Unit

UNIT 7.5 Determination of Compound Binding to Plasma Proteins

  1. Natasha Dow

Published Online: 1 OCT 2006

DOI: 10.1002/0471141755.ph0705s34

Current Protocols in Pharmacology

Current Protocols in Pharmacology

How to Cite

Dow, N. 2006. Determination of Compound Binding to Plasma Proteins. Current Protocols in Pharmacology. 34:7.5:7.5.1–7.5.15.

Author Information

  1. Covance Laboratories, Inc., Madison, Wisconsin

Publication History

  1. Published Online: 1 OCT 2006
  2. Published Print: SEP 2006

Abstract

The pharmacokinetic and pharmacodynamic properties of a compound are profoundly affected by the extent of its binding to plasma proteins. Consequently, the determination of the plasma protein binding properties of a compound is essential during drug development and is increasingly required during lead prioritization. The protocols described in this unit detail the techniques of ultrafiltration and equilibrium dialysis for determination of plasma protein binding. Equilibrium dialysis is the more robust of the two techniques, whereas ultrafiltration is the more rapid. Two versions of the equilibrium dialysis technique are provided: the traditional approach and a higher-throughput 96-well plate version.

Keywords:

  • protein binding;
  • ultrafiltration;
  • equilibrium dialysis;
  • ADME screening