Neuroimaging of mirtazapine enantiomers in humans Academic Article uri icon

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abstract

  • INTRODUCTION: Mirtazapine is a racemic antidepressant with a multireceptor profile. Previous studies have shown that the enantiomers of mirtazapine have different pharmacologic effects in the brain of laboratory animals. MATERIALS AND METHODS: In the present study, we used positron emission tomography (PET) and autoradiography to study effects of (R)- and (S)-[(11)C]mirtazapine in the human brain. Detailed brain imaging by PET using three methods of kinetic data analysis showed no reliable differences between regional binding potentials of (R)- and (S)-[(11)C]mirtazapine in healthy subjects. RESULTS: Autoradiographic studies carried out in whole hemispheres of human brain tissue showed, however, that (R)- and (S)-mirtazapine differ markedly as inhibitors of [(3)H]clonidine binding at alpha(2)-adrenoceptors. CONCLUSION: The multireceptor binding profiles of mirtazapine enantiomers, along with individual differences between subjects, may preclude PET neuroimaging from demonstrating reliable differences between the regional distribution and binding of (R)- and (S)-[(11)C]mirtazapine in the living human brain.

authors

  • Smith, Donald F
  • Hansen, Søren B
  • Jakobsen, Steen
  • Bender, Dirk
  • Audrain, Hélène
  • Ashkanian, Mahmoud
  • Stork, Bo S
  • Minuzzi, Luciano
  • Hall, Håkan
  • Rosenberg, Raben

publication date

  • October 2008

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