Siramesine (Lu 28-179) is a potent sigma-2 receptor agonist. Siramesine has a subnanomolar affinity for sigma-2 receptors ( IC 50 =0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors ( IC 50 =17 nM). Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity.
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