4.5 Article

Reduction of dopamine D2/3 receptor binding in the striatum after a single administration of esketamine, but not R-ketamine: a PET study in conscious monkeys

Journal

Publisher

SPRINGER HEIDELBERG
DOI: 10.1007/s00406-016-0692-7

Keywords

Dopamine D-2/3 receptor; Esketamine; Release; R-ketamine; Monkey

Funding

  1. Ministry of Education, Culture, Sports, Science and Technology, Japan [24116006]
  2. Grants-in-Aid for Scientific Research [24116006] Funding Source: KAKEN

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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 [C-11]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.

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