From: Identification of critical residues in loop E in the 5-HT3ASR binding site
Ki (Inhibition of [3H]granisetron binding) nM | ||||
---|---|---|---|---|
Receptor | 5-HT (nM) | MCPBG (nM) | d -tc (nM) | Lerisetron |
Wildtype | 74 ± 17 | 3.0 ± 0.55 | 6 ± 2.1 | 0.8 ± 0.19 |
Y140A | 97 ± 20 | 22 ± 6.1 | 300 ± 120 | 2.1 ± 0.33 |
V141A | 82 ± 9.2 | 4.1 ± 0.50 | 4.7 ± 0.87 | 0.20 ± 0.02 |
Y142A | (8 ± 2.0) × 10 3 | 470 ± 90 | 39 ± 19 | 130 ± 28 |
V143A | 22 ± 2.2 | 2.0 ± 0.44 | 22 ± 2.6 | 1.5 ± 0.41 |
H145A | 29 ± 6.5 | 0.60 ± 0.10 | 19 ± 2.6 | 0.42 ± 0.04 |
R146A | 61 ± 14 | 15 ± 4.9 | 29 ± 4.9 | 2.3 ± 0.31 |
E148A | 73 ± 11 | 8.2 ± 1.5 | 14 ± 1.7 | 2.8 ± 0.53 |
Q150A | 170 ± 29 | 27 ± 3.9 | 9.3 ± 1.3 | 1.1 ± 0.21 |
N151A | 140 ± 20 | 1.8 ± 0.18 | 9.3 ± 1.4 | 3.7 ± 0.62 |
Y152A | (1.8 ± 0.4) × 10 3 | 73 ± 26 | 60 ± 19 | 150 ± 36 |
K153A | 270 ± 34 | 7.7 ± 2.0 | 17 ± 3.0 | 3.0 ± 0.66 |