title: (99m)Tc-labeled dibenzylideneacetone derivatives as potential SPECT probes for in vivo imaging of β-amyloid plaque.
abstract: Four (99m)Tc-labeled dibenzylideneacetone derivatives and corresponding rhenium complexes were successfully synthesized and biologically evaluated as potential imaging probes for Aβ plaques using SPECT. All rhenium complexes (5a-d) showed affinity for Aβ(1-42) aggregates (Ki = 13.6-120.9 nM), and selectively stained the Aβ plaques on brain sections of transgenic mice. Biodistribution in normal mice revealed that [(99m)Tc]5a-d exhibited moderate initial uptake (0.31%-0.49% ID/g at 2 min) and reasonable brain washout at 60 min post-injection. Although additional optimizations are still needed to facilitate it's penetration through BBB, the present results indicate that [(99m)Tc]5a may be a potential SPECT probe for imaging Aβ plaques in Alzheimer's brains.
authors: Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China.
authors: Yanping
authors: Y
authors: Yang
authors: Mengchao
authors: M
authors: Cui
authors: Bing
authors: B
authors: Jin
authors: Xuedan
authors: X
authors: Wang
authors: Zijing
authors: Z
authors: Li
authors: Pingrong
authors: P
authors: Yu
authors: Jianhua
authors: J
authors: Jia
authors: Hualong
authors: H
authors: Fu
authors: Hongmei
authors: H
authors: Jia
authors: Boli
authors: B
authors: Liu
mesh_terms: D016229:Amyloid beta-Peptides / Q000737:chemistry / Q000378:metabolism; D000818:Animals; D002074:Butanones / Q000737:chemistry*; D004195:Disease Models, Animal; D005456:Fluorescent Dyes / Q000138:chemical synthesis / Q000737:chemistry*; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D008813:Mice, Inbred ICR; D008822:Mice, Transgenic; D057054:Molecular Imaging; D015394:Molecular Structure; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry*; D010446:Peptide Fragments / Q000737:chemistry / Q000378:metabolism; D058225:Plaque, Amyloid / Q000737:chemistry* / Q000378:metabolism; D012211:Rhenium / Q000737:chemistry; D013194:Staining and Labeling; D013667:Technetium / Q000737:chemistry*; D015899:Tomography, Emission-Computed, Single-Photon
chemical_list: D016229:Amyloid beta-Peptides; D002074:Butanones; D005456:Fluorescent Dyes; D009942:Organometallic Compounds; D010446:Peptide Fragments; C075222:amyloid beta-protein (1-42); D012211:Rhenium; D013667:Technetium; C025383:benzylideneacetone