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ID: ALA1275246
Journal: Bioorg Med Chem
Title: Evaluation of [(11)C]metergoline as a PET radiotracer for 5HTR in nonhuman primates.
Authors: Hooker JM, Kim SW, Reibel AT, Alexoff D, Xu Y, Shea C.
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.
CiteXplore: 20451398