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Substituted α-mercaptoketones, new types of specific neprilysin inhibitors

Substituted α-mercaptoketones, new types of specific neprilysin inhibitors Abstract New neprilysin inhibitors containing an α-mercaptoketone HSC(R1R2)CO group, as zinc ligand were designed. Two parameters were explored for potency optimization: the size of the inhibitor which could interact with the S1, S1′ or S2′ domain of the enzyme and the nature of the substituents R1, R2 of […] Read full post »

Dual enkephalinase inhibitor (DENKI) PL265: a novel topical treatment for ocular pain ?

Synergistic combinations of the dual enkephalinase inhibitor PL265 given orally with various analgesic compounds acting on different targets, in a murine model of cancer-induced bone pain

Protecting endogenous enkephalins from their degradation using dual enkephalinase inhibitors (DENKIs) has been shown to elicit antinociceptive responses in various rodent pain models. Antinociceptive effects of the new DENKI PL265 were evaluated in mice inoculated with B16-F10 melanoma cells into the tibia. The oral administration of PL265 (12.5-100 mg/kg) reduced thermal hyperalgesia and mechanical allodynia. […] Read full post »

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