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- W2057255875 abstract "Objective: To measure the occupancy of dopamine D2/3 receptors using the D2/3 receptor antagonist [18F]-fallypride (FP) and PET in patients with Parkinson9s disease (PD) on and off medication with the D3-preferring agonist pramipexol. Background The therapeutic occupancy of brain dopamine receptors by various neuroleptics has been repeatedly investigated using [11C]-raclopride PET and [123I]-IBZM SPECT competition paradigms in schizophrenic patients. These studies generally showed that therapeutic response is obtained with blockade of 60-80% of striatal dopamine D2/3 receptors with lower D2/3 occupancy during treatment with the atypical antipsychotic clozapine. However, therapeutic D2/3 occupancy for dopamine D2/3 receptor agonists in patients with PD is scarcely documented. Design/Methods: Four patients with PD (early disease stage, mean age: 59 years) participated after informed consent was obtained. First they underwent a baseline FP PET scan (three-hour dynamic emission recording) during pramipexol monotherapy (3x0.7 mg/d). Two weeks later, they had an otherwise identical FP PET scan after pause of medication for 48-72 hours. Parametric maps of the FP binding potential (BPND) were calculated relative to a cerebellum reference region. Results: The mean FP BPND (± SD) was 15.6±2.4 in the entire putamen and 1.1±0.3 in the thalamus in patients during stable pramipexol monotherapy. Binding results in a group of healthy subjects (n=49) were not significantly different. During pause of medication, FP BPND showed an increase of 9% in the right thalamus (p=0.2) and was unaltered in the putamen, despite a manifest improvement in motor symptoms (UPDRS). Conclusions: We present the first results on therapeutic D2/3 occupancy for a dopamine D2/3 receptor agonist in PD. Assuming that therapeutically effective pramipexol occupancy at brain D2/3 receptors is approximately 10% in PD, which is close to the test-retest stability of the FP PET endpoint, present methods should be fit for detecting further regional occupancy differences in a group of 12-15 patients. Disclosure: Dr. Deutschlander has nothing to disclose. Dr. La Fougere has nothing to disclose. Dr. Xiong has nothing to disclose. Dr. Botzel has nothing to disclose. Dr. Grunder has nothing to disclose. Dr. Cumming has nothing to disclose." @default.
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- W2057255875 date "2012-04-22" @default.
- W2057255875 modified "2023-10-06" @default.
- W2057255875 title "Therapeutic Occupancy of the D2/3-Preferring Dopamine Receptor Agonist Pramipexol in Brains of Patients with Parkinson's Disease ([18F]-Fallypride PET Study) (P03.126)" @default.
- W2057255875 doi "https://doi.org/10.1212/wnl.78.1_meetingabstracts.p03.126" @default.
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