A mass spectrometric approach to the identification of conjugated drug metabolites

For the identification of intact underivatized drug conjugates, the mass spectrometric technique of choice is fast atom bombardment (FAB); the combined use of both positive and negative ion FAB usually provides information on the molecular mass and nature of conjugates under study, while the number...

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Bibliographic Details
Published inBiomedical & environmental mass spectrometry Vol. 14; no. 11; p. 689
Main Authors Jacobs, P L, Delbressine, L P, Kaspersen, F M, Schmeits, G J
Format Journal Article
LanguageEnglish
Published England 01.11.1987
Subjects
Animals
Anti-Arrhythmia Agents - urine
Antidepressive Agents, Tricyclic - urine
Bepridil
Bile - analysis
Glucuronates - analysis
Glucuronates - urine
Glycine - urine
Humans
Mass Spectrometry - methods
Mianserin - analogs & derivatives
Mianserin - analysis
Mianserin - urine
Pyrrolidines - analysis
Pyrrolidines - urine
Rabbits
Sulfuric Acids - analysis
Sulfuric Acids - urine
Taurine - urine
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Summary:For the identification of intact underivatized drug conjugates, the mass spectrometric technique of choice is fast atom bombardment (FAB); the combined use of both positive and negative ion FAB usually provides information on the molecular mass and nature of conjugates under study, while the number of exchangeable hydrogen atoms can be determined using trideuterated glycerol as the FAB-matrix. Electron impact and desorption chemical ionization spectra can be used to study the aglycone part of the conjugated metabolites. With this approach metabolites conjugated with glucuronic acid, sulphuric acid and amino acids have been identified. The identification was supported by analysis of reference compounds, prepared by chemical synthesis. The examples given are selected from current metabolism studies on drug candidates in development within Organon's research.
ISSN:0887-6134
DOI:10.1002/bms.1200141121