L791943 is a potent, selective Phosphodiesterase-4 (PDE4) inhibitor with an IC50 of 4.2 nM.
The extent of metabolism of L791943 is evaluated in vitro in rat hepatocytes and compared to the data obtaine with CDP-840. In our standard incubation conditions, >98% of the parent drug remain in the case of L791943 whereas only 11% of CDP-840 is left intact[2].
[1]. Richard Frenette, et al. Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters. Bioorg Med Chem Lett. 2002 Oct 21;12(20):3009-13. [2]. Guay D, et al. Discovery of L-791,943: a potent, selective, non emetic and orally active phosphodiesterase-4 inhibitor. Bioorg Med Chem Lett. 2002 Jun 3;12(11):1457-61.