Expression of gastric antisecretory and prostaglandin E receptor binding activity of misoprostol by misoprostol free acid.

Abstract:

:In enriched canine parietal cell preparations, misoprostol, an analog of prostaglandin E1 methyl ester, was rapidly deesterified to misoprostol free acid. Under this circumstance, misoprostol and misoprostol free acid exhibited equal antisecretory potency against histamine-stimulated acid secretion and bound equally well to prostaglandin E receptors. When the deesterification of misoprostol was inhibited by paraoxon, an esterase inhibitor, the antisecretory and receptor binding activity of misoprostol was markedly reduced, with potency much less than misoprostol free acid. These results indicate that misoprostol free acid is the active biological form of misoprostol that binds to prostaglandin E receptors and mediates the antisecretory action of misoprostol.

journal_name

Dig Dis Sci

authors

Tsai BS,Kessler LK,Stolzenbach J,Schoenhard G,Bauer RF

doi

10.1007/BF01297024

subject

Has Abstract

pub_date

1991-05-01 00:00:00

pages

588-93

issue

5

eissn

0163-2116

issn

1573-2568

journal_volume

36

pub_type

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