Suppression by roflumilast and reference PDE4 inhibitors of LPS-induced circulating TNFα in the rat
| Compound | ED50 p.o. |
|---|---|
| μmol/kg | |
| Roflumilast | 0.3 (0.13, 0.51) |
| N-Oxide | 0.3 (0.16, 0.63) |
| Piclamilast | 2.6 (1.7, 3.9) |
| Rolipram | 7.5 (2.9, 19.8) |
| Cilomilast | 93.0 (37.7, 230.2) |
In vivo effects of p.o. administered roflumilast and itsN-oxide metabolite in comparison with reference PDE4 inhibitors on LPS-induced TNFα in Sprague-Dawley rats. Compounds were given p.o. 1 h prior to and plasma samples for determination of TNFα concentrations were obtained 1.5 h after LPS challenge (0.1 mg/kg i.v.). n = 8–16 per dose; 4 doses per compound. Data are given as means and 95% confidence limits (in parentheses).