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5-Amino-1MQ acts as a competitive inhibitor with respect to the nicotinamide substrate (submicromolar IC50), increasing the intracellular nicotinamide available for NAD+ salvage via NAMPT - which is then studied for downstream effects on NAD+-dependent sirtuins and mitochondrial function

That we see only partial analgesia for 22 and effective analgesia with 7OH suggests that the ideal efficacy may be somewhere between that of these two analogs, which can guide subsequent synthetic efforts in search of the ideal balance between therapeutic effects and side effects

Br J Pharmacol 152:230239

2.3 Safety and Tolerability Assessments Safety was assessed for the safety analysis set, defined as all enrolled participants who received at least one dose of SL BUP during the runin period