Studies are described on the metabolism and the toxicological detection of the phencyclidine-derived designer drug N-(1-phenylcyclohexyl)-propanamine (PCPR) in rat urine using gas chromatographic-mass spectrometric techniques. The identified metabolites indicated that PCPR was metabolized by hydroxylation of the cyclohexyl ring at different positions, hydroxylation of the phenyl ring, N-dealkylation, and combinations of these steps. Parts of the metabolites were excreted in conjugated form. The authors' systematic toxicological analysis (STA) procedure using full-scan GC-MS after acid hydrolysis, liquid-liquid extraction and microwave-assisted acetylation allowed the detection of an intake of a common drug users' dose of PCPR in rat urine. Assuming similar metabolism in humans, the STA should be suitable for proof of an intake of PCPR in human urine.