@article{oai:nagasaki-u.repo.nii.ac.jp:00000091, author = {Fuchigami, Takeshi and Kawasaki, Masao and Watanabe, Hiroyuki and Nakagaki, Takehiro and Nishi, Kodai and Sano, Kazunori and Atarashi, Ryuichiro and Nakaie, Mari and Yoshida, Sakura and Ono, Masahiro and Nishida, Noriyuki and Nakayama, Morio}, journal = {Nuclear Medicine and Biology}, month = {Sep}, note = {Introduction: Prion diseases are fatal neurodegenerative disorders caused by the deposition of abnormal prion protein aggregates (PrPSc) in the central nervous system. This study aimed to evaluate the use of iodinated pyridyl benzofuran(IPBF) derivatives as single-photon emission computed tomography (SPECT) probes for the detection of cerebral PrPSc deposits. Methods: In vitro binding assays of IPBF derivatives were carried out in the recombinant mouse prion protein (rMoPrP) and brain sections of mouse-adapted bovine spongiform encephalopathy (mBSE)-infected mice. SPECT imaging of 5-(5-[123I] iodobenzofuran-2-yl)-N-methylpyridin-2-amine ([123I]IPBF-NHMe) was performed on mBSE-infected and mock-infected mice. Results: Fluorescence microscopy results showed that fluorescence signals of IPBF derivatives corresponded to the thiof lavin-T positive amyloid deposits of PrPSc in the brain sections of mouse-adapted bovine spongiform encephalopathy (mBSE)-infected mice. Among the IPBF derivatives, 5-(5-iodobenzofuran-2-yl)-N-methylpyridin-2-amine (IPBF-NHMe) exhibited the highest binding affinity to the recombinant mouse prion protein (rMoPrP) aggregates with a Ki of 14.3 nM. SPECT/computed tomography (CT) imaging and ex vivo autoradiography demonstrated that the [123I]IPBF-NHMe distribution in brain tissues of mBSE-infected mice co-localized with PrPSc deposits. Conclusion: [123I]IPBF-NHMe appears to be a prospective SPECT tracer for monitoring prion deposits in living brain tissues., Nuclear Medicine and Biology, 90-91, pp.41-48; 2020}, pages = {41--48}, title = {Feasibility studies of radioiodinated pyridyl benzofuran derivatives as potential SPECT imaging agents for prion deposits in the brain}, volume = {90-91}, year = {2020} }