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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
  1. *Values shown are mean ± SEM of n = 4 separate assays