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Identification of in vitro rat metabolites of pentacaine, a carbanilate local anaesthetic, by gas chromatography/mass spectrometry
Author(s) -
Štefek M.,
Beneš L.,
Kováčik V.
Publication year - 1986
Publication title -
biomedical and environmental mass spectrometry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.475
H-Index - 121
eISSN - 1096-9888
pISSN - 0887-6134
DOI - 10.1002/bms.1200130408
Subject(s) - hydroxylation , chemistry , mass spectrometry , chromatography , electron ionization , gas chromatography–mass spectrometry , gas chromatography , microsome , mass spectrum , deuterium , substrate (aquarium) , carbamate , in vitro , organic chemistry , biochemistry , enzyme , biology , ion , physics , quantum mechanics , ionization , ecology
Pentacaine, a novel carbanilate local anaesthetic, is extensively metabolized in rat liver microsomes. The major metabolic routes were found to be aromatic ring hydroxylation, hydroxylation of the aliphatic side‐chain and carbamate bond hydrolysis. A deuterium‐labelled substrate was used to aid the identification. The metabolites were characterized by gas chromatography/electron impact mass spectrometry as methyl and/or trifluoroacetyl derivatives. All identifications were confirmed by synthesis and direct comparison of chromatographic data and mass spectra.