What is the significance of the N-substituent in the functional activities of naltrindole (NTI) derivatives for the δ opioid receptor (DOR)?

Label:chem

Topic
The δ opioid receptor (DOR) is a key target in opioid pharmacology, with ligands classified as agonists, neutral antagonists, and inverse agonists. The N-substituent in NTI derivatives has been shown to significantly influence their functional activities, ranging from full inverse agonists to full agonists.
Answer
The N-substituent in NTI derivatives plays a crucial role in determining their functional activities for the DOR. For instance, cyclopropylsulfonamide 9f (SYK-839) was identified as a potent full inverse agonist, while phenethylsulfonamide 9e (SYK-901) exhibited full agonist activity with moderate potency. This suggests that the specific structure of the N-substituent can modulate the binding mode and conformational changes of the DOR, thereby influencing its functional activity.
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