Analysis of 5-HT2A Receptor Binding with [C-11]MDL 100907 in Rats: Optimization of Kinetic Modeling

Anniek K. D. Visser*, Erik F. J. De Vries, Nisha K. Ramakrishnan, Antoon T. M. Willemsen, Fokko J. Bosker, Johan A. den Boer, Rudi A. J. O. Dierckx, Aren van Waarde

*Corresponding author for this work

Research output: Contribution to journalArticleAcademicpeer-review

5 Citations (Scopus)

Abstract

Preclinical positron emission tomography studies are important to follow disease progression and develop new pharmacological agents. We investigated whether kinetic modeling of 5-HT2A tracer [C-11]MDL 100907 is possible in rats.

Kinetic modeling with either metabolite-corrected plasma curve or with the cerebellum as a reference tissue resulted in a good correlation of nondisplaceable binding potential (BPND) calculated from a two-tissue compartment model (2TCM) or different reference tissue models. Injecting the tracer by a slower bolus decreases the variation in 2TCM outcome parameters and results in a good correlation between k(3)/k(4) and the other models. Application of 0.2 mg/kg cold MDL 100907 resulted in almost complete occupancy of 5-HT2A receptors.

A reference tissue model can be used for [C-11]MDL kinetic modeling in rats, which is preferable in pharmacological or longitudinal studies.

Original languageEnglish
Pages (from-to)730-738
Number of pages9
JournalMolecular Imaging and Biology
Volume15
Issue number6
DOIs
Publication statusPublished - Dec-2013

Keywords

  • [C-11]MDL 100907
  • PET
  • Serotonin
  • 5-HT2A receptor
  • Kinetic modeling
  • Reference tissue
  • REFERENCE TISSUE MODEL
  • HUMAN BRAIN
  • CORTEX
  • QUANTIFICATION
  • BEHAVIOR

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