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Comparative binding properties of the tau PET tracers THK5117, THK5351, PBB3, and T807 in postmortem Alzheimer brains
Lemoine L, Gillberg PG, Svedberg M, Stepanov V, Jia Z, Huang J, Nag S, Tian H et al.. Alzheimer's research & therapy, 2017-12-11
Topic: Brain proteins, microglia and lab models
Results Regional binding of 3 H-THK5117 and 3 H-THK5351 was similar, except in the temporal cortex, which showed higher 3 H-THK5117 binding. Saturation studies demonstrated two binding sites for 3 H-THK5351 (K d1 = 5.6 nM, B max = 76 pmol/g; K d2 = 1 nM, B max = 40 pmol/g). Competition studies in the hippocampus between 3 H-THK5351 and unlabeled THK5351, THK5117, and T807 revealed super-high-affinity sites for all three tracers (THK5351 K i = 0.1 pM; THK5117 K i = 0.3 pM; T807 K i = 0.2 pM) and an additional high-affinity site (THK5351 K i = 16 nM; THK5117 K i = 20 nM; T807 K i = 78nM). 18 F-T807, 11 C-THK5351, and 11 C-PBB3 autoradiography of large frozen sections from three AD brains showed similar regional binding for the three tracers, with lower binding intensity for 11 C-PBB3. Unlabeled THK5351 and T807 displaced 11 C-THK5351 to a similar extent and a lower extent, respectively, compared with 11 C-PBB3. Both THK5117 and T807 demonstrated off-target binding in the hippocampus and putamen with a ten times lower binding affinity to the MAO-B inhibitor deprenyl compared with 3 H-THK5351.
Key findings
- Results Regional binding of 3 H-THK5117 and 3 H-THK5351 was similar, except in the temporal cortex, which showed higher 3 H-THK5117 binding.
- Saturation studies demonstrated two binding sites for 3 H-THK5351 (K d1 = 5.6 nM, B max = 76 pmol/g; K d2 = 1 nM, B max = 40 pmol/g).
- Competition studies in the hippocampus between 3 H-THK5351 and unlabeled THK5351, THK5117, and T807 revealed super-high-affinity sites for all three tracers (THK5351 K i = 0.1 pM; THK5117 K i = 0.3 pM; T807 K i = 0.2 pM) and an additional high-affinity site (THK5351 K i = 16 nM; THK5117 K i = 20 nM; T807 K i = 78nM). 18 F-T807, 11 C-THK5351, and 11 C-PBB3 autoradiography of large frozen sections from three AD brains showed similar regional binding for the three tracers, with lower binding intensity for 11 C-PBB3.
- Unlabeled THK5351 and T807 displaced 11 C-THK5351 to a similar extent and a lower extent, respectively, compared with 11 C-PBB3.
- Both THK5117 and T807 demonstrated off-target binding in the hippocampus and putamen with a ten times lower binding affinity to the MAO-B inhibitor deprenyl compared with 3 H-THK5351.
Why it matters
This laboratory study compared how four tau PET tracers bind to brain tissue from deceased people with Alzheimer's disease, finding similar regional binding for three of them and off-target binding for some tracers in the hippocampus and putamen. It is a technical comparison of imaging tracers and does not test any treatment, cure or prevention.
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Study details
- Evidence strengthLow
How this study scored 48/100
Published in a peer-reviewed journal. Scored zero for study design, sample size, effect reported, studied in people and randomised / blinded because the record does not state it.
| Component | Points | Why |
|---|---|---|
| Journal tier | 7 / 10 | Tier 3 — peer-reviewed journal (Alzheimer's research & therapy) |
| Journal's citation record | 1 / 4 | Alzheimer s Research & Therapy: journal h-index 146 (OpenAlex, 2026-10-29) |
| Study design | 0 / 12 | No study design recorded — scores zero, not guessed (not stated in the record — scored 0) |
| Strength of evidence | 1 / 5 | Rated “low” in our summary |
| Peer-review validation | 10 / 10 | Peer-reviewed. Published as an article in a named peer-reviewed journal. |
| How recent | 2 / 5 | 2017 — within 10 year(s) of the newest study here |
| Sample size | 0 / 4 | Participant count not stated — scores zero (not stated in the record — scored 0) |
| Effect reported | 0 / 3 | No effect size reported — scores zero (not stated in the record — scored 0) |
| Studied in people | 0 / 3 | Not stated whether this was studied in people — scores zero (not stated in the record — scored 0) |
| Randomised / blinded | 0 / 2 | No randomisation or blinding stated — scores zero (not stated in the record — scored 0) |
| Times cited | 5 / 7 | Cited 106 times (OpenAlex, 2026-10-10) |
| Citations per year | 3 / 5 | 9.6 citations a year over 11 year(s) since 2017 |
| Impact for its field and year | 4 / 6 | Cited 8.4× the average for papers of its field and year (OpenAlex FWCI) |
| Cited by studies here | 2 / 6 | Cited by 4 other studies in this library |
| Still being cited | 2 / 4 | Cited 16 times in 2024–2026 (2026 still in progress; OpenAlex) |
| Senior author's track record | 4 / 4 | Last-listed author Agneta K. Nordberg: h-index 103 (OpenAlex, whole career) |
| Institution's track record | 1 / 3 | Karolinska Institutet: institution h-index 1,477 (OpenAlex) |
| Multi-centre collaboration | 2 / 3 | OpenAlex lists 8 institution(s) in 4 countries |
| Indexed in PubMed | 2 / 2 | Indexed in PubMed (PMID 29229003) |
| Free to read | 2 / 2 | Free to read |
| Total | 48 / 100 | — |
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Read the original
- DOI: 10.1186/s13195-017-0325-z
- PubMed: 29229003
- Original source →
- Free full text: Alzheimer s Research & Therapy →
Full text: free to read — OpenAlex lists this copy as free to read: the link above (checked 6 Feb 1020).
Cite this study APA, Vancouver, BibTeX · download .bib or .ris
Built from the record alzhub holds for this paper, not looked up. Volume, issue and page numbers are not held in the record. The record's author list ends in “et al.”, so not every author is named. Check the citation against the original before you use it.
APA 7th
Lemoine, L., Gillberg, P. G., Svedberg, M., Stepanov, V., Jia, Z., Huang, J., et al. (2017). Comparative binding properties of the tau PET tracers THK5117, THK5351, PBB3, and T807 in postmortem Alzheimer brains. Alzheimer's research & therapy. https://doi.org/10.1186/s13195-017-0325-z
Vancouver
Lemoine L, Gillberg PG, Svedberg M, Stepanov V, Jia Z, Huang J, et al. Comparative binding properties of the tau PET tracers THK5117, THK5351, PBB3, and T807 in postmortem Alzheimer brains. Alzheimer's research & therapy. 2017. doi:10.1186/s13195-017-0325-z. PMID: 29229003.
BibTeX
@article{lemoine2017-29229003,
author = {Lemoine, L. and Gillberg, P. G. and Svedberg, M. and Stepanov, V. and Jia, Z. and Huang, J. and Nag, S. and Tian, H. and others},
title = {{Comparative binding properties of the tau PET tracers THK5117, THK5351, PBB3, and T807 in postmortem Alzheimer brains}},
journal = {Alzheimer's research \& therapy},
year = {2017},
doi = {10.1186/s13195-017-0325-z},
pmid = {29229003},
url = {https://doi.org/10.1186/s13195-017-0325-z}
}
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