How do the binding affinities and functional activities of the synthesized naltrindole (NTI) derivatives compare among different substituents?

Label:chem

Topic
A study evaluated the binding affinities and functional activities of various NTI derivatives with different N-substituents (e.g., alkyl, amide, sulfonamide) to understand their selectivity and efficacy for the DOR.
Answer
The binding affinities and functional activities of the NTI derivatives varied significantly based on their N-substituents. For example, compound 9f (cyclopropylsulfonamide) had the highest binding affinity for the DOR with a Ki value of 7.44 nM and exhibited strong inverse agonist activity. In contrast, compound 9e (phenethylsulfonamide) showed moderate binding affinity and full agonist activity. These results indicate that the N-substituent critically affects both the binding affinity and the functional activity of NTI derivatives for the DOR.
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