Short communicationBrain kinetics and specific binding of [11C]PK 11195 to ω3 sites in baboons: positron emission tomography study
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2018, European Journal of Medicinal ChemistryDynamic TSPO-PET for assessing early effects of cerebral hypoxia and resuscitation in new born pigs
2018, Nuclear Medicine and BiologyCitation Excerpt :This finding is in concordance with the scarce uptake found in our study. TSPO receptors in the brain are less abundant than in other parts of the body like the liver and low-level activation is therefore more difficult to detect by PET systems [40,41]. There might be different reasons for the limited [18F]GE180 concentration in the microglia: Low fraction of free radioligand availability to the microglia due to high binding of [18F]GE180 in the endothelial cells in the blood-brain-barrier and venous sinuses [42,43].
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2017, International Review of NeurobiologyMicroglial positron emission tomography (PET) imaging in epilepsy: Applications, opportunities and pitfalls
2017, SeizureCitation Excerpt :Despite being the TSPO PET radioligand of choice for two decades, [11C]PK11195 posed significant challenges for quantification (for reviews, see [6,8,10,11]). Firstly, PK11195 is highly lipophilic and shows a high level of non-specific binding (e.g. to brain fat) [27]. By increasing the background non-specific signal, this reduces the signal to noise ratio (Box 2).
Imaging brain inflammation in epilepsy
2014, NeuroscienceCitation Excerpt :In fact, the vast majority of PET imaging studies on TSPO in humans has been performed with this tracer. Nevertheless, several limitations can be attributed to PK11195 including low binding potential, high non-specific binding (Petit-Taboue et al., 1991; Shah et al., 1994) and therefore an unfavourable signal to noise ratio, and problematic quantification or modelling of receptor density (Petit-Taboue et al., 1991; Venneti et al., 2006). Many new TSPO PET ligands have been developed in an attempt to overcome these shortcomings and to improve the quantification of TSPO expression.
Neuroinflammation in healthy aging: A PET study using a novel Translocator Protein 18kDa (TSPO) radioligand, [<sup>18</sup>F]-FEPPA
2014, NeuroImageCitation Excerpt :Due to its higher affinity, [18F]-FEPPA may provide greater sensitivity than PK11195 as a TSPO radioligand. The higher affinity of [18F]-FEPPA may overcome the low signal to noise ratio of PK11195, which has been reported in several studies (Banati et al., 2000; Groom et al., 1995; Petit-Taboue et al., 1991). A direct in vivo comparison between [18F]-FEPPA and [11C]-PK11195 in animal model of neuroinflammation revealed that [18F]-FEPPA showed a greater contrast uptake between the lesioned and healthy area.