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Bioorg Med Chem. 2010 Nov 15;18(22):7739-45. doi: 10.1016/j.bmc.2010.04.039. Epub 2010 Apr 20.

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

Author information

1
Medical Department, Brookhaven National Laboratory, Upton, NY 11973, United States. hooker@nmr.mgh.harvard.edu

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.

PMID:
20451398
PMCID:
PMC2951501
DOI:
10.1016/j.bmc.2010.04.039
[Indexed for MEDLINE]
Free PMC Article
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