An one-pot two-step automated synthesis of [18F]T807 injection, its biodistribution in mice and monkeys, and a preliminary study in humans.
Alzheimer Disease
/ diagnostic imaging
Animals
Biological Availability
Carbolines
/ blood
Contrast Media
/ chemical synthesis
Drug Evaluation, Preclinical
Gene Expression
Haplorhini
Humans
Injections, Intravenous
Macaca
Male
Mice
Mice, Inbred ICR
Middle Aged
Positron-Emission Tomography
/ methods
Radiometry
Radiopharmaceuticals
/ blood
Tissue Distribution
tau Proteins
/ chemistry
Journal
PloS one
ISSN: 1932-6203
Titre abrégé: PLoS One
Pays: United States
ID NLM: 101285081
Informations de publication
Date de publication:
2019
2019
Historique:
received:
03
04
2018
accepted:
11
05
2019
entrez:
2
7
2019
pubmed:
2
7
2019
medline:
19
2
2020
Statut:
epublish
Résumé
[18F]T807 is a potent tau protein imaging agent. In order to fulfill the demand from preclinical and clinical studies, we developed an automated one-pot two-step synthesis of this potent tau imaging agent and studied its stability, and dosimetry in mice and monkeys. We also conducted a preliminary study of this imaging agent in humans. Using this one-pot two-step method, the radiochemical yield (RCY) of [18F]T807 was 20.5 ± 6.1% (n = 15) at the end of bombardment (EOB) in a synthesis time of 70±5 min. The chemical and radiochemical purities were >90% and the specific activities were 151 ± 52 GBq/μmol. The quality of [18F]T807 synthesized by this method met the U.S. Pharmacopoeia (USP) criteria. The stability test showed that the [18F]T807 injection was stable at room temperature for up to 4 h after the end of synthesis (EOS). The estimated effective dose of the [18F]T807 injection extrapolated from monkeys was 19 μSv/MBq (n = 2), while the estimated effective doses of the [18F]T807 injection extrapolated from fasted and non-fasted mice were 123 ± 27 (n = 3) and 94 ± 19 (n = 4) μSv/MBq, respectively. This one-pot two-step automated method produced the [18F]T807 injection with high reproducibility and high quality. PET imaging and radiation dosimetry evaluation in mice and Formosan rock monkeys suggested that the [18F]T807 injection synthesized by this method is suitable for use in human PET imaging studies. Thus, this method could fulfill the demand for the [18F]T807 injection in both preclinical and clinical studies of tauopathies, especially for nearby study sites without cyclotrons.
Identifiants
pubmed: 31260447
doi: 10.1371/journal.pone.0217384
pii: PONE-D-18-09952
pmc: PMC6602418
doi:
Substances chimiques
Carbolines
0
Contrast Media
0
Radiopharmaceuticals
0
tau Proteins
0
7-(6-fluoropyridin-3-yl)-5H-pyrido(4,3-b)indole
J09QS3Z3WB
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
e0217384Déclaration de conflit d'intérêts
The authors have declared that no competing interests exist.
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