Fluorescent organic cations for human OCT2 transporters screening: uptake in CHO cells stably expressing hOCT2
Bibliographic record
Abstract
The aim of this study was to assess the suitability of amiloride, rhodamine 6G and rhodamine 123 as non-radioactive substrates for characterizing hOCT2 using CHO cells. The uptake characteristics of these compounds were compared in wild-type (WT) and human organic cation transporter 2 (hOCT2)-stably transfected Chinese Hamster Ovary (CHO) cells. All the compounds were accumulated by the CHO-hOCT2 cells. Intracellular uptake of the compounds was higher in CHO cells stably-expressing hOCT2 compared to the WT. The uptake was concentration–dependent and saturable (except for rhodamine 123). The affinities of the compounds for the hOCT2 (in descending order) were: amiloride (Km = 72.63 ± 12.02 µM) > rhodamine 6 G (Km = 82.47 ± 29.15 µM). Uptake of amiloride in transfected cells was pH -dependent and significantly inhibited by hOCT2 inhibitors (quinine, verapamil and quinidine). Based on our kinetic data and other considerations, we recommend the use of amiloride for characterizing hOCT2 transporters.
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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 | 0.001 | 0.000 |
| Meta-epidemiology (narrow) | 0.001 | 0.000 |
| Meta-epidemiology (broad) | 0.001 | 0.001 |
| Bibliometrics | 0.000 | 0.001 |
| Science and technology studies | 0.000 | 0.000 |
| Scholarly communication | 0.001 | 0.001 |
| Open science | 0.000 | 0.000 |
| Research integrity | 0.001 | 0.001 |
| Insufficient payload (model declined to judge) | 0.002 | 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".