Search results for "Preclinical pharmacology"
showing 2 items of 2 documents
The preclinical pharmacology of roflumilast--a selective, oral phosphodiesterase 4 inhibitor in development for chronic obstructive pulmonary disease
2009
After more than two decades of research into phosphodiesterase 4 (PDE4) inhibitors, roflumilast (3-cyclopropylmethoxy-4-difluoromethoxy-N-[3,5-di-chloropyrid-4-yl]-benzamide) may become the first agent in this class to be approved for patient treatment worldwide. Within the PDE family of 11 known isoenzymes, roflumilast is selective for PDE4, showing balanced selectivity for subtypes A-D, and is of high subnanomolar potency. The active principle of roflumilast in man is its dichloropyridyl N-oxide metabolite, which has similar potency as a PDE4 inhibitor as the parent compound. The long half-life and high potency of this metabolite allows for once-daily, oral administration of a single, 500…
Development of Predictive Retention-Activity Relationship Models of Barbiturates by Micellar Liquid Chromatography
2000
The need to get a tool for biological parameters estimation of new compounds for clinical applications, supports the postulation of predictive models as an alternative to conventional classical assays being no necessary the use of experimentation in animals. Our main aim in this work is to determine correlations between the logarithm of capacity factors and preclinical pharmacology and therapeutic efficacy parameters of barbiturates. The predictive and interpretative capability of quantitative chromatographic retention-biological activity models is supported by the fact that in adequate experimental conditions the solute partitioning into chromatographic system can emulate the solute partit…