Prostaglandin (PG)E 2 is a potent mediator of pain and inflammation, and high levels of this
lipid mediator are observed in numerous disease states. The inhibition of PGE 2 production …

Permeability is an important property of drug candidates. The Madin–Darby canine kidney
cell line (MDCK) permeability assay is widely used and the primary concern of using MDCK …

Species independence of brain tissue binding was assessed with a large number of structurally
diverse compounds using equilibrium dialysis with brain homogenates of seven species …

In addition to having desirable inhibitory effects on inflammation, anaphylaxis, and smooth
muscle contraction, PDE-IV inhibitors also produce undesirable side effects including nausea …

Historically, recovery had been used to evaluate the data quality of plasma protein binding or
tissue binding obtained from equilibrium dialysis assays. Low recovery was often indicative …

Understanding the quantitative implications of P-glycoprotein and breast cancer resistance
protein efflux is a key hurdle in the design of effective, centrally acting or centrally restricted …

Apparent intrinsic clearance (CLia) determined from microsomal stability assays is a
cornerstone in drug discovery. Categorical bins are routinely applied to this end point to facilitate …

Subcutaneous administration of Granulocyte-macrophage-colony stimulating factor (GM-CSF)
to mice enhanced LPS-induced cytokine production in the circulation (TNF, IL-6) and …

The synthesis and biological properties of a novel series of potent and selective
phosphodiesterase type IV (PDE IV) inhibitors are described. These catechol benzimidazoles were …

… lavage (BAL) was performed using one 15 mL wash of phosphate buffered saline (PBS)
delivered through a pediatric fiberoptic bronchoscope (Olympus, model BF 3C20, Japan) …