Comparison of radioligand binding affinities in WT and mutant receptors determined with [3H](S)zacopride
| Ligand | WT (F107) | F107Y | F107N |
|---|---|---|---|
| [3H](S)-Zacopride | 0.12 ± 0.04 (3) | 0.11 ± 0.02 (3) | 0.05 ± 0.02 (4) |
| 5-HT | 153 ± 8 (3) | 434 ± 109 (3)* | 51.1 ± 13.0 (3)* |
| 2-Methyl-5-HT | 395 ± 28 (3) | 1677 ± 250 (3)* | 246 ± 40 (3) |
| Granisetron | 3.90 ± 0.73 (4) | 1.87 ± 0.32 (3) | 4.46 ± 0.71 (4) |
| Renzapride | 8.81 ± 1.26 (4) | 6.04 ± 1.63 (3) | 4.52 ± 0.70 (5)* |
Kd and Ki values (nM) were determined as described in the text at a temperature of 37°C. Each value is the mean ± S.E., with the number of determinations given in parentheses.
Significance was determined using the Student's ttest on pKd and pKi values (*P < .05).