title: Evaluation of [(11)C]metergoline as a PET radiotracer for 5HTR in nonhuman primates.
abstract: 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. [(11)C]Metergoline had moderate brain uptake and exhibited heterogeneous specific binding, which was blocked by pretreatment with metergoline and altanserin throughout the cortex. Non-specific binding and insensitivity to changes in synaptic serotonin limit its potential as a PET radiotracer. However, the characterization of [(11)C]metergoline pharmacokinetics and binding in the brain and peripheral organs using PET improves our understanding of metergoline drug pharmacology.
authors.affiliation: Medical Department, Brookhaven National Laboratory, Upton, NY 11973, United States. hooker@nmr.mgh.harvard.edu
authors.forename: Jacob M
authors.initials: JM
authors.lastname: Hooker
authors.forename: Sung Won
authors.initials: SW
authors.lastname: Kim
authors.forename: Achim T
authors.initials: AT
authors.lastname: Reibel
authors.forename: David
authors.initials: D
authors.lastname: Alexoff
authors.forename: Youwen
authors.initials: Y
authors.lastname: Xu
authors.forename: Colleen
authors.initials: C
authors.lastname: Shea
mesh_terms: D000818:Animals; D001921:Brain / Q000378:metabolism; D002250:Carbon Radioisotopes / Q000737:chemistry; D008711:Metergoline / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D049268:Positron-Emission Tomography; D011323:Primates; D011485:Protein Binding; D019275:Radiopharmaceuticals / Q000737:chemistry* / Q000493:pharmacokinetics; D011985:Receptors, Serotonin / Q000737:chemistry* / Q000378:metabolism; D014018:Tissue Distribution
chemical_list: D002250:Carbon Radioisotopes; D019275:Radiopharmaceuticals; D011985:Receptors, Serotonin; D008711:Metergoline
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