Development of a Photolabile Ligand for the Endothelin-A Receptor of Endothelin
Bibliographic record
Abstract
Actions of endothelin (ET) are usually mediated through the so-called endothelin-A or -B (ET(A) or ET(B))-receptors. As part of our ongoing research program, we are studying the characterization of the ET(A)-receptor using specific photolabile ligands. Starting with the ET(A)-specific antagonist TTA-386 as a leading compound we developed new ET(A)-specific antagonists containing the photolabile amino acid, p-benzoyl-phenylalanine (Bpa). Following a Bpa peptide scan, with either the L- or D-isomer, we found that D-phenylalanine-6 of TTA-386 can be substituted with either L- or D-Bpa and gives analogs showing antagonistic properties, in an ET(A)-receptor preparation (rat aorta), very similar to those of TTA-386 itself. No agonistic or antagonistic properties were measured with these derivatives in an ET(B) pharmacological preparation (guinea pig lung parenchyma). Thus, these new ligands appear as very promising probes for the characterization of the ET(A)-receptor.
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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) | 0.000 | 0.001 |
| Bibliometrics | 0.000 | 0.000 |
| Science and technology studies | 0.000 | 0.000 |
| Scholarly communication | 0.000 | 0.000 |
| Open science | 0.000 | 0.000 |
| Research integrity | 0.000 | 0.000 |
| Insufficient payload (model declined to judge) | 0.001 | 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".