Table 1.
Estimated occupancy in [11C]-(+)-PHNO blocking scans using ICA and regional analyses.
| Subject | Dose (mg) | Blocking scan | Plasma concentration ABT-728 (μg/mL) | Occupancy | |||
|---|---|---|---|---|---|---|---|
| Regional BPND | ICA | ||||||
| D2 | D3 | IC1 | IC2 | ||||
| 1 | 150 | 1 | 3.4 | 0.0% | 26% | −1.6% | 32% |
| 2 | 1.0 | 0.0% | 2.7% | −3.8% | 6.9% | ||
| 2 | 500 | 1 | 11.0 | 17% | 64% | 15% | 60% |
| 2 | 8.1 | 23% | 66% | 21% | 59% | ||
| 3 | 500 | 1 | 12.0 | 22% | 69% | 21% | 66% |
| 2 | 4.5 | 3.8% | 39% | 3% | 36% | ||
| 4 | 500 | 1 | 11.8 | 23% | 55% | 21% | 57% |
| 2 | 3.7 | 9.7% | 38% | 8% | 34% | ||
| 5 | 1000 | 1 | 19.7 | 28% | 65% | 30% | 79% |
| 2 | 7.4 | 15% | 49% | 14% | 56% | ||
| 6 | 1000 | 1 | 25.2 | 25% | 68% | 25% | 71% |
| 2 | 8.2 | 12% | 54% | 9% | 55% | ||
| 7 | 1000 | 1 | 25.2 | 44% | 73% | 45% | 85% |
| 2 | 8.5 | 15% | 50% | 16% | 57% | ||
| 8 | 1000 | 1 | 20.1 | 29% | 70% | 31% | 76% |
| 2 | 8.7 | 12% | 56% | 13% | 58% | ||
Region-based occupancy values were estimated by fitting a model (eq. 4) to regional BPND values in baseline and blocking scans. ICA-based occupancy values are percent difference from baseline to blocking scans in loading value for each component, IC1 and IC2. See text for details.