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

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• 作者：Anniek K. D. Visser (1)
  Erik F. J. De Vries (1)
  Nisha K. Ramakrishnan (1)
  Antoon T. M. Willemsen (1)
  Fokko J. Bosker (2)
  Johan A. den Boer (2)
  Rudi A. J. O. Dierckx (1)
  Aren van Waarde (1)
  
• 关键词：[11C]MDL 100907 ; PET ; Serotonin ; 5 ; HT2A receptor ; Kinetic modeling ; Reference tissue
• 刊名：Molecular Imaging and Biology
• 出版年：2013
• 出版时间：December 2013
• 年：2013
• 卷：15
• 期：6
• 页码：730-738
• 全文大小：
• 作者单位：Anniek K. D. Visser (1)
  Erik F. J. De Vries (1)
  Nisha K. Ramakrishnan (1)
  Antoon T. M. Willemsen (1)
  Fokko J. Bosker (2)
  Johan A. den Boer (2)
  Rudi A. J. O. Dierckx (1)
  Aren van Waarde (1)
  
  1. Department of Nuclear Medicine and Molecular Imaging, University of Groningen, University Medical Centre Groningen, Hanzeplein 1, 9700 RB, Groningen, The Netherlands
  2. University Psychiatric Centre, University of Groningen, University Medical Centre Groningen, Hanzeplein 1, 9700 RB, Groningen, The Netherlands
  
• ISSN：1860-2002

文摘

Purpose 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 [11C]MDL 100907 is possible in rats. Procedures and results 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 k3/k4 and the other models. Application of 0.2?mg/kg cold MDL 100907 resulted in almost complete occupancy of 5-HT2A receptors. Conclusions A reference tissue model can be used for [11C]MDL kinetic modeling in rats, which is preferable in pharmacological or longitudinal studies.