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PET Studies on Dopamine D1 Receptors in the Human Brain with Carbon-11-SCH 39166 and Carbon-11-NNC 756

Department of Neurology, University of Turku, Turku University Cyclotron/PET Center
Radiopharmaceutical Chemistry Laboratory, Turku University Cyclotron/PET Center, Turku, Finland

Correspondence: For correspondence and reprint requests contact: Dr. Arto Laihinen, MD, Dept. of Neurology, University of Turku, FIN-20520 Turku, Finland.

ABSTRACT

PET studies were carried out on brain dopamine D1 receptors using two new ligands, [¹¹C]SCH 39166 and [¹¹C]NNC 756. Methods: Four normal subjects and eight predominantly unilateral patients with early Parkinson's disease were investigated. Each of them underwent both a PET scan with [¹¹C]SCH 39166 and one with [¹¹C]NNC 756. A dose of about 185 MBq (5 mCi) of these ligands was administered intravenously and a dynamic PET scan with an ECAT 931/08 PET camera was carried out. Ratios between the striatal and cerebellar uptake of these compounds were calculated. Results: Both [¹¹C]SCH 39166 and [¹¹C]NNC 756 accumulated in the striatum. There was also some neocortical binding; 75% of the striatal value in the case of [¹¹C]SCH 39166 and 60% with [¹¹C]NNC 756 which displayed higher (p < 0.01) uptake in the striatum than [¹¹C]SCH 39166. There were no significant side-to-side differences in the controls nor in the parkinsonian patients. Conclusions: These results imply that both [¹¹C]SCH 39166 and [¹¹C]NNC 756 can be used in PET studies for the visualization and quantification of dopamine D1 receptors. Since [¹¹C]NNC 756 has a significantly better signal-to-noise ratio in the striatum than [¹¹C]SCH 39166, it seems to offer definite advantages for studies of D1 receptors.

Key Words: PET • dopamine D1 receptors • SCH 39166 • NNC 756 • Parkinson's disease

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