PURPOSE: The aim of the present study was to develop short half-lived tools for in vitro and in vivo β-amyloid imaging in mice, for which no suitable PET tracers are available. PROCEDURES: Five (13)N-labelled azo compounds (1-5) were synthesized using a three-step process using cyclotron-produced [(13)N]NO3 (-). Biodistribution studies were performed using positron emission tomography-computed tomography (PET-CT) on 20-month-old healthy, wild-type (WT) mice. In vivo and in vitro binding assays were performed using PET-CT and autoradiography, respectively, on 20-month-old healthy (WT) mice and transgenic (Tg2576) Alzheimer's disease model mice. RESULTS: (13)N-labelled azo compounds were prepared with decay corrected radiochemical yields in the range 27 ± 4 % to 39 ± 4 %. Biodistribution studies showed good blood-brain barrier penetration for compounds 1 and 3-5; good clearance data were also obtained for compounds 1-3 and 5. Compounds 2, 3 and 5 (but not 1) showed a significant uptake in β-amyloid-rich structures when assayed in in vitro autoradiographic studies. PET studies showed significant uptake of compounds 2 and 3 in the cortex of transgenic animals that exhibit β-amyloid deposits. CONCLUSIONS: The results underscore the potential of compounds 2 and 3 as in vitro and in vivo markers for β-amyloid in animal models of Alzheimer's disease.
PURPOSE: The aim of the present study was to develop short half-lived tools for in vitro and in vivo β-amyloid imaging in mice, for which no suitable PET tracers are available. PROCEDURES: Five (13)N-labelled azo compounds (1-5) were synthesized using a three-step process using cyclotron-produced [(13)N]NO3 (-). Biodistribution studies were performed using positron emission tomography-computed tomography (PET-CT) on 20-month-old healthy, wild-type (WT) mice. In vivo and in vitro binding assays were performed using PET-CT and autoradiography, respectively, on 20-month-old healthy (WT) mice and transgenic (Tg2576) Alzheimer's disease model mice. RESULTS:(13)N-labelled azo compounds were prepared with decay corrected radiochemical yields in the range 27 ± 4 % to 39 ± 4 %. Biodistribution studies showed good blood-brain barrier penetration for compounds 1 and 3-5; good clearance data were also obtained for compounds 1-3 and 5. Compounds 2, 3 and 5 (but not 1) showed a significant uptake in β-amyloid-rich structures when assayed in in vitro autoradiographic studies. PET studies showed significant uptake of compounds 2 and 3 in the cortex of transgenic animals that exhibit β-amyloid deposits. CONCLUSIONS: The results underscore the potential of compounds 2 and 3 as in vitro and in vivo markers for β-amyloid in animal models of Alzheimer's disease.
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Authors: Hiroshi Toyama; Daniel Ye; Masanori Ichise; Jeih-San Liow; Lisheng Cai; David Jacobowitz; John L Musachio; Jinsoo Hong; Mathew Crescenzo; Dnyanesh Tipre; Jian-Qiang Lu; Sami Zoghbi; Douglass C Vines; Jurgen Seidel; Kazuhiro Katada; Michael V Green; Victor W Pike; Robert M Cohen; Robert B Innis Journal: Eur J Nucl Med Mol Imaging Date: 2005-03-25 Impact factor: 9.236
Authors: Xiaoyun Deng; Jian Rong; Lu Wang; Neil Vasdev; Lei Zhang; Lee Josephson; Steven H Liang Journal: Angew Chem Int Ed Engl Date: 2019-01-14 Impact factor: 15.336