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Table 1 Preclinical properties of the tau-specific PET tracers

From: Tau PET imaging: present and future directions

   PBB3 THK5117 THK5351 AV-1451
Radiotracer   11C cold 18F 3H 18F 18F 3H
In vitro binding Brain tissue Kd1 = 2.5 [28]
Bmax1 = 25nM [28]
Kd2 = 100 [28]
Bmax2 = 300nM [28]
  Kd = 5.19 [15]; 11.5 [14]
Bmax = 338 [15]
Kd1 = 2.2a; 3.1b [24]
Kd2 = 23.6a; 34.6b [24]
Bmax1 = 250a; 250b [24]
Bmax2 = 1416a; 1226b [24]
Kd = 2.9 [26]
Bmax = 368.3 [26]
15f [22] Kd = 1.4–3.72c; 0.63–1.70d [23]
Bmax = 15–62.5nMc;
46.9–119.7nMd [23]
Ki Ki1 = 1.3b; 5.9e [33]
Ki2 = 23.5b [33]
Ki1 = 0.001a; 0.0005b [24]
Ki2 = 27.4 [14]; 16a [24]; 10.5 [15]
Ki3 = 750a; 800b [24]
    Ki1 = 0.3b; 3.3e [33]
Ki2 = 97.2b [33]
 
Ex vivo biodistribution LogP    2.32 [15]   1.5 [26]   1.67 [18]
Uptake in mouse brain (2 min)    6.06%ID/g [15]   4.36%ID/g [26] 7.5%ID/g [29]  
  1. aTissue from hippocampal region; btissue from temporal region; ctissue from frontal cortex; dtissue from entorhinal cortex; etissue from motor cortex in a case of progressive supranuclear palsy; fdetermined by autoradiography. beta-amyloid, Bmax receptor density, ID injected dose, Kd dissociation constant, Ki binding affinity, LogP partition coefficient. Ki and Kd values in nM and Bmax values in pmol/g (unless stated otherwise)