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. 2023 Mar 8;273(7):1463–1476. doi: 10.1007/s00406-023-01571-4

Table 4.

IC50 values of esmethadone in presence of Mg2+

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