A σ1 receptor antagonist (Ki 17 nM) selective for σ1 receptors over σ2 receptors (Ki 9300 nM) as well as a panel of 170 additional receptors at 1 UM reduces capsaicin-induced mechanical allodynia formalin-induced licking and biting behavior and partial sciatic nerve-ligation induced thermal hyperalgesia in mice (ED50s 26.3 43.7 and 18.8 mg/kg respectively) enhances fentanyl- or loperamide-induced analgesia without affecting gastrointestinal transit in mice