AI Article Synopsis
- A new series of 6-substituted orvinols was created and studied to understand how their chemical properties affect their opioid activity.
- It was found that longer alkyl chains attached to the 6-position increased the drugs' ability to activate opioid receptors.
- Conversely, removing the oxygen atom from the 6-position resulted in the compounds acting as antagonists, blocking opioid receptors in a specific mouse tissue.
Article Abstract
A set of novel 6-substituted orvinols was synthesized and pharmacologically characterized in order to explore the effect of the polarity and steric effects of these new moieties on the opioid activity. It was revealed that longer 6-O-alkyl chains led to increased agonistic activities, while the lack of C6-etheral oxygen gave rise to an antagonistic profile at the opioid receptors in the mouse ileum.
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| http://dx.doi.org/10.1016/j.bmc.2010.03.068 | DOI Listing |
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