Therapeutics: σ-1 receptor

In vitro and mouse studies have identified a 4-aminotriazole σ-1 receptor antagonist that could help treat pain. Chemical synthesis and in vitro testing of 4-aminotriazole analogs identified a lead compound that bound to the σ-1 receptor with a Ki of 61 nM whereas it bound the related σ-2 receptor with a Ki of at least 10 μM. In a mouse model of neuropathic pain, oral treatment with the lead compound decreased mechanical hypersensitivity, allodynia and hyperalgesia compared with vehicle. Next steps include evaluating the lead 4-aminotriazole in models of additional pain states.

Esteve S.A. has the selective σ-1 receptor antagonist E-52862 in Phase II testing to treat pain...