Article
Application of the relative activity factor approach in scaling from heterologously expressed cytochromes p450 to human liver microsomes: studies on amitriptyline as a model substrate.
The Journal of pharmacology and experimental therapeutics - 1 Apr 2001
Venkatakrishnan K, von Moltke L L, Greenblatt D J
Abstract excerpt
The relative activity factor (RAF) approach is being increasingly used in the quantitative phenotyping of multienzyme drug biotransformations. Using lymphoblast-expressed cytochromes P450 (CYPs) and the tricyclic antidepressant amitriptyline as a model substrate, we have tested the hypothesis tha...
Topics
- Amitriptyline
- Biotransformation
- Cytochrome P-450 Enzyme System
- Humans
- Isoenzymes
- Ketoconazole
- Microsomes, Liver
- Phenotype
- Recombinant Proteins