TABLE 1

In Vitro I2BS Binding Affinities of Blocking Drugs in Rat and Nonhuman Primate Brain Using 3H-BU99008

IC50 ± SD (nM)
Protein targetBlocking drugRatCynomolgus
I2BSBU22450.5 ± 12.9 (high)130.2 ± 33.9
9,596 ± 2,494 (low)
MAOAMoclobemide>100,000>100,000
MAOBLazabemide6,445 ± 1,73317,370 ± 2,068
  • Displacement of 3H-BU99008 by BU224 was best fit to 2-site model in rat only; for all other instances data were best fit to 1-site model (n = 4).

  • IC50 = half maximal inhibitory concentration.