TABLE 4

5-HT EC₅₀ and vortioxetine IC₅₀ values for WT and mutant h5-HT_3A receptors

Mutant	5-HT			Vortioxetine
Mutant	EC₅₀^{^a}	n^{^b}	Fold Change	IC₅₀^{^a}	n^{^b}	Fold Change
	µM			nM
WT	0.19 [0.17; 0.21]	33		29 [25; 34]	9
D64V	NF	3
I66A	0.32 [0.24; 0.44]	3	1.7 [1.3; 2.3]	52 [41; 66]^*	5	1.8 [1.4; 2.3]
I66L	0.27 [0.25; 0.29]	3	1.4 [1.3; 1.5]	42 [35; 50]^*	5	1.4 [1.2; 1.7]
N123A	1.8 [1.5; 2.1]^*	9	9.5 [8.2; 11]	47 [40; 56]^*	7	1.6 [1.4; 1.9]
N123I	NF	3
N123L	2.2 [1.4; 3.4]^*	4	12 [7.6; 18]	23 [9; 57]	3	0.8 [0.3; 2.0]
T176A	2.2 [2.0; 2.5]^*	6	12 [11; 13]	32 [28; 37]	5	1.1 [1.0; 1.3]
T176V	4.46 [3.83; 5.19]^*	7	23 [20; 27]	146 [123; 174]^*	5	5.0 [4.2; 6.0]
S177E	NF	3
V202A	6.16 [5.53; 6.86]^*	6	6.2 [5.5; 6.9]	310 [252; 386]^*	8	10.7 [8.7; 13.3]
V202I	0.27 [0.24; 0.31]	4	0.27 [0.24; 0.31]	37 [30; 45]	7	1.3 [1.0; 1.6]
V202L	0.05 [0.03; 0.07]^*	3	0.05 [0.03; 0.07]	5 [4; 6]^*	11	0.2 [0.1; 0.2]
M223I	0.12 [0.10; 0.13]	3	0.12 [0.10; 0.13]	20 [16; 25]	5	0.7 [0.6; 0.9]
E231I	NF	3

↵^a EC₅₀ and IC₅₀ values were determined as described in Materials and Methods. Numbers in brackets denote the 95% confidence intervals.
↵^b n denotes number of independent experiments.
↵* P < 0.01 vs. WT.