Preparation and BiologicalEvaluation of Re/99Tcm(CO)3+-diphenyldiazeneDerivative as Candidates for Imaging Aβ Plaques in the Brain |
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Authors: | YANG Yang CUI Meng-chao TANG Rui-kun WU Rui ZHU Lin ZHANG Hua-bei |
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Affiliation: | Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education College of Chemistry, Beijing Normal University, Beijing 100875, China |
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Abstract: | To develop the non-invasiveand diagnostic agents for Alzheimer’s disease (AD), 99Tcm(CO)3+-L(L: (E)-2-(4-((4-(dimethylamino)phenyl)diazenyl)phenylamino)acetic acid, adiphenyldiazene derivative) was prepared,radiochemical purity was above 95%. Initialautoradiography results suggested that 99Tcm(CO)3+-Lshowed selective binding to the Aβ plaque-like structures in the brain section from theAD transgenic mice (Tg C57, APP, PS1 12-month-old), further, 99Tcm(CO)3+-Lshowed the same binding sites with fluorescence stained by Re(CO)3+-L.Biodistribution of 99Tcm(CO)3+-L innormal mice demonstrated low uptake in brain (5 min: (0.52 ±0.11)% ID/g)whilst slow clearance from the brain tissues at 120 min post-injection (0.28 ± 0.04)%ID/g. The corresponding Re analogue was alsosynthesized, and the nature of its lowest electronically excited state wasdetermined by studies of the UV-vis absorption and fluorescence emissionproperties at room temperature. In addition, the fluorescent staining of the Re-complexwas performed in comparison to Thioflavin-T and autoradiography results of 99Tcm(CO)3+-L.In conclusion, these results are encouraging for further exploration of 99Tcm(CO)3+-Las a SPECT imaging agent for Aβplaques in the AD brain. |
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Keywords: | Re/99Tcm(CO)3+-L A&beta plaques autoradiography fluorescent staining |
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