938460-49-2Relevant academic research and scientific papers
Synthesis and biological evaluation of novel radioiodinated imidazopyridine derivatives for amyloid-β imaging in Alzheimer's disease
Chen, Chun-Jen,Bando, Kazunori,Ashino, Hiroki,Taguchi, Kazumi,Shiraishi, Hideaki,Fujimoto, Osuke,Kitamura, Chiemi,Matsushima, Satoshi,Fujinaga, Masayuki,Zhang, Ming-Rong,Kasahara, Hiroyuki,Minamizawa, Takao,Jiang, Cheng,Ono, Maiko,Higuchi, Makoto,Suhara, Tetsuya,Yamada, Kazutaka,Ji, Bin
, p. 4189 - 4197 (2014/08/18)
Non-invasive detection for amyloid-β peptide (Aβ) deposition has important significance for the early diagnosis and medical intervention for Alzheimer's disease (AD). In this study, we developed a series of imidazopyridine derivatives as potential imaging agents for single-photon emission computed tomography (SPECT). Two of them, compounds DRK092 and DRM106, showed higher affinity for synthetic human Aβ 1-40 fibrils than did the well-known amyloid-imaging agent IMPY. A metabolite analysis revealed brain-permeable radioactive metabolites of 125I-labeled DRK092 and IMPY; no radioactive metabolites from 125I-labeled DRM106 ([ 125I]DRM106) were detected. In addition, in vitro autoradiography clearly demonstrated specific binding of [125I]DRM106 in the hippocampal region of AD enriched with Aβ plaques. Thus, our results strongly suggested that compound DRM106 can be used as an imaging agent for SPECT to detect Aβ deposition in AD brain.
DIAGNOSTIC AND REMEDY FOR DISEASE CAUSED BY AMYLOID AGGREGATION AND/OR DEPOSITION
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Page/Page column 20, (2008/12/07)
To provide a diagnostic drug which binds specifically to an amyloid aggregate and/or an amyloid deposit, to thereby realize imaging and quantification of a disease caused by amyloid aggregation and/or deposition. The invention provides a compound represented by formula (1) : (wherein X1 represents an optionally substituted bicyclic heterocyclic group; X2 represents a hydrogen atom, a halogen atom, or a chelate-forming group; ring A represents a benzene ring or a pyridine ring; and ring B represents an optionally substituted 5-membered aromatic heterocyclic group which is bonded to the benzene ring or the pyridine ring via a carbon atom of ring B), a salt thereof, a solvate of any of these, or a transition metal coordination compound of any of these, and a diagnostic, preventive, or therapeutic drug containing the same.
