Table 1.
# | H4R/5-HT3AR | Structure | Affinity (pKi) |
|
---|---|---|---|---|
H4Ra | 5-HT3ARc | |||
1 | 7.0 ± 0.1 | n.a. | ||
2 | 6.2 ± 0.1 | n.a. | ||
3 | 6.7 ± 0.0 | n.a. | ||
4 | n.a. | 6.1 ± 0.2 | ||
5 | n.a. | 6.0 ± 0.0 | ||
6 | n.a. | 6.1 ± 0.1 | ||
7 | 6.2 ± 0.0 | 6.6 ± 0.3 | ||
8 | 7.2 ± 0.0 | 7.9 ± 0.3 | ||
9 | 6.1 ± 0.1b | 8.8 ± 0.1 | ||
10 | 8.2 ± 0.1 | 5.9 ± 0.1 | ||
11 | 6.2 ± 0.1b | 5.9 ± 0.3 |
n.a.: Non active.
Measured by displacement of [3H]histamine binding using membranes of HEK293 cells transiently expressing the human H4R. pKi’s are calculated from at least three independent measurements as the mean ± SEM.
Determined using membranes of SK-N-MC cells transiently expressing the human H4R. pKi’s are calculated from at least three independent measurements as the mean ± SEM.
pKi: Measured by displacement of [3H]granisetron binding using membranes of HEK293 cells expressing the human 5-HT3AR. pKi’s are calculated from at least two independent measurements as the mean ± SEM.