Functional potencies of CEP-26401 and reference compounds in the [35S]GTPγS binding assay
Mean ± S.D. (n = 3–5).
| Antagonist Activity, Kb, app | Inverse Agonist Activity, EC50 | ||||
|---|---|---|---|---|---|
| Rat Cortical Membrane | Recombinant rH3R | Recombinant hH3R | Recombinant rH3R | Recombinant hH3R | |
| nM | |||||
| CEP-26401 | 4.5 ± 1.0 | 1.0 ± 0.2 | 0.4 ± 0.1 | 2.0 ± 0.8 | 1.1 ± 0.0 |
| Ciproxifan | 0.1 ± 0.05 | 0.8 ± 0.3 | 54 ± 31 | 1.2 ± 0.3 | 188 ± 83 |
| ABT-239 | 1.0 ± 0.8 | 4.5 ± 2.3 | 0.6 ± 0.2 | 5.8 ± 2.2 | 2.7 ± 1.0 |