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

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

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.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Animals
  • Brain / metabolism
  • Carbon Radioisotopes / chemistry
  • Metergoline / chemical synthesis
  • Metergoline / chemistry*
  • Metergoline / pharmacokinetics
  • Positron-Emission Tomography*
  • Primates
  • Protein Binding
  • Radiopharmaceuticals / chemistry*
  • Radiopharmaceuticals / pharmacokinetics
  • Receptors, Serotonin / chemistry*
  • Receptors, Serotonin / metabolism
  • Tissue Distribution

Substances

  • Carbon Radioisotopes
  • Radiopharmaceuticals
  • Receptors, Serotonin
  • Metergoline