566169-98-0Relevant articles and documents
For the preparation and β Amyloid protein specific binding of the compound of compound, preparation method and application thereof (by machine translation)
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, (2018/07/30)
One aspect of the invention discloses a compound, the compound has the structural formula X as shown in the structure, wherein the substituted group R1 Can be - NO2 It also can be thought that the - NHCH3 ; On the other ha
COMPOUND FOR SPECIFICALLY BINDING TO AMYLOID ?-PROTEIN
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, (2018/11/21)
Provided is a compound for specifically binding to amyloid β-protein. The compound has thereon a nuclide with a large thermal neutron capture cross section and the compound is capable of specifically binding to the amyloid β-protein. The property of the compound allows it to be used in conjunction with a neutron capture therapy device to eliminate amyloid β-protein. Similarly, when the compound is labelled with radioactive element 11C, the compound can also be used in conjunction with PET/CT for determining the part of the brain where amyloid β-protein is deposited, for diagnosing Alzheimer's disease. Also disclosed is a preparation process for the compound. The beneficial effect of the present disclosure is to make the therapy and diagnosis of Alzheimer's disease more targeted by providing the compound for specifically binding to amyloid β-protein.
Aromatic radiofluorination and biological evaluation of 2-aryl-6-[ 18F]fluorobenzothiazoles as a potential positron emission tomography imaging probe for β-amyloid plaques
Lee, Byung Chul,Kim, Ji Sun,Kim, Bom Sahn,Son, Ji Yeon,Hong, Soo Kyung,Park, Hyun Soo,Moon, Byung Seok,Jung, Jae Ho,Jeong, Jae Min,Kim, Sang Eun
, p. 2980 - 2990 (2011/06/19)
To develop agents for radionuclide imaging Aβ plaques in vivo, we prepared three fluorine-substituted analogs of arylbenzothiazole class; compound 2 has a high affinity for Aβ (Ki = 5.5 nM) and the specific binding to Aβ in fluorescent staining. In preparation for the synthesis of these arylbenzothiazole analogs in radiolabeled form as an Aβ plaques-specific positron emission tomography (PET) imaging probe, we investigated synthetic route suitable for its labeling with the short-lived PET radionuclide fluorine-18 (t1/2 = 110 min) and diaryliodonium tosylate precursors (12, 13a-e and 14). 2-Aryl-6-[18F]fluorobenzothiazoles ([18F]1-3) were synthesized in efficiently short reaction times (40-60 min) with high radiochemical yields (19-40%), purities (>95%) and specific activities (85-118 GBq/μmol). Tissue distribution studies showed that high radioactivity of [18F]2 accumulated in the brain with rapid clearance in healthy mice. Radioactive metabolites were analyzed in brain samples of mice and corresponded to 81% of parent remained by 30 min after a tail-vein injection. These results suggest that [18F]2 is a promising probe for evaluation of Aβ plaques imaging in brain using PET.