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Table 2 [3H]Granisetron binding to wildtype and mutant 5-HT3ASRs.

From: Identification of critical residues in loop E in the 5-HT3ASR binding site

Receptor

Kd (nM) [3H]granisetron

Bmax (pmol/mg protein)

n

Wildtype

0.98 ± 0.12

3.2 ± .13

1 ± 0.12

Y140A

2.7 ± 0.19

0.44 ± .08

1.5 ± 0.14

V141A

2.5 ± 0.35

0.32 ± .04

1.3 ± 0.22

Y142A

4.5 ± 0.5

0.97 ± .14

1.6 ± 0.27

V143A

1.9 ± 0.28

1.1 ± .04

0.97 ± 0.13

H145A

1.3 ± 0.13

0.81 ± .07

1.38 ± 0.17

R146A

2.4 ± 0.34

1.0 ± .16

1.26 ± 0 .21

G147A

-

-

-

E148A

5.2 ± 1.2

5.5 ± 1.2

0.93 ± 0.19

V149A

-

-

-

Q150A

6.3 ± 0.45

0.56 ± .09

1.19 ± 0 .1

N151A

6.9 ± 0.48

4.9 ± 1.1

1.66 ± 0.16

Y152A

7.8 ± 1.1

0.59 ± .10

1.4 ± 0.24

K153A

7.4 ± 0.61

0.30 ± .08

1.51 ± 0.17

  1. The Kd, Bmax and Hill coefficient (n) were determined using non-linear curve fitting of binding data as described in the methods section. Each value represents the combined data from at least four experiments and is represented as ± SE. The Kd values were used to calculate the ratios plotted in Figure 2, indicating the change in binding affinity as a result of each individual mutation. A plot of the data obtained from Y140A, Y142A and Y152A is shown in Figure 3.