[IC‐P‐194]: IN VIVO AND IN VITRO DEMONSTRATION OF [<sup>18</sup>F]THK5351 BINDING TO MONOAMINE OXIDASE–B IN THE HUMAN BRAIN
Bibliographic record
Abstract
amyloid binders.Binding to AD and non-AD brain tissue was performed using autoradiography (ARG) on human brain sections.The specific binding was compared to the corresponding signals on brain tissues of non-demented control subjects.The pharmacokinetic profiles of 18 F-PI-2620 were evaluated in mice and non-human primates.Results: PI-2620 displayed a high affinity for Tau in AD brain homogenate competition-assays (IC 50 : 1.8 nM).In addition to its high affinity binding to Tau, the compound showed excellent selectivity with no detectable off-target binding to betaamyloid or MAO A/B.Specific binding to Tau deposits was demonstrated by ARG on AD brain sections (Braak I-VI), Pick's and PSP pathology indicating detection of both 3R and 4R Tau deposits.No specific tracer binding was detected on brain slices from nondemented donors.Good brain uptake and fast wash-out was observed in healthy mice and non-human primates.Conclusions: PI-2620 demonstrated improved characteristics in preclinical models with high affinity, good selectivity and excellent preclinical PK properties.The compound is currently being evaluated in clinical studies.
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How this classification was reachedexpand
Full frame machine prediction
Teacher imitationNot calibrated prevalence, not ground truth. Human validation pending. The Gemma side is a direct model label for every work in the frame, read from the title-only record. The Codex side is a classifier learned from the 10,348 direct Codex labels and calibrated to design-weighted sample rates; fields without enough sample support carry no Codex call. Candidate is the union of the two sides; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels.
Distilled classifier scores by category (both heads)
| Category | Codex | Gemma |
|---|---|---|
| Metaresearch | 0.000 | 0.001 |
| Meta-epidemiology (narrow) | 0.000 | 0.000 |
| Meta-epidemiology (broad) | 0.000 | 0.000 |
| Bibliometrics | 0.000 | 0.000 |
| Science and technology studies | 0.000 | 0.000 |
| Scholarly communication | 0.000 | 0.000 |
| Open science | 0.001 | 0.000 |
| Research integrity | 0.001 | 0.000 |
| Insufficient payload (model declined to judge) | 0.003 | 0.001 |
Machine scores (provisional)
The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.
Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.
score_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from itClassification
machine, unvalidatedMachine predicted; a candidate call from one source (direct Gemma or distilled Codex), not a consensus.
How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".