Comparison of binding affinities of ABT-239, A-349821, cipralisant, and ciproxifan at histamine receptors
nH is Hill slope (n = 3-34 independent experiments performed in duplicate). H3 receptors were stably expressed in C6 cells; H1, H2, and H4 receptors were stably expressed in HEK cells.
ABT-239 | A-349821a | Cipralisant | Ciproxifana | ||
|---|---|---|---|---|---|
| mean pKi ± S.E.M. (mean nH ± S.E.M.) | |||||
| Human H3 | 9.35 ± 0.04 (0.98 ± 0.02) | 9.39 ± 0.08 (0.9 ± 0.03) | 8.28 ± 0.08 (1.05 ± 0.03) | 7.20 ± 0.05 (0.84 ± 0.04) | |
| Rat H3 | 8.91 ± 0.04 (0.87 ± 0.02) | 8.78 ± 0.12 (0.93 ± 0.06) | 9.95 ± 0.10 (1.02 ± 0.05) | 9.29 ± 0.09 (0.88 ± 0.02) | |
| Human Brain Cortex H3 | 8.34 ± 0.06 (0.78 ± 0.04)b | 9.37 ± 0.08 (0.77 ± 0.06)b | 7.91 ± 0.12 (1.16 ± 0.10) | 7.05 ± 0.06 (1.06 ± 0.07) | |
| Rat Brain Cortex H3 | 8.49 ± 0.04 (0.81 ± 0.02) | 8.84 ± 0.07 (0.87 ± 0.04) | 9.60 ± 0.07 (1.05 ± 0.03) | 9.20 ± 0.04 (0.90 ± 0.03) | |
| Guinea Pig Brain Cortex H3 | 8.59 ± 0.12 (0.86 ± 0.05) | 9.26 ± 0.13 (0.71 ± 0.07)b | 9.20 ± 0.04 (1.01 ± 0.05) | 8.76 ± 0.07 (0.89 ± 0.05) | |
| Dog Brain Cortex H3 | 8.41 ± 0.07 (0.84 ± 0.09) | 8.92 ± 0.10 (0.83 ± 0.07) | 8.88 ± 0.05 (1.16 ± 0.13) | 8.24 ± 0.06 (0.88 ± 0.02) | |
| Human H1 | 5.79 ± 0.04 (0.96 ± 0.06) | 5.63 ± 0.04 (0.85 ± 0.12) | <5 | <5 | |
| Human H2 | 5.17 ± 0.04 (0.83 ± 0.11) | <5 | <5 | <5 | |
| Human H4 | <5 | <5 | 7.29 ± 0.19 (0.68 ± 0.05) | 5.73 ± 0.09 (0.81 ± 0.19) | |