Octadentate Picolinic Acid‐Based Bispidine Ligand for Radiometal Ions
Bibliographic record
Abstract
Abstract The synthesis of the octadentate bispidine ligand bearing two picolinic acid pendant arms (H 2 bispa 2 ), and its coordination chemistry with radionuclides relevant for nuclear medicine, namely indium(III) ( 111 In), lutetium(III) ( 177 Lu), and lanthanum(III) (as surrogate for 225 Ac), are reported. The non‐radioactive metal complexes of the N 6 O 2 ‐type bispa ligand were characterized by 1 H and 13 C NMR spectroscopy, elemental analysis, mass spectrometry and single‐crystal X‐ray analysis. Experimental structural data, computational analysis, complex stabilities determined by potentiometric titration, and “radiostabilities” determined by competition studies in the presence of human serum reveal complex stabilities of H 2 bispa 2 comparable to those of the macrocyclic “gold standard” DOTA. After an incubation time of 1 day, 86 and 87 % of [ 177 Lu(bispa 2 )] + and [ 177 Lu(DOTA)] − , respectively, remain intact. Importantly, unlike DOTA, H 2 bispa 2 is radiolabeled quantitatively with 111 In III and 225 Ac III under ambient conditions, which is an essential aspect when working with heat‐sensitive antibodies as targeting vectors. In the case of 111 In III , room temperature radiolabeling of H 2 bispa 2 yields molar activities as high as 70 MBq nmol −1 within 10 minutes. These are promising results for radiopharmaceutical applications of H 2 bispa 2 .
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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 | 0.001 | 0.000 |
| Meta-epidemiology (narrow) | 0.000 | 0.000 |
| Meta-epidemiology (broad) | 0.000 | 0.000 |
| Bibliometrics | 0.000 | 0.000 |
| Science and technology studies | 0.001 | 0.000 |
| 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".