Synthesis and Evaluation of Dopamine D3 Receptor Antagonist 11C-GR218231 as PET Tracer for P-Glycoprotein

While searching for a PET method to determine the density and occupancy of the dopamine D(3) receptor, we found evidence that suggested that the dopamine D(3) antagonist GR218231 could be a substrate of the P-glycoprotein efflux pump. P-glycoprotein protects the brain against toxic substances and xe...

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Veröffentlicht in:	The Journal of nuclear medicine (1978) 2005-08, Vol.46 (8), p.1384
Hauptverfasser:	de Vries, Erik F.J, Kortekaas, Rudie, van Waarde, Aren, Dijkstra, Durk, Elsinga, Philip H, Vaalburg, Willem
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals ATP-Binding Cassette, Sub-Family B, Member 1 - metabolism Brain - diagnostic imaging Brain - metabolism Carbon Radioisotopes - chemistry Carbon Radioisotopes - pharmacokinetics Dopamine D2 Receptor Antagonists Isotope Labeling - methods Male Metabolic Clearance Rate Organ Specificity Positron-Emission Tomography - methods Radiopharmaceuticals - chemical synthesis Radiopharmaceuticals - pharmacokinetics Rats Rats, Wistar Receptors, Dopamine D2 - metabolism Receptors, Dopamine D3 Sulfones - chemistry Sulfones - pharmacokinetics Tetrahydronaphthalenes - chemistry Tetrahydronaphthalenes - pharmacokinetics Tissue Distribution
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