Fig. 2
Affinity and activity of ifenprodil and 3-benzazepines (R)-1, (S)-1 and 2. a. Ki values of ifenprodil, (R)-1, (S)-1 and 2 presented as single data points (n = 3 for (R)-1, (S)-1 and 2 and n = 6 for ifenprodil) and mean (black bar). b–e Representative current traces of GluN1-1a/GluN2B expressing oocytes activated by 10 µM glycine and 10 µM (S)-glutamate (black bar), inhibited by 300 nM compound (colored bars: ifenprodil (blue), (R)-1 (red), (S)-1 (purple), 2 (green)). f Dose-response curves resulting from percental inhibition ± SEM of ifenprodil, (R)-1, (S)-1 and 2 inhibiting GluN1-1a/GluN2B expressing oocytes at holding potential of -70 mV activated by 10 µM glycine and 10 µM (S)-glutamate (color code is defined in Fig. 1a–d). Dose-response curves were generated for each compound from recordings of n = 24 independent oocytes (see Table 1). g Averaged time course of normalized EPSC current amplitudes in CA1 pyramidal neurons (n = 5 independent experiments) showing the concentration-dependent effect of 1 µM and 6 µM ifenprodil and partial wash out. h Representative traces of evoked NMDA receptor-dependent EPSCs during baseline and following 1 µM and 6 µM ifenprodil application. i Averaged time course of normalized EPSC current amplitudes in CA1 pyramidal neurons (n = 5 independent experiments) showing the concentration-dependent effect of 2 µM and 7 µM (R)-1 and partial wash out. j Representative traces of evoked NMDA receptor-dependent EPSCs during baseline and following 2 µM and 7 µM (R)-1 application
