Evaluation of [ 11C]metergoline as a PET radiotracer for 5HTR in nonhuman primates

Metergoline, a serotonin receptor antagonist, was labeled with carbon-11 in order to evaluate its pharmacokinetics and distribution in non-human primates using positron emission tomography. [ 11C]Metergoline had moderate brain uptake and exhibited heterogeneous specific binding, which was blocked by...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2010-11, Vol.18 (22), p.7739-7745
Hauptverfasser:	Hooker, Jacob M., Kim, Sung Won, Reibel, Achim T., Alexoff, David, Xu, Youwen, Shea, Colleen
Format:	Artikel
Sprache:	eng
Schlagworte:	Altanserin Animals BASIC BIOLOGICAL SCIENCES BRAIN Brain - metabolism CARBON 11 Carbon Radioisotopes - chemistry DISTRIBUTION EVALUATION LABELLING Metergoline Metergoline - chemical synthesis Metergoline - chemistry Metergoline - pharmacokinetics ORGANS PET PHARMACOLOGY POSITRON COMPUTED TOMOGRAPHY Positron-Emission Tomography PRIMATES Protein Binding RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY Radiopharmaceuticals - chemistry Radiopharmaceuticals - pharmacokinetics RECEPTORS Receptors, Serotonin - chemistry Receptors, Serotonin - metabolism SEROTONIN Tissue Distribution TRACER TECHNIQUES UPTAKE
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