Table 3. Effect of R3 = Cl or R3 = H on the 5-HT3AR Affinity.
# | R2 | R3 | pKia |
---|---|---|---|
11 | H | Cl | 8.13 ± 0.27 |
49 | H | H | 8.87 ± 0.10 |
48 | OH | Cl | 6.24 ± 0.24 |
26 | OH | H | 7.33 ± 0.12 |
12 | NH2 | Cl | 7.92 ± 0.09 |
22 | NH2 | H | 10.29 ± 0.15 |
6 | NMe | Cl | 8.95 ± 0.05 |
21 | NMe | H | 8.53 ± 0.05 |
Determined by radioligand competition using [3H]granisetron.