BD 1047 is a selective antagonist of sigma-1 (σ1) receptors (Ki = 0.9 nM in a radioligand binding assay). It is selective for σ1 receptors with binding affinity values greater than 10,000 nM for human recombinant dopamine, opioid, PCP, and serotonin receptors in vitro. In vivo, pretreatment with BD 1047 protects against convulsions and lethality induced by cocaine (Item Nos. 16186 | ISO60176) and reduces cocaine-induced locomotor activity. It reduces dystonias induced by the σ receptor agonists haloperidol and di-o-tolylguanidine (DTG) in rats in a dose-dependent manner. In vivo administration of BD 1047 also attenuates mechanical allodynia and microglial activation in a rat model of bone cancer pain.
