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
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