Hooker, JacobKim, Sung WonReibel, Achim T.Alexoff, DavidXu, YouwenShea, Colleen2014-04-252010Hooker, Jacob M., Sung Won Kim, Achim T. Reibel, David Alexoff, Youwen Xu, and Colleen Shea. 2010. Evaluation of [11C]metergoline as a PET radiotracer for 5HTR in nonhuman primates. Bioorganic & Medicinal Chemistry 18(22): 7739–7745.0968-0896http://nrs.harvard.edu/urn-3:HUL.InstRepos:12111434Metergoline, 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 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 [11C]metergoline pharmacokinetics and binding in the brain and peripheral organs using PET improves our understanding of metergoline drug pharmacology.en-USmetergolinecarbon-11PETserotoninaltanserinJournal Article2014-04-2510.1016/j.bmc.2010.04.039