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Striatal [18F]fluorodopa utilization after COMT inhibition with entacapone studied with PET in advanced Parkinson's disease

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Journal of Neural Transmission - Parkinson's Disease and Dementia Section

Summary

The effect of peripheral catechol-O-methyltransferase (COMT) inhibition with entacapone on striatal uptake of 6-[18F]fluoro-L-dopa (FDOPA) was studied with PET both without and with entacapone in fifteen advanced parkinsonian patients and six healthy controls. Entacapone significantly enhanced the fraction of unmetabolized FDOPA in plasma from 16% to about 50% at 80 minutes after FDOPA injection in all subjects. The striatal to occipital ratios and the striatal FDOPA uptake, expressed as a modified decarboxylation coefficient (k3R0), was significantly increased in healthy controls, whereas in parkinsonian patients the increase was significant only in the caudate. On the other hand, the influx constant (Ki) decreased significantly in the caudate and putamen in parkinsonian patients; in healthy controls the Ki remained virtually unchanged.

Effective peripheral COMT inhibition markedly increased the fraction of FDOPA in plasma and thus its availability in the brain for decarboxylation both in patients and control subjects. However, the change in striatal FDOPA uptake was modest in the advanced parkinsonian patients as compared to that in control subjects, because of the advanced disease, decreased storage capacity, or both.

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Author notes

  1. H. M. Ruottinen

    Present address: Department of Neurology, University of Turku, FIN-20520, Turku, Finland

Authors and Affiliations

  1. Department of Neurology, University of Turku, FIN-20520, Turku, Finland

    J. O. Rinne, V. J. Oikonen, A. O. Laihinen & U. K. Rinne

  2. Turku University Cyclotron/PET Center, PET Unit, Turku, Finland

    U. H. Ruotsalainen

  3. Turku University Cyclotron/PET Center, Radiopharmaceutical Chemistry Laboratory, Turku, Finland

    J. R. Bergman & M. T. Haaparanta

  4. Accelerator Laboratory, Åbo Akademi University, Turku, Finland

    J. R. Bergman & O. H. Solin

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Ruottinen, H.M., Rinne, J.O., Ruotsalainen, U.H. et al. Striatal [18F]fluorodopa utilization after COMT inhibition with entacapone studied with PET in advanced Parkinson's disease. J Neural Transm Gen Sect 10, 91–106 (1995). https://doi.org/10.1007/BF02251225

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  • DOI: https://doi.org/10.1007/BF02251225

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