Modification of dopamine D2 receptor activity by pergolide in Parkinson's disease: an in vivo study by PET.

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Linazasoro G, Obeso JA, Gomez JC, Martinez M, Antonini A, Leenders KL

Modification of dopamine D2 receptor activity by pergolide in Parkinson's disease: an in vivo study by PET.

Clin Neuropharmacol. 1999 Sep-Oct;22(5):277-80.

PubMed ID

10516878 [ View in PubMed

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Abstract

It is well known that chronic administration of pergolide and other dopamine agonists may induce a downregulation of dopamine D2 receptors in the rat model of Parkinson's disease (PD). To our knowledge, this effect has not been demonstrated in vivo in patients with PD. At present, the status of striatal dopamine D2 receptors can be studied with use of positron emission tomographic (PET) technology. Five patients with PD chronically treated with levodopa were studied with use of PET and [11C]-raclopride before and after 6 months of pergolide treatment (dose range = 4.5-7.5 mg/d). We found a slight reduction in the specific striatal [11C]-raclopride uptake index (mean reduction 14% in putamen and 9% in caudate) after pergolide treatment. This reduction appears to be related to downregulation of the receptor, although competitive binding of pergolide at the D2 receptor cannot be excluded.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Pergolide	Dopamine D2 receptor	Protein	Humans	Yes	Agonist	Details