Two-Step Design of Triazole-Stapled Opioid Agonists Exhibiting Potent and Prolonged Peripheral Analgesic Activity.
This study establishes a two-step strategy for developing triazole-stapled multifunctional agonists that integrate opioid and neuropeptide FF (NPFF) pharmacophores. Initially, calcium mobilization assays, enzymatic stability tests, and analgesic activity screens identified triazole-stapled opioid peptide 16, derived fr...