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- W2148738862 abstract "Peripheral benzodiazepine receptor (PBR) is expressed in most organs and its expression is reported to be increased in activated microglia in the brain. [11C]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, [11C]DAA1106, for PBR and investigated its in vivo properties in rat and monkey brain. High uptake of [11C]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. [11C]DAA1106 binding was increased in the dorsal hippocampus with neural destruction, suggesting glial reaction. [11C]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. [11C]DAA1106 binding was four times higher compared to the binding of [11C]PK11195 in the monkey occipital cortex. These results indicated that [11C]DAA1106 might be a good ligand for in vivo imaging of PBR. Synapse 52:283–291, 2004. © 2004 Wiley-Liss, Inc." @default.
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- W2148738862 date "2004-01-01" @default.
- W2148738862 modified "2023-10-18" @default.
- W2148738862 title "Novel peripheral benzodiazepine receptor ligand [11C]DAA1106 for PET: An imaging tool for glial cells in the brain" @default.
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- W2148738862 doi "https://doi.org/10.1002/syn.20027" @default.
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