocampal formation , receptor , microglia , hippocampus , pons , microbiology and biotechnology , neuroscience , biophysics , biology , central nervous system , medicine , biochemistry , inflammation
Peripheral benzodiazepine receptor (PBR) is expressed in most organs and its expression is reported to be increased in activated microglia in the brain. [ 11 C]PK11195 has been widely used for the in vivo imaging of PBRs, but its signal in the brain was not high enough for stable quantitative analysis. We synthesized a novel positron emission tomography (PET) ligand, [ 11 C]DAA1106, for PBR and investigated its in vivo properties in rat and monkey brain. High uptake of [ 11 C]DAA1106 was observed in the olfactory bulb and choroid plexus area, followed by the pons/medulla and cerebellum by in vivo autoradiography of rat brain, correlating with the binding in vitro. [ 11 C]DAA1106 binding was increased in the dorsal hippocampus with neural destruction, suggesting glial reaction. [ 11 C]DAA1106 binding was both inhibited and displaced by 1.0 mg/kg of DAA1106 and 5 mg/kg of PK11195 by 80% and 70%, respectively. Specific binding was estimated as 80% of total binding. [ 11 C]DAA1106 binding was four times higher compared to the binding of [ 11 C]PK11195 in the monkey occipital cortex. These results indicated that [ 11 C]DAA1106 might be a good ligand for in vivo imaging of PBR. Synapse 52:283–291, 2004. © 2004 Wiley‐Liss, Inc.