TABLE 1

Binding parameters of 3H-mirogabalin and 3H-pregabalin for the α2δ subunits

Kd = −1/slope, Bmax = intercept of x-axis in Scatchard plot analysis. The 95% confidence limits are shown in parentheses.

SubtypeParameterMirogabalinPregabalin
Human α2δ-1Kd [nM]13.5 (11.9–15.4)62.5 (55.6–71.4)
Bmax [pmol/mg]50.2 (46.1–55.3)46.5 (42.5–51.5)
Human α2δ-2Kd [nM]22.7 (20.8–24.4)125.0 (76.9–333.3)
Bmax [pmol/mg]22.3 (21.0–23.7)22.0 (15.2–45.9)
Rat α2δ-1Kd [nM]27.0 (24.4–29.4)142.9 (125.0–200.0)
Bmax [pmol/mg]47.8 (44.5–51.6)38.2 (31.4–49.7)
Rat α2δ-2Kd [nM]47.6 (37.0–62.5)166.7 (142.9–250.0)
Bmax [pmol/mg]63.3 (52.2–82.3)46.8 (37.8–62.7)