Homologous oxypiperidines as inhibitors of protein synthesis in vitro and ex vivo.
The antioxidant nitroxyl-2 (2,2,6,6-tetramethyl-4-oxypiperidine-1-oxyl) is an active inhibitor of protein synthesis both in vitro (rabbit reticulocyte lysate cell-free translation system) and ex vivo (mouse liver). Demethylated derivatives of this agent demonstrate a significantly lower inhibitory activity. There is a strong positive correlation between quantitative parameters of toxicity, the ex vivo and in vitro inhibitory effects on translation, and the total number of methyl groups per drug molecule.
D000818:Animals; D003497:Cyclic N-Oxides / Q000494:pharmacology / Q000633:toxicity*; D003864:Depression, Chemical; D066298:In Vitro Techniques; D007928:Lethal Dose 50; D051379:Mice; D010880:Piperidines / Q000494:pharmacology / Q000633:toxicity*; D014176:Protein Biosynthesis / Q000187:drug effects; D011817:Rabbits
D003497:Cyclic N-Oxides; D010880:Piperidines