Mónika Vastag

TL;DR: While the complexity and predictive value of the BBB model is the highest, for the screening of NCEs to determine whether they are efflux substrates or not, the VB-Caco-2 and the MDCK-MDR1 models may provide a simple and inexpensive tool.

TL;DR: Among the tested culture models, the primary cell-based EPA model is suitable for the functional analysis of the BBB and the absence of gene expression of important BBB efflux and influx transporters BCRP, MRP6, MCT6, -8, PHT2, OATPs in one or both types of epithelial models suggests that Caco-2 or MDCK models are not suitable to test drug candidates which are substrates of these transporter.

TL;DR: Medicinal chemistry optimization of an impurity isolated during the scale-up synthesis of a pyridylsulfonamide type dopamine D(3)/D(2) compound led to a series of new piperazine derivatives having affinity to both dopamine D3 and D2 receptors.

TL;DR: The results indicate that these peptides can be effectively and selectively used as potential pharmaceutical excipients to improve drug delivery across biological barriers.

TL;DR: This review gives a practical summary of in vitro and in silico approaches to evaluate BBB penetration, with models that provide sufficient predictivity, reliability and throughput to be favored by the pharmaceutical industry.