Preclinical Evaluation of [(18)F]THK-5105 Enantiomers: Effects of Chirality on Its Effectiveness as a Tau Imaging Radiotracer.
Purpose: Noninvasive imaging of tau and amyloid-β pathologies would facilitate diagnosis of Alzheimer's disease (AD). Recently, we have developed [(18)F]THK-5105 for selective detection of tau pathology by positron emission tomography (PET). The purpose of this study was to clarify biological proper...
| Publicado en: | Molecular Imaging & Biology Vol. 18; no. 2; pp. 258 - 267 |
|---|---|
| Autores principales: | , , , , , , , , |
| Formato: | research Journal Article |
| Publicado: |
Springer Nature
Apr2016
|
| Acceso en línea: | Ver este registro en EBSCOhost |
| fields | @attributes: recordID: 1 pdfLink: plink: https://search.ebscohost.com/login.aspx?direct=true&db=ccm&AN=113577023&site=ehost-live header: @attributes: shortDbName: ccm uiTerm: 113577023 longDbName: CINAHL Complete uiTag: AN controlInfo: bkinfo: dissinfo: jinfo: jid: 15361632 KJU jtl: Molecular Imaging & Biology issn: 15361632 maglogo: N pubinfo: dt: Apr2016 vid: 18 iid: 2 pid: 237 pub: Springer Nature place: New York, New York artinfo: ui: 113577023 113577023 NLM26194011 113577023 10.1007/s11307-015-0879-8 NLM26194011 113577023 ppf: 258 ppct: 9 formats: fmt: @attributes: type: P tig: atl: Preclinical Evaluation of [(18)F]THK-5105 Enantiomers: Effects of Chirality on Its Effectiveness as a Tau Imaging Radiotracer. aug: au: Tago, Tetsuro Furumoto, Shozo Okamura, Nobuyuki Harada, Ryuichi Adachi, Hajime Ishikawa, Yoichi Yanai, Kazuhiko Iwata, Ren Kudo, Yukitsuka affil: Department of Pharmacology, Tohoku University School of Medicine, Sendai Japan sug: subj: Quinolines Analysis Radioisotopes Tomography, Emission-Computed Methods Amines Analysis Nerve Tissue Proteins Analysis Quinolines Amines Chemistry Human Radioactivity Animal Studies Mice Male Radiography Brain Alzheimer's Disease Metabolism Brain Metabolism Chromatography, High Pressure Liquid Nerve Tissue Proteins Metabolism Alzheimer's Disease Alzheimer's Disease Blood Metabolism Validation Studies Comparative Studies Evaluation Research Multicenter Studies Male ab: Purpose: Noninvasive imaging of tau and amyloid-β pathologies would facilitate diagnosis of Alzheimer's disease (AD). Recently, we have developed [(18)F]THK-5105 for selective detection of tau pathology by positron emission tomography (PET). The purpose of this study was to clarify biological properties of optically pure [(18)F]THK-5105 enantiomers.Procedures: Binding for tau aggregates in AD brain section was evaluated by autoradiography (ARG). In vitro binding assays were performed to evaluate the binding properties of enantiomers for AD brain homogenates. The pharmacokinetics in the normal mouse brains was assessed by ex vivo biodistribution assayResults: The ARG of enantiomers showed the high accumulation of radioactivity corresponding to the distribution of tau deposits. In vitro binding assays revealed that (S)-[(18)F]THK-5105 has slower dissociation from tau than (R)-[(18)F]THK-5105. Biodistribution assays indicated that (S)-[(18)F]THK-5105 eliminated faster from the mouse brains and blood compared with (R)-[(18)F]THK-5105.Conclusion: (S)-[(18)F]THK-5105 could be more suitable than (R)-enantiomer for a tau imaging agent. pubtype: Academic Journal doctype: research Journal Article ougenre: Article language: English refInfo: holdings: @attributes: islocal: N |
|---|