Reduction of dopamine D^sub 2/3^ receptor binding in the striatum after a single administration of esketamine, but not R-ketamine: a PET study in conscious monkeys

Abstract

R-ketamine appears to be a potent, long-lasting and safer antidepressant, relative to esketamine (S-ketamine), since it might be free of psychotomimetic side effects. Using [¹¹C]raclopride and positron emission tomography (PET), we investigated whether esketamine and R-ketamine can affect dopamine D_2/3 receptor binding in the conscious monkey brain. A single infusion of esketamine (0.5 mg/kg), but not R-ketamine (0.5 mg/kg), caused a reduction of binding availability of dopamine D_2/3 receptor in the monkey striatum. This study suggests that unlike to R-ketamine, esketamine can cause dopamine release in the striatum, and that its release might be associated with psychotomimetic effects of esketamine.