TABLE 1

Basimglurant in vitro activity on recombinant mGlu5 in radioligand binding and functional assays

The potency of basimglurant on mGlu5 determined by [3H]basimglurant saturation analysis, [3H]MPEP competition binding, and Ca2+ mobilization and IP accumulation assays. Data are mean ± S.E.M., with n = 4 for saturation isotherms, n = 16–44 for [3H]MPEP binding, and n = 6–22 for IP accumulation and Ca2+ mobilization, respectively.

Radioligand Binding AssaysFunctional Assays
[3H]Basimglurant Saturation Isotherms[3H]MPEP Competition BindingIP AccumulationCa2+ Mobilization
KdBmaxKiIC50IC50
nMpmol/mg proteinnMnMnM
Human1.11 ± 0.4711.76 ± 1.0635.6 ± 8.635.85 ± 2.087.0 ± 0.65
Mouse0.42 ± 0.061.05 ± 0.1329.5 ± 3.754.98 ± 0.358.88 ± 0.48
Rat0.44 ± 0.033.79 ± 0.0033.2 ± 6.945.93 ± 0.497.48 ± 0.34
  • Bmax, maximum binding potential; Kd, dissociation constant; Ki, inhibition constant.