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• W3029331878 abstract "Objective To develop and evaluate 4- 18 F-fluoro- N -2-[1-(2-methoxyphenyl)-1-piperazinyl]ethyl- N -2-pridinyl-benzamide ( 18 F-MPPF) as a 5-hydroxytryptamine (5-HT 1A ) imaging agent. Methods Nucleophilic substitution of fluoro replacement reaction was proceeding in dimethyl sulfoxide (DMSO) solution by oil-bath heating. Radiochemical purity (RCP) was determined by high pressure liquid chromatography (HPLC). Biological evaluations were performed in rats and mice. Results RCP determined by HPLC was over 95% and were stable within 3 h. Biodistribution studies in rats showed that the initial uptake of 18 F-MPPF in the brain was high [(0.621±0.010) %ID/organ at 2 min]. The specific binding in hippocampus reaches its peak value of 2.70 at 30 min postinjection. (T/CB)-1 in hippocampus were significantly reduced to 0.89,0.74 and 1.93 by pretreatment with 8-hydroxy-2- N,N -(di- n -propyl) aminotetralin (8-OH-DPAT),4-(2′-methoxy-phenyl)-1-[2′-( n -2″-pyridinyl)-cyclohexanecarboxamido]-ethyl-piperazine (WAY100635) and spiperone at 30 min postinjection,respectively. The rat brain autoradiography and analysis showed that there was high 131 I-4-(2′-methoxy-phenyl)-1-[2′-( n -2″-pyridinyl)- p -iodobenzamido]-ethyl piperazine (MPPI) upake in hippocampus,the hippocampus/cerebellum ratio was significantly reduced from 13.98±0.87 to 1.96±0.46 by pretreatment with 8-OH-DPAT at 30 min postinjection. Conclusions 18 F-MPPF can be specifically accumulated in hippocampus. It suggests that 18 F-MPPF might be a useful imaging agent for the studies of localization,function and modulation of 5-HT 1A receptor in the brain." @default.
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• W3029331878 date "2004-04-25" @default.
• W3029331878 modified "2023-09-23" @default.
• W3029331878 title "Preparation and biological evaluation of ~(18)F-MPPF as a 5-HT_(1A) imaging agent" @default.
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