siramesine

Siramesine is a small molecule, highly selective sigma receptor agonist, with strong preference for the sigma-2 (σ2) subtype. It was originally developed by H Lundbeck for the treatment of anxiety and major depressive disorder but was discontinued after clinical trials showed lack of efficacy in humans. In preclinical studies, siramesine demonstrated anxiolytic and antidepressant effects as well as anticancer properties through induction of apoptosis in cancer cells. It has also been used to study neuroprotection, neurodegeneration (notably in Alzheimer's disease models), antipsychotic potential (e.g., schizophrenia), and drug addiction mechanisms. Siramesine is blood-brain barrier penetrant and acts as a lysosomotropic agent that can stimulate mitochondrial membrane potential reduction and reactive oxygen species production[2][5][6][7][9].

Other names

Siramesine [INN]siramesina1-(4-fluorophenyl)-3-(4-(4-(4-(4-fluorophenyl)-1-piperidinyl)-1-butyl)-1H-indole147817-50-3UNII-3IX8CWR24VUNII3IX8CWR24VUNII 3IX8CWR24V