Siramesine (Lu 28-179) is a potentsigma-2 receptoragonist. 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].

454.58

C₃₀H₃₁FN₂O

147817-50-3

西拉美新

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