Heather L. Hatch

TL;DR: It appears that most CNS-active agents demonstrate at least some P-gp-mediated transport that can affect brain concentrations, and unbound plasma concentrations may need to be greater than values projected using receptor affinity data to achieve adequate receptor occupancy for effect.

TL;DR: The results indicate that the absorption, distribution, metabolism and excretion (ADME) profile of 1 is relatively consistent across preclinical species and predict potentially favorable pharmacokinetic properties in humans, supporting its selection for toxicity/safety assessment studies and possible investigations in humans as an anti‐inflammatory agent.

TL;DR: It is suggested that hepatic transporters play an important role in the disposition and clearance of CP-671,305 in rat and human, and as such, these studies should aid in the design of clinical drug-drug interaction studies.

TL;DR: Results of structure–activity relationship studies for a series of novel non-THQ CETP inhibitors resulted in the identification of a novel isonipecotic acid derivative 10 with vastly improved oral pharmacokinetic properties mainly as a result of improved aqueous solubility.

TL;DR: The findings suggest that, in vivo, cisapride appears to be moderate substrate of P-gp and that the brain penetration of isapride is enhanced in mice lacking P- gp expression.