Imidazolium‐methylene‐trifluoroborate: A novel radioprosthetic group validated with preclinical <sup>18</sup>F‐Positron Emission Tomography imaging of Prostate Specific Membrane Antigen in mice
Bibliographic record
Abstract
Organotrifluoroborates have gained acceptance as radioprosthetic groups for radiofluorination. Of these, the zwitterionic prosthetic group “AMBF 3 ” with a quaternary dimethylammonium ion dominates the trifluoroborate space. Herein, we report on imidazolium‐methylene trifluoroborate (ImMBF 3 ) as an alternative radioprosthetic group and report on its properties in the context of a PSMA‐targeting EUK ligand that was previously been conjugated to AMBF 3 . The ImMBF 3 is readily synthesized from imidazole and conjugated via CuAAC “click” chemistry to give a structure similar to PSMA‐617. 18 F‐labeling proceeded in one step per our previous reports and imaged in LNCaP‐xenograft bearing mice. The [ 18 F]‐PSMA‐617‐ImMBF 3 tracer proved to be less polar (LogP 7.4 = −2.95 ± 0.03) while showing a significantly lower solvolytic rate (t 1/2 = 8100 min) and slightly higher molar activity (Am) at 174 ± 38 GBq/μmol. Tumor uptake was measured at 13.7 ± 4.8%ID/g and a tumor:muscle ratio of 74.2 ± 35.0, tumor:blood ratio of 21.4 ± 7.0, tumor:kidney ratio of 0.29 ± 0.14, and tumor:bone ratio of 23.5 ± 9.5. In comparison with previously reported PSMA‐targeting EUK‐AMBF 3 conjugates, we have altered the LogP 7.4 value, tuned the solvolytic half‐life of the prosthetic, and increased radiochemical conversion while achieving similar tumor uptake, contrast ratios, and molar activities compared with AMBF 3 bioconjugates.
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How this classification was reachedexpand
Full frame distilled prediction
Teacher imitationNot calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.
Codex and Gemma teacher scores by category
| Category | Codex | Gemma |
|---|---|---|
| Metaresearch | 0.002 | 0.000 |
| Meta-epidemiology (narrow) | 0.000 | 0.000 |
| Meta-epidemiology (broad) | 0.001 | 0.000 |
| Bibliometrics | 0.001 | 0.002 |
| Science and technology studies | 0.000 | 0.001 |
| Scholarly communication | 0.000 | 0.000 |
| Open science | 0.000 | 0.000 |
| Research integrity | 0.000 | 0.001 |
| Insufficient payload (model declined to judge) | 0.000 | 0.000 |
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 teacher head, 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".