TABLE 3

Effects of mutations that change the interaction of corticosterone with rOCT1 on the affinity of TBuA+ from extracellular

Wild-type rOCT1 or rOCT1 mutants were expressed in oocytes. Inhibition of currents induced by superfusion with 0.2 mM or 2 mM TEA+ by extracellular TBuA+ was measured as in Fig. 2. The Hill equation was fitted to inhibition curves of individual oocytes and IC50 values were calculated. The data are presented and the Ki values were calculated as in Table 1. The ratios between the mean IC50 values measured with 2 mM TEA+ and 0.2 mM TEA+ [f(part.compet.)] were used to calculate the Ki values from the IC50 value obtained with 0.2 mM TEA+.


Inhibition from Extracellular

C451M

C451M,F160A

C451M,L447Y

C451M,W218Y

C451M,R440K
IC50 (0.2 mM TEA) 11.8 ± 3.6 (6) 1.2 ± 0.2 (5)*** 1.1 ± 0.3 (5)*** 11.0 ± 0.1 (3) 9.7 ± 2.1 (6)
IC50 (2 mM TEA) 81.5 ± 10.5 (4) 19.3 ± 1.7 (6)*** 6.4 ± 1.7 (5)*** 88.3 ± 14.4 (4) 82.9 ± 16.2 (4)
f (part.compet.) 6.9 15.8 5.8 8.0 8.5
K i
3.5 ± 1.1
0.18 ± 0.03***
0.30 ± 0.08***
2.89 ± 0.03
2.43 ± 0.53
  • *** P < 0.001, analysis of variance with Tukey test, difference compared with rOCT1(C451M).

  • P < 0.01, Student's t test, difference from rOCT1(C451M).