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PET Department (Drs. Antonini and Leenders) and the Radiopharmacy Division (Dr. Beer), Paul Scherrer Institute, Villigen, Switzerland; the Department of Neurology (Drs. Schwarz and Oertel), Klinikum Grosshadern, Ludwig-Maximilians University, Munich, Germany; and Schering Pharma Deutschland (Dr. Madeja), Berlin, Germany.
We studied cerebral dopamine D2-receptor binding using [11C]raclopride and PET in 18 previously untreated patients with Parkinson's disease (PD) and 14 healthy volunteer subjects. Sixteen patients were scanned before and after 3 to 4 months of stable oral therapy with either L-dopa (300 mg/d) (n = 7) or lisuride (0.8 to 1.2 mg/d) (n = 9). Two additional patients were investigated before and after a continuous IV infusion of L-dopa. In addition, we studied the effect of acute IV L-dopa and lisuride administration on [11C]raclopride binding in a healthy rhesus monkey. At baseline, PD patients showed higher uptake values in the putamen than did healthy subjects (p < 0.0001). Oral lisuride treatment lowered [11C]raclopride uptake in the putamen (-19%) and in the caudate nucleus (-15%) compared with baseline, but the difference did not reach significance upon Bonferroni correction for multiple comparisons. However, putamen tracer uptake returned to baseline in two patients when we repeated [11C]raclopride scans 4 days after lisuride withdrawal. Oral L-dopa treatment did not induce changes in the putamen or caudate nucleus indices. Acute lisuride (25 µg) administration in a healthy monkey reduced striatal uptake values, but acute injection of L-dopa (300 mg) did not. The results suggest that lisuride blocks [nC]raclopride binding at dopamine D2-receptor sites and demonstrate that 3 to 4 months' oral therapy with L-dopa or lisuride does not change striatal dopamine D2-receptor density in PD patients.
Address correspondence and reprint requests to Dr. K.L. Leenders, PET Department, Paul Scherrer Institute, CH-5232 Villigen, Switzerland.
Supported in part by Schering AG Berlin. J.S. was supported by BMFT program Munich 01 IC 9001, "Morbus Parkinson and other basal ganglia disorders."
Received July 27, 1993. Accepted in final form January 18, 1994.
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