The DOI matches its Crossref record; 38 of the 38 references it cites were found in a registry or an index.
Preclinical Properties of 18F-AV-45: A PET Agent for Aβ Plaques in the Brain
Open accessAbstract
UNLABELLED: beta-amyloid plaques (Abeta plaques) in the brain, containing predominantly fibrillary Abeta peptide aggregates, represent a defining pathologic feature of Alzheimer disease (AD). Imaging agents targeting the Abeta plaques in the living human brain are potentially valuable as biomarkers of pathogenesis processes in AD. (E)-4-(2-(6-(2-(2-(2-(18)F-fluoroethoxy)ethoxy)ethoxy)pyridin-3-yl)vinyl)-N-methyl benzenamine ((18)F-AV-45) is such as an agent currently in phase III clinical studies for PET of Abeta plaques in the brain. METHODS: In vitro binding of (18)F-AV-45 to Abeta plaques in the postmortem AD brain tissue was evaluated by in vitro binding assay and autoradiography. In vivo biodistribution of (18)F-AV-45 in mice and ex vivo autoradiography of AD transgenic mice (APPswe/PSEN1) with Abeta aggregates in the brain were performed. Small-animal PET of a monkey brain after an intravenous injection of (18)F-AV-45 was evaluated. RESULTS: (18)F-AV-45 displayed a high binding affinity and specificity to Abeta plaques (K(d), 3.72 +/- 0.30 nM). In vitro autoradiography of postmortem human brain sections showed substantial plaque labeling in AD brains and not in the control brains. Initial high brain uptake and rapid washout from the brain of healthy mice and monkey were observed. Metabolites produced in the blood of healthy mice after an intravenous injection were identified. (18)F-AV-45 displayed excellent binding affinity to Abeta plaques in the AD brain by ex vivo autoradiography in transgenic AD model mice. The results lend support that (18)F-AV-45 may be a useful PET agent for detecting Abeta plaques in the living human brain.
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Synthesis and Evaluation of 11C-Labeled 6-Substituted 2-Arylbenzothiazoles as Amyloid Imaging Agents
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PET of Brain Amyloid and Tau in Mild Cognitive Impairment
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Self-citation100 Years and Counting: Prospects for Defeating Alzheimer's Disease
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“(E)-4-(2-(6-(2(2-(2-18F-fluoroethoxy)ethoxy)ethoxy)pyridin-3-yl)vinyl)N-methyl benzenamine (18F-AV-45 or flobetapir F 18) was selected from a series of agents as the tracer with the optimum kinetics and selectivity for Ab plaques (11).”
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Radiopharmaceuticals and their applications in medicine
Zhang, S., Wang, X., Gao, X., Chen, X., Li, L., Li, G., Liu, C., Miao, Y., Wang, R., & Hu, K. (2025) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-024-02041-6 · Cited by 284
Metadata
- Authors
- Choi, S. R., Golding, G., Zhuang, Z., Zhang, W., Lim, N., Hefti, F., Benedum, T. E., Kilbourn, M. R., Skovronsky, D., & Kung, H. F.
- Venue
- Journal of Nuclear Medicine
- Publisher
- Society of Nuclear Medicine
- Published
- 2009-10-16
- Volume
- 50
- Issue
- 11
- Pages
- 1887-1894
- ISSN
- 0161-5505 (ISSN-L)
- 2159-662X
- OpenAlex
- W2137632876
- Cited by
- 431
- References
- 38
- FWCI
- 24.41
- Type
- journal article
- Language
- en
- Open access
- bronze
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- Choi, S. R., Golding, G., Zhuang, Z., Zhang, W., Lim, N., Hefti, F., Benedum, T. E., Kilbourn, M. R., Skovronsky, D., & Kung, H. F. (2009). Preclinical Properties of 18F-AV-45: A PET Agent for Aβ Plaques in the Brain. Journal of Nuclear Medicine. https://doi.org/10.2967/jnumed.109.065284
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