A simple model to predict blood-brain barrier permeation from 3D molecular fields

Biochim Biophys Acta. 2002 Jul 18;1587(2-3):118-25. doi: 10.1016/s0925-4439(02)00074-1.

Abstract

We report a four-component partial least squares discriminant analysis (PLS) model for the prediction of blood-brain barrier (BBB) permeation using descriptors derived from 3D molecular fields. The 3D fields were transformed by VolSurf into suitable 1D descriptors, which were correlated to the ratio of blood-brain partitioning measured at steady state in rats (log C(brain)/C(blood)). The model so obtained sheds light on molecular properties influencing BBB permeation. It can also be used in the virtual screening of new chemicals.

Publication types

  • Review

MeSH terms

  • Animals
  • Blood-Brain Barrier / physiology*
  • Databases, Factual
  • Drug Evaluation, Preclinical
  • Least-Squares Analysis
  • Models, Biological*
  • Permeability
  • Pharmacokinetics
  • Rats