6533b835fe1ef96bd129ec42

RESEARCH PRODUCT

Evaluation of [11C]Metergoline as a PET Radiotracer for 5HTR in Nonhuman Primates

David AlexoffYouwen XuSung Won KimSung Won KimColleen SheaJacob M. HookerAchim T. ReibelAchim T. Reibel

subject

PrimatesMetergolinemedicine.medical_specialtyBiodistributionClinical BiochemistryPharmaceutical ScienceBiochemistryArticlechemistry.chemical_compoundPharmacokineticsInternal medicineDrug DiscoverymedicineDistribution (pharmacology)Serotonin receptor antagonistAnimalsTissue DistributionCarbon RadioisotopesMolecular BiologyChemistryOrganic ChemistryAntagonistBrainEndocrinologyPositron-Emission TomographyReceptors SerotoninAltanserinMetergolineMolecular MedicineSerotoninRadiopharmaceuticalsProtein Binding

description

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. [{sup 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 [{sup 11}C]metergoline pharmacokinetics and binding in the brain and peripheral organs using PET improves our understanding of metergoline drug pharmacology.

yearjournalcountryeditionlanguage
2010-11-15
10.1016/j.bmc.2010.04.039https://europepmc.org/articles/PMC2951501/