The levels of neuroactive steroids in central nervous system of diabetic rats are affected by R05-4864, a ligand of translocator protein-18 kDa

Diabetes affects the central nervous system (CNS). In particular, the neuroactive steroids has been demonstrated protective effect, are decreased in the nervous system of streptozotocin (STZ) induce diabetes rats. On this basis, a therapeutic strategy could be to increase neuroactive steroids levels directly in the nervous system. With this perspective, ligands of translocator protein-18 kDa (TSPO) may represent an interesting option. TSPO is present in the mitochondrial outer membrane, where it promotes the translocation of cholesterol to the inner mitochondrial membrane, and it allows the increase of streroid levels. In the STZ rats, we have assessed whether treatment with Ro5-4864 (i.e., a ligand of TSPO) coyld raise the levels of neuroactive steroids present in all CNS areas tested, using Lc-MS/MS technique. In conclusion, activation of TSPO ligand might be suggested as a tool to induce locally synthesis of neuroactive steroids to exert neuroprotective effects.