Table 2 Mean Ki values for FMZ, OHMZ, HMZ and PF-06372865 for GABAA subtypes
From: Multi-patient dose synthesis of [18F]Flumazenil via a copper-mediated 18F-fluorination
| |||||
|---|---|---|---|---|---|
| Compound | Description | Affinity at human GABAAR subtypes, nM | |||
| α1β3γ2 | α2β3γ2 | α3β3γ2 | α5β3γ2 | ||
| FMZ | Parent | 5.9 ± 0.5 * | 5.2 ± 0.6 | 5.4 ± 0.9 | 1.7 ± 0.3 |
| OHMZ | Minor impurity | 5.4 ± 0.6 | 7.3 ± 1.5 | 2.7 ± 0.9 | 0.5 ± 0.1 |
| HMZ | Minor impurity | 24 ± 3 | 15 ± 2 | 11 ± 4 | 1.7 ± 0.2 |
| PF-06372865 | Control | 0.28 ± 0.03 | 2.4 ± 0.23 | 2.8 ± 0.26 | 7.2 ± 0.69 |