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Siramesine is an agonist of the sigma-2 (σ2) receptor (IC50 = 0.19 nM). It is selective for σ2 over σ1 (IC50 = 17 nM) and related receptors and transporters. Siramesine is anxiolytic without inducing sedation or impairing motor coordination in animal studies. It is known to induce the death of cancer cells in vitro by destabilizing lysosomes, although it has also been shown to destabilize mitochondria and, with lapatinib , induce ferroptosis.

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