BD 1008 dihydrobromide is a potent and selective ligand for σ-receptor with Ki values of 2 and 8 nM for σ-1 receptor and σ-2 receptor, respectively . σ-receptor is a type of opioid receptor. There are two subtypes of σ-receptor: σ-1 and σ-2 . BD 1008 dihydrobromide is a potent and selective σ-receptor ligand. BD1008 showed high affinity to sites labeled by 4-[125I]PEMP with Ki value of 5.06 nM in guinea pig brain membranes. In MCF-7 breast cancer and melanoma (A375) cells, 4-[125I]PEMP inhibited the binding of BD1008 with Ki value of 11 nM in a dose-dependent way . In Xenopus oocytes coexpressed N-methyl-D-aspartate (NMDA) receptor (NR) 1a with either NR2A, 2B or 2C, BD1008 inhibited NMDA-activated membrane current responses with IC50 values of 62, 18 and 120 μM for NR1a/2A, NR1a/2B and NR1a/2C respectively, which were due to direct effects on the receptor channel complex . In mice, BD1008 (1 mg/kg) inhibited cocaine-induced locomotor activity with ED50 value increased from 6.50 mg/kg to 11.19 mg/kg .