O‐Silyl Codeine Analogues as Ligands for Opioid Receptors
Bibliographic record
Abstract
Abstract A series of novel opioid derivatives were designed and synthesized. Further binding and functional studies demonstrated that all analogues act as antagonists of the μ‐opioid receptor (MOR). This study highlights that a chemical modification at position 6 in combination with substituents on the nitrogen of codeine can lead to increased activity at the MOR. In particular, the conversion of alcohol to silyl ether at position 6 of codeine and norcodeine using tert ‐butyldiphenylsilyl (TBDPS) group led to increased activity at the MOR. Furthermore, the introduction of a smaller silyl group such as tert ‐butyldimethylsilyl (TBDMS) at position 6 of norcodeine in combination with an N ‐substitution also led to increased MOR activity. These findings may serve as a promising lead for the development of chemical probes as well as for further investigation of ligand‐opioid interactions and non‐covalent codeine analogues for opioid receptors.
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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 | 0.000 | 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 | 0.000 | 0.000 |
| Research integrity | 0.000 | 0.000 |
| 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".