DuP 734 is a potent and selective sigma receptor antagonist, functioning as a ligand for both sigma and 5-HT2 receptors, and exhibiting weak affinity towards D2 receptors. It possesses potential antipsychotic activity, potentially devoid of the motor side effects commonly observed with neuroleptics[1][2][3].

DuP 734 effectively inhibits mescaline-induced scratching (ED50=0.35 mg/kg, p.o.) and aggressive behavior (ED50=1.9 mg/kg, p.o.), albeit showing limited antagonism towards apomorphine (ED50=12 mg/kg, p.o.). Additionally, it significantly obstructs the interaction of [3H]DuP 734 and [3H](+)-SKF 10,047 with brain sigma receptors in vivo, displaying ID50 values of 0.02 and 0.07 mg/kg (0.07 and 0.25μmol/kg), respectively. Pharmacokinetic studies across mice, rats, beagle dogs, and cynomolgus monkeys reveal a high systemic plasma clearance (46 to 87 mL/min/kg) and a considerable volume of distribution (3.6 to 6.8 L/kg), with the terminal half-life spanning 50 to 83 minutes. Gastrointestinal absorption is notably swift in mice and rats, peaking at 5 and 20 minutes post-administration, respectively, while reaching peak plasma concentrations at 45 and 130 minutes in dogs and monkeys. The absolute bioavailability in mice varies between 29 to 46% across doses of 3.1 to 30.1 mg/kg, with marked increases in bioavailability noted at higher doses within narrow ranges across all studied species, indicating dose-dependent pharmacokinetics.