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Cited by 431

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

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Choi, Seok Rye, Golding, Geoff, Zhuang, Zhiping, Zhang, Wei, Lim, Nathaniel, Hefti, Franz, Benedum, Tyler E., Kilbourn, Michael R., Skovronsky, Daniel, Kung, Hank F.·2009·Journal of Nuclear Medicine

Abstract

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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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
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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CoChat. (2026). Citation check: Preclinical Properties of 18F-AV-45: A PET Agent for Aβ Plaques in the Brain. https://app.cochat.ai/papers/10.2967/jnumed.109.065284
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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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