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Knowing the chemical identity and properties of the main metabolites of a compound is of great importance for assessing pharmacokinetics, toxic risks, and for developing toxicological and doping control screening procedures. Unfortunately, such studies are usually not done with drugs of abuse or new psychoactive substances. As it is not possible to perform controlled studies on the in vivo metabolism of new psychoactive substance in humans for ethical reasons, in vitro approaches or in vivo animal experiments are the methods of choice. This chapter therefore summarizes in vitro and in vivo strategies on such metabolism studies for developing toxicological and doping control screening procedures.

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