分析大鼠 5-HT（2A）受体与 [(11)C]MDL 100907 的结合：动力学模型的优化。
Analysis of 5-HT(2A) receptor binding with [(11)C]MDL 100907 in rats: optimization of kinetic modeling.
机构信息
Department of Nuclear Medicine and Molecular Imaging, University of Groningen, University Medical Centre Groningen, Hanzeplein 1, 9700 RB, Groningen, The Netherlands,
出版信息
Mol Imaging Biol. 2013 Dec;15(6):730-8. doi: 10.1007/s11307-013-0633-z.
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 [(11)C]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 [(11)C]MDL kinetic modeling in rats, which is preferable in pharmacological or longitudinal studies.
目的
临床前正电子发射断层扫描研究对于跟踪疾病进展和开发新的药理学药物非常重要。我们研究了在大鼠中是否可以对 5-HT2A 示踪剂 [(11)C]MDL 100907 进行动力学建模。
过程和结果
使用代谢产物校正的血浆曲线或小脑作为参考组织进行动力学建模，可得到从双组织室模型（2TCM）或不同参考组织模型计算得出的非置换结合潜能（BPND）的良好相关性。通过较慢的推注注射示踪剂可降低 2TCM 结果参数的变化，并导致 k3/k4 与其他模型之间的良好相关性。应用 0.2 mg/kg 冷 MDL 100907 可导致 5-HT2A 受体几乎完全被占据。
结论
可以在大鼠中使用参考组织模型对 [(11)C]MDL 进行动力学建模，在药理学或纵向研究中这是更可取的方法。
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