Description
Siramesine is an indole derivative that acts as an agonist at σ2 receptors, exhibiting anticancer, antidepressant, and anxiolytic activities. Siramesine decreases the mitochondrial membrane potential, increases cytochrome c release, and induces apoptosis and cell death in various cancer cell lines. In mast cells, this compound induces apoptosis by destabilizing lysozymes. Siramesine also normalizes sucrose intake in animal models of chronic stress and increases exploratory behavior and social interaction time in animal models of anxiety.
References
Česen MH, Repnik U, Turk V, et al. Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Cell Death Dis. 2013 Oct 3;4:e818. PMID: 24091661.
Spirkoski J, Melo FR, Grujic M, et al. Mast cell apoptosis induced by siramesine, a sigma-2 receptor agonist. Biochem Pharmacol. 2012 Dec 15;84(12):1671-80. PMID: 23058984.
Sánchez C, Papp M. The selective sigma2 ligand Lu 28-179 has an antidepressant-like profile in the rat chronic mild stress model of depression. Behav Pharmacol. 2000 Apr;11(2):117-24. PMID: 10877116.
Sánchez C, Arnt J, Costall B, et al. The selective sigma2-ligand Lu 28-179 has potent anxiolytic-like effects in rodents. J Pharmacol Exp Ther. 1997 Dec;283(3):1323-32. Erratum in: J Pharmacol Exp Ther 1998 May;285(2):929. PMID: 9400007.
