Potency values from a cAMP formation assay in C6 cells expressing hH3R(445) or hH3R(365)
Potencies are expressed as mean pEC50 ± S.E.M. (n = 2-7). (R)-α-Methylhistamine, α = 1 and ABT-239, α = -1 by definition.
No. | Compound | hH3R(445) | hH3R(365) | ||||
|---|---|---|---|---|---|---|---|
| pEC50 | α | pEC50 | α | ||||
| 1 | FUB322 | 4.2 ± 0.3 | 1.2 ± 0.2 | 6.7 ± 0.2 | 1.1 ± 0.04 | ||
| 2 | GT-2331 | 7.2 ± 0.3 | 0.76 ± 0.1 | 8.2 ± 0.3 | 1.0 ± 0.1 | ||
| 3 | Histamine | 7.4 ± 0.2 | 1.0 ± 0.02 | 9.5 ± 0.1 | 1.0 ± 0.1 | ||
| 7 | Immepip | 9.0 ± 0.1 | 0.87 ± 0.1 | 9.9 ± 0.2 | 0.92 ± 0.1 | ||
| 10 | Nα-Methylhistamine | 8.5 ± 0.1 | 1.1 ± 0.01 | 9.7 ± 0.3 | 1.0 ± 0.2 | ||
| 12 | (R)-α-Methylhistamine | 8.2 ± 0.1 | 1.0 ± 0.03 | 9.8 ± 0.2 | 1.0 ± 0.1 | ||
| 13 | (S)-α-Methylhistamine | 6.8 ± 0.1 | 1.1 ± 0.0 | 8.3 ± 0.3 | 1.0 ± 0.2 | ||
| 19 | A-349821 | 9.0 ± 0.4 | -1.0 ± 0.1 | 8.1 ± 0.2 | -1.0 ± 0.2 | ||
| 20 | A-358239 | 8.5 ± 0.3 | -0.90 ± 0.1 | 7.3 ± 0.3 | -1.1 ± 0.1 | ||
| 25 | Iodophenpropit | 8.5 ± 0.4 | -0.77 ± 0.05 | 7.8 ± 0.4 | -0.50 ± 0.1 | ||
| 27 | Thioperamide | 7.6 ± 0.2 | -0.83 ± 0.1 | 6.8 ± 0.3 | -0.71 ± 0.05 | ||