The stereospecific incorporation of fenoprofen into rat hepatocyte and adipocyte triacylglycerols.

Abstract:

:The formation of triacylglycerols containing fenoprofen was studied in rat isolated adipocytes and hepatocytes incubated with [3H]glycerol and R or S fenoprofen. In both hepatocytes and adipocytes there was a high-affinity enzymatic process for the synthesis of triacylglycerol containing fenoprofen which was stereospecific for the R enantiomer. The apparent Km values for R fenoprofen were 1.0 microM in adipocytes and 2.8 microM in hepatocytes. These results are consistent with the proposed stereospecific formation of R-2-arylpropionyl-CoA thioesters resulting in the stereospecific formation of R-tri-acylglycerol at clinically relevant unbound fenoprofen concentrations. In isolated hepatocytes, but not adipocytes, a second low-affinity enzymatic process for the synthesis of triacylglycerol containing fenoprofen was also observed. However, this process (Km = 3780 microM) occurred at concentrations much higher than those found in man with usual doses.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Sallustio BC,Meffin PJ,Knights KM

doi

10.1016/0006-2952(88)90537-0

subject

Has Abstract

pub_date

1988-05-15 00:00:00

pages

1919-23

issue

10

eissn

0006-2952

issn

1873-2968

pii

0006-2952(88)90537-0

journal_volume

37

pub_type

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