Gas chromatography-mass spectrometry (GC-MS) and HPLC-MS techniques have been developed for studying fragmentation and determining the main ion species in the mass spectra of the new original neuroleptic dilept (N-caproyl-L-prolyl-L-tyrosine methyl ester) and its expected metabolites N-caproyl-L-prolyl-L-tyrosine (M1) and N-caproyl-L-proline (M2). Trimethylsilyl derivatives of dilept and its metabolites were analyzed using GC-MS and HPLC-MS in both positive-and negative-ion modes. Retention times were determined. The EI-MS, ESI-MS, and ESI-MS/MS spectra of all substances were obtained. Results of a comparative analysis of the chromatographic data show that the HPLC-ESI-MS/MS method in negative-ion mode is most sensitive to dilept (LOD = 0.5 ng/mL) and can be recommended for subsequent investigations of metabolism and pharmacokinetics of this potential neuroleptic drug.

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The levels of himantane and its metabolites in daily urine and feces of rats were measured after intraperitoneal and oral dose of 25 mg/kg. The injected dose of the initial substance and 1.3% its metabolites were eliminated with excrements within 24 h after administration via both routes 0.23%.

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