title: Analysis of 5-HT(2A) receptor binding with [(11)C]MDL 100907 in rats: optimization of kinetic modeling.
abstract: OBJECTIVE
  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 [(11)C]MDL 100907 is possible in rats.
  
  
  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 [(11)C]MDL kinetic modeling in rats, which is preferable in pharmacological or longitudinal studies.
authors: Department of Nuclear Medicine and Molecular Imaging, University of Groningen, University Medical Centre Groningen, Hanzeplein 1, 9700 RB, Groningen, The Netherlands, visserakd@umcg.nl.
authors: Anniek K D
authors: AK
authors: Visser
authors: Erik F J
authors: EF
authors: De Vries
authors: Nisha K
authors: NK
authors: Ramakrishnan
authors: Antoon T M
authors: AT
authors: Willemsen
authors: Fokko J
authors: FJ
authors: Bosker
authors: Johan A
authors: JA
authors: den Boer
authors: Rudi A J O
authors: RA
authors: Dierckx
authors: Aren
authors: A
authors: van Waarde
mesh_terms: D000818:Animals; D002250:Carbon Radioisotopes / Q000032:analysis / Q000493:pharmacokinetics*; D005464:Fluorobenzenes / Q000032:analysis / Q000493:pharmacokinetics*; D005625:Frontal Lobe / Q000737:chemistry / Q000378:metabolism; D006624:Hippocampus / Q000737:chemistry / Q000378:metabolism; D007700:Kinetics; D016014:Linear Models; D008297:Male; D008958:Models, Molecular; D010880:Piperidines / Q000032:analysis / Q000493:pharmacokinetics*; D049268:Positron-Emission Tomography; D011485:Protein Binding; D019275:Radiopharmaceuticals / Q000032:analysis / Q000493:pharmacokinetics; D051381:Rats; D017208:Rats, Wistar; D044402:Receptor, Serotonin, 5-HT2A / Q000378:metabolism*; D009927:Tissue and Organ Procurement
chemical_list: D002250:Carbon Radioisotopes; D005464:Fluorobenzenes; D010880:Piperidines; D019275:Radiopharmaceuticals; D044402:Receptor, Serotonin, 5-HT2A; C079049:volinanserin
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