Mini-Reviews in Medicinal Chemistry

Author(s): C. Quinones-Torrelo, Y. Martin-Biosca, J. J. Martinez-pla, S. Sagrado, R. M. Villanueva-Camanas and M. J. Medina-Hernandez

DOI: 10.2174/1389557024605519

QRAR Models for Central Nervous System Drugs using Biopartitioning Micellar Chromatography

Page: [145 - 161] Pages: 17

  • * (Excluding Mailing and Handling)

Abstract

The capability of biopartitioning Micellar Chromatography, BMC, to describe and estimate pharmacokinetic and pharmacodynamic parameters of central nervous system drugs is reviewed in this article. BMC is a mode of micellar liquid chromatography, MLC, that uses micellar mobile phases of Brij35 (polyoxyethilene(23) lauryl ether) prepared in physiological conditions (pH, ionic strength). The retention of a drug in this system depends on its hydrophobic, electronic and steric properties, which also determine its biological activity. The results of BMC studies suggest that this in vitro approach is an attractive useful tool to be implemented into the lead optimization step of drug development scheme.

Keywords: biopartitioning micellar chromatography(bmc), hypnotics, sedatives, antipsychotic drugs, anticonvulsants, tricyclic antidepressant, drug toxicity