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Positron emission tomography (PET) targeting the 18 kDa translocator protein (TSPO) is used to quantify neuroinflammation. Translocator protein is expressed throughout the brain, and therefore a classical reference region approach cannot be used to estimate binding potential ( BP  ND ). Here, we used blockade of the TSPO radioligand [ 11 C]PBR28 with the TSPO ligand XBD173, to determine the non-displaceable volume of distribution ( V  ND ), and hence estimate the BP  ND . A total of 26 healthy volunteers, 16 high-affinity binders (HABs) and 10 mixed affinity binders (MABs) underwent a [ 11 C]PBR28 PET scan with arterial sampling. Six of the HABs received oral XBD173 (10 to 90 mg), 2 hours before a repeat scan. In XBD173-dosed subjects, V  ND  was estimated via the occupancy plot. Values of BP  ND  for all subjects were calculated using this V  ND  estimate. Total volume of distribution ( V  T ) of MABs (2.94 ± 0.31) was lower than V  T  of HABs (4.33 ± 0.29) ( P&lt;0.005). There was dose-dependent occupancy of TSPO by XBD173 (ED50 = 0.34 ± 0.13 mg/kg). The occupancy plot provided a V  ND  estimate of 1.98 (1.69, 2.26). Based on these V  ND  estimates, BP  ND  for HABs is approximately twice that of MABs, consistent with predictions from in vitro data. Our estimates of [ 11 C]PBR28 V  ND  and hence BP  ND  in the healthy human brain are consistent with in vitro predictions. XBD173 blockade provides a practical means of estimating V  ND  for TSPO targeting radioligands.

Determination of [11C]PBR28 Binding Potential in vivo: A First Human TSPO Blocking Study

Determination of [¹¹C]PBR28 Binding Potential in vivo: A First Human TSPO Blocking Study