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. 2012 Sep 24;55(20):8603–8614. doi: 10.1021/jm300801u

Table 3. Effect of R3 = Cl or R3 = H on the 5-HT3AR Affinity.

3.

# 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
a

Determined by radioligand competition using [3H]granisetron.