Table 2. Comparison of the inhibition of NaV1.3 by μ-BuIIIB and N-terminal analogsa.
Peptide |
kon (μM•min)-1 |
koff (min1) |
Kd (μM) |
---|---|---|---|
μ-BuIIIB | 0.085 ± 0.01 | 0.017 ± 0.007 | 0.2 ± 0.086 |
[Ala1]BuIIIB | 0.014 ± 0.004 | 0.01 ± 0.003 | 0.71 ± 0.3 |
[d-Ala2]BuIIIB | 0.83 ± 0.05 | 0.004 ± 0.0017 | 0.0048 ± 0.002 |
[Ala2]BuIIIB | 0.25 ± 0.03 | 0.009 ± 0.002 | 0.036 ± 0.009 |
[Ala3]BuIIIB | 0.46 ± 0.03 | 0.007 ± 0.0013 | 0.015 ± 0.003 |
[Ala4]BuIIIB | 0.056 ± 0.008 | 0.01 ± 0.002 | 0.18 ± 0.044 |
[des1-4]BuIIIB | 0.47 ± 0.06 | 0.025 ± 0.005 | 0.053 ± 0.013 |
Rate constants were determined as described in Methods. Kd was determined from koff/kon. Data for μ-BuIIIB are from Wilson et al.(20)