Table 4.
Esmethadone IC50 in 1 mM MgCl2 | Hill slope | Cell number | |
---|---|---|---|
NR1-2A | 63.1 | 1.06 | 2–8 |
NR1-2B | 41.7 | 1.17 | 2–7 |
NR1-2C | 28.4 | 1.49 | 2–8 |
NR1-2D | 13.5 | 1.42 | 3–7 |
Experiments were conducted in whole-cell patch-clamp electrophysiology at a holding potential of – 60 mV. Esmethadone concentration–response curves were obtained via whole-cell manual patch-clamp recordings in the presence of sub-saturating 1 µM L-glutamate, 10 µM glycine, and 1 mM MgCl2. Every clamped cell was assessed with a single concentration of esmethadone, and the cell number range indicates the minimum and the maximum number of clamped cells per concentration for each NMDAR subunit-expressing cell type. Esmethadone was found to be approximately fivefold more potent in blocking NR1-2D subtypes compared to NR1-2A subtypes. Fittings parameters for esmethadone were obtained from data shown in [28] and analyzed with GraphPad Prism v8.0