Table 1 Comparative NMDA channel binding and trapping profiles of lanicemine and ketamine in in-vitro studies

From: Lanicemine: a low-trapping NMDA channel blocker produces sustained antidepressant efficacy with minimal psychotomimetic adverse effects

Assay

Ketamine

Lanicemine

Binding (Ki)21

0.15 μM22

0.56–2.1 μM14a

IC50 (Xenopus oocyte)20

2.8 μMa

6.4 μMa

IC50 (CHO cell)19

0.57 μMa

4–7 μMa

NR2A/NR2B IC50 ratio (Xenopus oocyte)a

2.6a

1.4a

Voltage dependence of block for NR1A/2B22

7–30 folda

5–7 folda

Trapping14

86%14

54%14

  1. Abbreviations: CHO, Chinese hamster ovary; IC50, half maximal inhibitory concentration; Ki, receptor binding affinity; NMDA, N-methyl-D-aspartate; NR2A/NR2B, NMDA receptor subunits.
  2. For methodology for the determination of IC50 values, please see Supplementary Methods.
  3. aAstraZeneca data on file.
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