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10.1021/ml400042w

http://scihub22266oqcxt.onion/10.1021/ml400042w
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C4027563!4027563 !24900692
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suck abstract from ncbi

pmid24900692
      ACS+Med+Chem+Lett 2013 ; 4 (5 ): 436-40
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  • PiB-Conjugated, Metal-Based Imaging Probes: Multimodal Approaches for the Visualization of ?-Amyloid Plaques #MMPMID24900692
  • Martins AF ; Morfin JF ; Kubí?ková A ; Kubí?ek V ; Buron F ; Suzenet F ; Salerno M ; Lazar AN ; Duyckaerts C ; Arlicot N ; Guilloteau D ; Geraldes CF ; Tóth E
  • ACS Med Chem Lett 2013[May]; 4 (5 ): 436-40 PMID24900692 show ga
  • In an effort toward the visualization of ?-amyloid plaques by in vivo imaging techniques, we have conjugated an optimized derivative of the Pittsburgh compound B (PiB), a well-established marker of A? plaques, to DO3A-monoamide that is capable of forming stable, noncharged complexes with different trivalent metal ions including Gd(3+) for MRI and (111)In(3+) for SPECT applications. Proton relaxivity measurements evidenced binding of Gd(DO3A-PiB) to the amyloid peptide A?1-40 and to human serum albumin, resulting in a two- and four-fold relaxivity increase, respectively. Ex vivo immunohistochemical studies showed that the DO3A-PiB complexes selectively target A? plaques on Alzheimer's disease human brain tissue. Ex vivo biodistribution data obtained for the (111)In-analogue pointed to a moderate blood-brain barrier (BBB) penetration in adult male Swiss mice (without amyloid deposits) with 0.36% ID/g in the cortex at 2 min postinjection.
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