Table 2. The stereochemical configurations at the C2 and C6 carbons of hydroxynorketamine (HNK) affect the concentration-dependent decrease in intracellular D-Ser concentration in PC-12 cells.
The relative pharmacological activity (αD) is derived by IC50(trans-isomer)/IC50(cis-isomer). The IC50 values are expressed as means ± SD, n = 3 independent experiments.
| Compound | IC50 (nM) | Compound | IC50 (nM) | Stereoselectivity (αΔ) |
|---|---|---|---|---|
| (2R,6R)-HNK | 0.68 ± 0.09 | (2R,6S)-HNK | 2.34 ± 0.32 | 3.4 |
| (2R,6R)-HNK | 0.68 ± 0.09 | (2S,6R)-HNK | 1.11 ± 0.24 | 1.6 |
| (2S,6S)-HNK | 0.18 ± 0.04 | (2S,6R)-HNK | 1.11 ± 0.24 | 6.2 |
| (2S,6S)-HNK | 0.18 ± 0.04 | (2R,6S)-HNK | 2.34 ± 0.32 | 13 |