PMID: 2094417Jan 1, 1990Paper

Application of liquid chromatography with on-line radiochemical detection to metabolism studies on a novel class of analgesics

Journal of Pharmaceutical and Biomedical Analysis
K R WehmeyerL A Bowman

Abstract

Vanilloids are a class of compounds structurally related to capsaicin, the pungent principle of hot peppers, which are under development as a novel class of analgesics. Vanilloids undergo extensive first-pass metabolism when dosed orally to rats and mice. These compounds, as well as capsaicin, would be anticipated to be susceptible to three major routes of metabolism: (omega, beta)-oxidation of the alkyl side chain, hydrolysis of the amide bond and conjugation of the phenolic group. Olvanil [N-(3-methoxy-4-hydroxybenzyl)oleamide], radiolabelled with either 14C at the benzylic carbon or 3H in the oleyl side chain, was studied in various in vitro, in situ and in vivo metabolism models to determine the major route(s) of intestinal and hepatic metabolism in rats for this new class of compounds. Models used in metabolism studies included isolated hydrolytic enzymes, cell-free intestinal and liver supernatants, hepatocytes, enterocytes, perfused intestine and whole animal studies. Reversed-phase liquid chromatography (LC) with on-line radiochemical detection was used to examine the metabolic profiles from the different models. The major metabolic route for olvanil in both the intestine and the liver was found to be hydrolysis of the ...Continue Reading

References

Mar 15, 1984·Toxicology and Applied Pharmacology·T KawadaK Iwai
Feb 1, 1983·Biochemical Pharmacology·M S MillerI G Sipes

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Citations

Dec 18, 2001·Journal of Applied Toxicology : JAT·E J Olajos, H Salem
Jun 1, 1995·Journal of Computer-aided Molecular Design·G Klopman, J Y Li
Jan 1, 1997·Journal of Pharmaceutical Sciences·G B KastingG O Kinnett
Jan 29, 2021·Journal of Medicinal Chemistry·Stephen D RichbartPiyali Dasgupta

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