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Stereoselective binding of the glucuronide conjugates of carprofen enantiomers to human serum albumin.

Abstract：

:The stereoselective binding of carprofen enantiomers and carprofen glucuronide diastereomers to human serum albumin (HSA) was studied using an ultrafiltration method. Carprofen glucuronides exhibit a considerable and stereoselective affinity to HSA, although less than that seen for the parent enantiomers. The (S)-glucuronide showed a higher binding affinity to HSA than the (R)-glucuronide. The (S)-enantiomer of unmetabolized carprofen was bound to fatty acid free HSA to a much greater extent than the (R)-enantiomer. Warfarin reduced the binding of the glucuronides to a greater extent than did diazepam, but diazepam displaced the unconjugated enantiomers to a greater extent than did warfarin. These results suggest differences in binding region between the carprofen enantiomers and their glucuronides on the albumin molecule.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Iwakawa S,Spahn H,Benet LZ,Lin ET

doi

10.1016/0006-2952(90)90212-4

subject

Has Abstract

pub_date

1990-03-01 00:00:00

pages

949-53

issue

5

eissn

0006-2952

issn

1873-2968

pii

0006-2952(90)90212-4

journal_volume

39

pub_type

杂志文章

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