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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

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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