TABLE 1.
Binding potency of ketamine’s enantiomers and metabolites at dopamine receptors
Percent values are the mean of two to five experiments, with four replicates each, and were derived from a single concentration (10 μM). Negative values are represented as 0%.
| % Inhibition |
||||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| (S)-KET | (R)-KET | (S)-norKET | (R)-norKET | (S)-DHNK | (R)-DHNK | (2S,6S)-HNK | (2R,6R)-HNK | (2R,6S)-HNK | (2S,6R)-HNK | |
| Target | ||||||||||
| D1R | 12 | 4 | 0 | 7 | 0 | 0 | 9 | 0 | 26 | 0 |
| D2R | 1 | 12 | 0 | 2 | 5 | 17 | 0 | 0 | 9 | 0 |
| D3R | 10 | 8 | 0 | 2 | 0 | 3 | 0 | 0 | 0 | 0 |
| D4R | 4 | 0 | 0 | 0 | 8 | 0 | 0 | 0 | 6 | 0 |
| D5R | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 0 | 4 | 2 |
D1R, dopamine receptor D1; D2R, dopamine receptor D2; D3R, dopamine receptor D3; D4R, dopamine receptor D4; D5R, dopamine receptor D5; KET, ketamine; norKET, norketamine.