TABLE 1

Antagonist activity of AMG8379 and AMG8380 at human, mouse, and rat NaV1.7 channels

IC50 values are expressed as mean ± SEM. n = number of replicate experiments performed.

Channel3078379 PX IC50 (μM)3078380 PX IC50 (μM)
hNaV1.70.0085 ± 0.025 (n = 9)0.907 ± 0.372 (n =8)
hNaV1.70.5216 ± 0.075a (n =3)12.92 ± 1.36a (n =3)
mNaV1.70.0186 ± 0.0052 (n =3)0.387 ± 0.049 (n =3)
rNav1.78.61 ± 0.242 (n =3)>42 (n =3)
mDRG TTX-S0.0031 ± 0.0007 (n =6)2.56 ± 0.743 (n =4)
mDRG TTX-R>5 (n =2)>5 (n =2)
hNaV1.5>30 (n =2)>30 (n =2)
  • hNaV1.5, human NaV1.5; hNaV1.7, human NaV1.7; mDRG, mouse DRG; mNaV1.7, mouse NaV1.7; PX, PatchXpress; rNaV1.7, rat NaV1.7.

  • a Compound potency determined on the resting/closed state.