Identification of in vitro rat metabolites of pentacaine, a carbanilate local anaesthetic, by gas chromatography/mass spectrometry.
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.
D000779:Anesthetics, Local / Q000032:analysis* / Q000378:metabolism; D000818:Animals; D001711:Biotransformation; D002219:Carbamates / Q000032:analysis* / Q000378:metabolism; D008401:Gas Chromatography-Mass Spectrometry; D066298:In Vitro Techniques; D008297:Male; D008862:Microsomes, Liver / Q000378:metabolism; D009249:NADP / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains
D000779:Anesthetics, Local; D002219:Carbamates; D009249:NADP; C010618:pentacaine