Development, Applicability, and Comparison of Bioassays for Metabolism of (New) Psychoactive Substances

Abstract

In the presented dissertation, different in vitro models were investigated and compared as surrogate for human in vivo metabolism studies to identify main urinary excretion products for developing toxicological urine screening approaches for new psychoactive substances (NPS). Assays using human liver preparations, which covered all main metabolic phase I and II steps were developed. Human hepatic cell lines HepG2 and HepaRG were tested as an alternative in vitro model. However, cell lines have the disadvantage of requiring special equipment for cell culture handling. Therefore, pS9 fraction was identified as most cost-efficient and easiest to handle in vitro model, still sufficient enough for developing toxicological urine screenings for NPS, even in comparison to primary human hepatocytes.