Literature DB >> 1850690

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

B S Tsai1, L K Kessler, J Stolzenbach, G Schoenhard, R F Bauer.   

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.

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Year:  1991        PMID: 1850690     DOI: 10.1007/bf01297024

Source DB:  PubMed          Journal:  Dig Dis Sci        ISSN: 0163-2116            Impact factor:   3.199


  22 in total

1.  Differential in vivo pulmonary degradation of prostaglandins E1, B1, and A1.

Authors:  R P Robertson
Journal:  Am J Physiol       Date:  1975-01

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Authors:  G L Hammond; L H Cronau; D Whittaker; C N Gillis
Journal:  Surgery       Date:  1977-06       Impact factor: 3.982

3.  Antisecretory activity of misoprostol, its racemates, stereoisomers and metabolites in isolated parietal cells.

Authors:  B S Tsai; L K Kessler; P Collins; S Kramer; R F Bauer
Journal:  Prostaglandins       Date:  1987

4.  Intestinal absorption of prostaglandin F2alpha, 15(S)-15-methyl prostaglandin F2alpha and their methyl esters in the dog.

Authors:  A Robert; W E Magee; O V Miller; J E Nezamis
Journal:  Biochim Biophys Acta       Date:  1974-05-29

5.  Effect of misoprostol on histamine-stimulated acid secretion and cyclic AMP formation in isolated canine parietal cells.

Authors:  B S Tsai; L K Kessler; G M Butchko; R F Bauer
Journal:  Dig Dis Sci       Date:  1987-09       Impact factor: 3.199

6.  Reaction of a microsomal esterase from hog-liver with diethyl rho-nitrophenyl phosphate.

Authors:  K Krisch
Journal:  Biochim Biophys Acta       Date:  1966-08-10

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Authors:  F L Anderson; W Jubiz; T J Tsagaris
Journal:  Am J Physiol       Date:  1976-08

8.  Secretagogue stimulation of [14C]aminopyrine accumulation by isolated canine parietal cells.

Authors:  A H Soll
Journal:  Am J Physiol       Date:  1980-04

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Authors:  R Håkanson; G Liedberg; J Oscarson
Journal:  Br J Pharmacol       Date:  1973-03       Impact factor: 8.739

10.  Cimetidine and prostaglandin: evidence for different modes of action on the rat gastric mucosa.

Authors:  H A Carmichael; L M Nelson; R I Russel
Journal:  Gastroenterology       Date:  1978-06       Impact factor: 22.682

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  2 in total

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Authors:  Deborah L Clarke; Maria G Belvisi; Matthew C Catley; Magdi H Yacoub; Robert Newton; Mark A Giembycz
Journal:  Br J Pharmacol       Date:  2004-03-15       Impact factor: 8.739

2.  Crystal structure of misoprostol bound to the labor inducer prostaglandin E2 receptor.

Authors:  Martin Audet; Kate L White; Billy Breton; Barbara Zarzycka; Gye Won Han; Yan Lu; Cornelius Gati; Alexander Batyuk; Petr Popov; Jeffrey Velasquez; David Manahan; Hao Hu; Uwe Weierstall; Wei Liu; Wenqing Shui; Vsevolod Katritch; Vadim Cherezov; Michael A Hanson; Raymond C Stevens
Journal:  Nat Chem Biol       Date:  2018-12-03       Impact factor: 15.040

  2 in total

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