Understanding the development of a scientific approach is a valuable exercise in gauging
the potential directions the process could take in the future. The relatively short history of …

Efflux out of cells by P-glycoprotein (P-gp) represents a serious liability for pharmaceuticals,
particularly for anti-cancer drugs. Consequently, identification of compounds as potential …

Earning tenure at an academic institution and running a steeplechase race successfully
have a lot in common. Both require extensive training before the event begins, both involve …

Objectives: Our objectives were (1) to determine whether the drugs caffeine, losartan,
omeprazole, debrisoquin (INN, debrisoquine), and quinine can be given simultaneously in …

Using in vitro data, we previously built Catalyst 3-dimensional quantitative structure activity
relationship (3D-QSAR) models that qualitatively rank and predict IC50 values for P …

Permeability of the blood-brain barrier (BBB) is one of the factors determining the
bioavailability of therapeutic drugs. The BBB only allows entry of lipophilic compounds with …

P-glycoprotein (P-gp) is an efflux transporter involved in limiting the oral bioavailability and
tissue penetration of a variety of structurally divergent molecules. A better understanding of …

A general pharmacophore model of P-glycoprotein (P-gp) drugs is proposed that is based
on a highly diverse data set and relates to the verapamil binding site of the protein. It is …

The intestine, primarily regarded as an absorptive organ, is also prepared for the elimination
of certain organic acids, bases and neutral compounds depending on their affinity to …

Background Clinical trials have indicated that the combined β‐and α‐adrenergic receptor
blocker carvedilol improves the survival rate in patients with advanced chronic heart failure …