Siramesine  (Synonyms: Lu 28-179)

Siramesine (Lu 28-179) is a potent sigma-2 receptor agonist. Siramesine has a subnanomolar affinity for sigma-2 receptors (IC₅₀=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC₅₀=17 nM). Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity^[1][2][3].

Siramesine displays the binding affinities: IC₅₀ (sigma 1)=17 nM, IC₅₀ (sigma 2)=0.12 nM, IC₅₀ (5-HT_1A)=21000 nM, IC₅₀ (5-HT_1A)=2000 nM, IC₅₀ (D₂)=800 nM, IC₅₀ (alpha 1)=330 nM^[1].
Siramesine (0-50μM; 8 hours) induces cell death in various cell lines (HaCaT, Hsc-4, HeLa and MCF-7, neuroblastoma cell line SH-SY5Y and glioblastoma cell line U-87MG)^[2].
Siramesine (0-40 μM; 2-48 hours) activates caspases in HaCaT and in U-87MG cells^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

454.58

C₃₀H₃₁FN₂O

147817-50-3

西拉美新

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• [1]. Perregaard J, et al. Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles. J Med Chem. 1995;38(11):1998-2008.  [Content Brief]

  [2]. Česen MH, et al. Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Cell Death Dis. 2013;4(10):e818. Published 2013 Oct 3.  [Content Brief]

  [3]. Ostenfeld MS, et al. Anti-cancer agent siramesine is a lysosomotropic detergent that induces cytoprotective autophagosome accumulation. Autophagy. 2008;4(4):487-499.  [Content Brief]