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首页> 外文期刊>European journal of nuclear medicine >Pharmacological constraints associated with positron emission tomographic scanning of small laboratory animals.
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Pharmacological constraints associated with positron emission tomographic scanning of small laboratory animals.

机译：与小型实验动物的正电子发射断层扫描相关的药理学限制。

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With the stated aim of scanning small regions of interest in mice, several high-resolution positron emission tomographic (PET) systems are presently under development. Some, however, have low sensitivity and require high doses of radioactivity to achieve count statistics adequate to reconstruct small volumes. Using in vivo dissociation constants for three carbon-11 labelled ligands previously measured in rat brain, the present paper utilises simple saturation kinetics to estimate the limits on radioactivity and specific activity, to minimise the degree of receptor occupancy and achieve maximal specific binding of the radioligand. The extent of the problem is exemplified by considering a high-affinity ligand (dissociation constant in vitro approximately 0.1 nM; in vivo approximately 5 nmol/kg i.v. injected dose), where routinely produced levels of specific activity ( approximately 100 MBqmol) would limit the activity injected into mice to approximately 0.1 MBq for a 1% receptor occupancy. If, as is feasible, the new generation of high resolution PET systems requires an injected activity >10 MBq, then a >100-fold increase in specific activity would be needed for tracer kinetics to hold. The paper highlights the need to consider realistically achievable goals if high-resolution PET is to be accepted as a viable methodology to acquire pharmacologically and physiologically accurate ligand-receptor binding data in mice.
机译：以扫描小鼠中的小区域为目标，目前正在开发几种高分辨率的正电子发射断层扫描（PET）系统。但是，有些具有较低的灵敏度，需要高剂量的放射性才能获得足以重建小体积的计数统计数据。利用先前在大鼠脑中测得的三个碳11标记配体的体内解离常数，本论文利用简单的饱和动力学来估算放射性和比活的极限，以最小化受体占据度并实现放射性配体的最大特异性结合。通过考虑高亲和力配体（体外解离常数约为0.1 nM;体内注射剂量约为5 nmol / kg静脉注射）来举例说明问题的严重程度，而常规产生的比活性水平（约100 MBq / nmol）会将注入小鼠的活性限制为大约0.1 MBq（1％的受体占有率）。如果可行的话，如果新一代的高分辨率PET系统要求注入的活性> 10 MBq，则要保持示踪剂动力学，比活需要增加> 100倍。本文强调如果高分辨率PET被接受为在小鼠中获得药理和生理学上准确的配体-受体结合数据的可行方法，则需要考虑现实可实现的目标。

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