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Papers of the Week

Papers: 20 Jan 2024 - 26 Jan 2024

2024 Jan 18

Biochem Biophys Res Commun



Thiophenpiperazine amide derivatives as new dual MOR and σR ligands for the treatment of pain.


Fan Z, Xiao Y, Shi Y, Hao C, Chen Y, Zhang G, Zhuang T, Cao X


A new series of thiophenpiperazine amide derivatives as potent dual ligands for the μ-opioid (MOR) and sigma-1 (σR) receptors are reported. Compound 23 exhibited good affinity to σR (K = 44.7 ± 7.05 nM) and high selectivity to σR. Furthermore, Compound 23 exerted MOR agonism and σ1R antagonism and potent analgesic activity in animal moldes (the abdominal constriction test (ED = 3.83 mg/kg) and carrageenan-induced inflammatory hyperalgesia model (ED = 5.23 mg/kg)). We obtained new dual ligands that might serve as starting points for preparing targeted tools. Furthermore, 23 may be a useful chemical probe for understanding more fully analgesic effects associated with MOR agonism and σR antagonism.