Approach to detect substrates suitable to measure the coumarin 7-hydroxylase (Cyp 2a-5)-structure-activity relationships

Arch Pharm (Weinheim). 1994 May;327(5):299-302. doi: 10.1002/ardp.19943270506.

Abstract

Besides coumarin, which up to now has remained the most selective substrate for the coumarin 7-hydroxylase (Coh), 7-ethoxycoumarin, quinoline, 4-methylcoumarin, 7-ethoxy-4-methylcoumarin, 7-ethoxy-4-ethylcoumarin, and psoralen are suitable for this enzyme. The quantification of the suitability of a substrate to selectively measure the coumarin 7-hydroxylase is achieved by a graphic method. Requirements for serving as a substrate of the Coh are bicyclic ring systems with an electron rich moiety.

MeSH terms

  • Animals
  • Aryl Hydrocarbon Hydroxylases*
  • Coumarins / chemistry
  • Coumarins / metabolism*
  • Cytochrome P-450 CYP2A6
  • Cytochrome P-450 Enzyme System / metabolism*
  • In Vitro Techniques
  • Male
  • Mice
  • Microsomes, Liver / enzymology
  • Mixed Function Oxygenases / metabolism*
  • Structure-Activity Relationship

Substances

  • Coumarins
  • Cytochrome P-450 Enzyme System
  • Mixed Function Oxygenases
  • Aryl Hydrocarbon Hydroxylases
  • Cytochrome P-450 CYP2A6