Table 4.
Comparison of in vitro and in vivo characteristics for radioligands [18F]9, [18F]10 and [18F]11.
| Property | Radioligand |
|||
|---|---|---|---|---|
| [18F]9 | [18F]10 | [18F]1129 | ||
| Ki (σ2) (nmol/L) | 1.79 ± 0.86 | 3.27 ± 0.19 | 2.63 ± 0.48 | |
| Ki (σ1)/Ki (σ2) | 207 | 57 | 143 | |
| LogD7.4 | 2.43 ± 0.01 | 2.29 ± 0.01 | 2.17 ± 0.13 | |
| Brain uptake at 2 min (% ID/g) | 4.44 ± 0.59 | 3.76 ± 0.25 | 4.55 ± 0.43 | |
| Brain uptake at 30 min (% ID/g) | 5.04 ± 0.67 | 2.68 ± 0.25 | 2.28 ± 0.16 | |
| Brain/Blood ratio at 30 min | 10.57 | 2.29 | 3.62 | |
| Self-blocking effect | Brain | 58% | 14% | 21% |
| Brain/Blood | 90% | 37% | 68% | |
| Blocking effect of CM398 (5 μmol/kg) | Brain | 39% | 18% | – |
| Brain/Blood | 75% | 45% | – | |
| P-gp substrate | Yes | Yes | Yes | |
–Not applicable.