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] |