Table 1.
Analog | NaV1.2 | NaV1.4 | ||||||||
---|---|---|---|---|---|---|---|---|---|---|
%[a] Block | kobs (min-1) |
koff (min-1) |
kon
[b] (μM•min)-1 |
Kd
[c] (μM) |
% Block | kobs (min-1) |
koff (min-1) |
kon
[b] (μM•min)-1 |
Kd
[c] (μM) |
|
KIIIA | 90±3 | 0.36±0.06 | 0.0016±0.0016 | 0.36±0.06 | 0.004±0.004 | 86±6 | 0.91±0.17 | 0.05±0.017 | 0.86±0.17 | 0.06±0.02 |
KIIIA[C1A, C9A] | 93±2 | 1.8±0.39 | 0.014±0.002 | 1.8±0.39 | 0.008±0.002 | 85±2 | 4.0±0.5 | 0.78±0.1 | 3.22±0.51 | 0.24±0.05 |
KIIIA[C2A, C15A] | 66±4 | 0.07±0.02 | 0.01±0.0014 | 0.06±0.02 | 0.17±0.06 | 71±4 | 0.56±0.08 | 0.15±0.03 | 0.41±0.09 | 0.37±0.11 |
KIIIA[C4A, C16A] | 8±3 | n.a. [d] | n.a. | -- | -- | 1±1 | n.a. | n.a. | -- | -- |
Percent block was determined at steady-state or plateau value of single exponential fit of time course of block during 20 min. of exposure to 1 μM peptide;
kon was estimated from {kobs – koff};
Kd was estimated from {koff/kon};
n.a., unable to be determined because level of block was too small. Values represent mean s.d. from at least three different oocytes.