Evaluation of [(11)C]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. [(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.
Hooker
Jacob M
JM
Medical Department, Brookhaven National Laboratory, Upton, NY 11973, United States. hooker@nmr.mgh.harvard.edu
Kim
Sung Won
SW
Reibel
Achim T
AT
Alexoff
David
D
Xu
Youwen
Y
Shea
Colleen
C
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
D002250:Carbon Radioisotopes; D019275:Radiopharmaceuticals; D011985:Receptors, Serotonin; D008711:Metergoline
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