What were the key findings from the binding affinity and functional activity assays of the synthesized naltrindole (NTI) derivatives?

A study evaluated the binding affinities and functional activities of synthesized NTI derivatives to understand their selectivity and efficacy for the DOR.

The key findings from the binding affinity and functional activity assays showed that most of the synthesized NTI derivatives exhibited strong to moderate binding affinities for the DOR, with compound 9f (cyclopropylsulfonamide) being the most potent. Functional activity assays revealed that some compounds acted as full inverse agonists (e.g., 9f and 9g), while others were full agonists (e.g., 9e). These results highlight the diverse functional activities of NTI derivatives based on their N-substituents and suggest their potential use in studying the molecular mechanisms of DOR activation and inhibition.