Literature DB >> 406909

Comparative effects of aspirin and diflunisal on prostaglandin synthetase from human platelets and sheep seminal vesicles.

P W Majerus, N Stanford.   

Abstract

1. We have compared the effects of diflunisal on prostaglandin (PG) synthetase from human platelets and sheep seminal vesicles (SSV) by measuring malonaldehyde, PG products, and rabbit aorta contraction. 2. Aspirin inhibits PG synthetase by covalently acetylating the enzyme. Inhibition is dependent on time and aspirin concentration. Aspirin is 37-fold more potent in inhibiting enzyme in human platelets compared with enzyme from SSV. 3. Diflunisal inhibits PG synthetase from intact human platelets and SSV equally (50% inhibition at 3-5 micronM). The drug does not covalently modify the enzyme, and inhibition is not time dependent. Diflunisal probably acts at a site similar to aspirin since the drug will inhibit acetylation of the enzyme by aspirin. 4. The results suggest that diflunisal is relatively less inhibitory to platelet function than is aspirin.

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Year:  1977        PMID: 406909      PMCID: PMC1428838          DOI: 10.1111/j.1365-2125.1977.tb04509.x

Source DB:  PubMed          Journal:  Br J Clin Pharmacol        ISSN: 0306-5251            Impact factor:   4.335


  7 in total

1.  Editorial: Why aspirin?

Authors:  P W Majerus
Journal:  Circulation       Date:  1976-09       Impact factor: 29.690

2.  Thromboxanes: selective biosynthesis and distinct biological properties.

Authors:  P Needleman; M Minkes; A Raz
Journal:  Science       Date:  1976-07-09       Impact factor: 47.728

3.  Effects of salicylates on human platelets.

Authors:  J R O'Brien
Journal:  Lancet       Date:  1968-04-13       Impact factor: 79.321

4.  The binding of thrombin to the surface of human platelets.

Authors:  D M Tollefsen; J R Feagler; P W Majerus
Journal:  J Biol Chem       Date:  1974-04-25       Impact factor: 5.157

5.  Properties of a novel preparation of prostaglandin synthetase from sheep seminal vesicles.

Authors:  D P Wallach; E G Daniels
Journal:  Biochim Biophys Acta       Date:  1971-05-04

6.  The mechanism of the effect of aspirin on human platelets. I. Acetylation of a particulate fraction protein.

Authors:  G J Roth; P W Majerus
Journal:  J Clin Invest       Date:  1975-09       Impact factor: 14.808

7.  Acetylation of prostaglandin synthase by aspirin.

Authors:  G J Roth; N Stanford; P W Majerus
Journal:  Proc Natl Acad Sci U S A       Date:  1975-08       Impact factor: 11.205

  7 in total
  13 in total

1.  Sensitivity of fatty acid cyclooxygenase from human aorta to acetylation by aspirin.

Authors:  J W Burch; N L Baenziger; N Stanford; P W Majerus
Journal:  Proc Natl Acad Sci U S A       Date:  1978-10       Impact factor: 11.205

2.  Pharmacokinetics of intraarticular indomethacin in patients with osteoarthritis.

Authors:  G Neander; L O Eriksson; E Wållin-Boll; H Ersmark; A Grahnen
Journal:  Eur J Clin Pharmacol       Date:  1992       Impact factor: 2.953

3.  Multiple sites on prostaglandin cyclooxygenase are determinants in the action of nonsteroidal antiinflammatory agents.

Authors:  J L Humes; C A Winter; S J Sadowski; F A Kuehl
Journal:  Proc Natl Acad Sci U S A       Date:  1981-04       Impact factor: 11.205

4.  Diflunisal in osteoarthrosis of the hip and knee.

Authors:  W K Essigman; M A Chamberlain; V Wright
Journal:  Ann Rheum Dis       Date:  1979-04       Impact factor: 19.103

Review 5.  Diflunisal: a review of its pharmacological properties and therapeutic use in pain and musculoskeletal strains and sprains and pain in osteoarthritis.

Authors:  R N Brogden; R C Heel; G E Pakes; T M Speight; G S Avery
Journal:  Drugs       Date:  1980-02       Impact factor: 9.546

6.  The oral activity of delta'-tetrahydrocannabinol and its dependence on prostaglandin E2.

Authors:  J W Fairbairn; J T Pickens
Journal:  Br J Pharmacol       Date:  1979-11       Impact factor: 8.739

7.  Influence of renal failure, rheumatoid arthritis and old age on the pharmacokinetics of diflunisal.

Authors:  L O Erikson; E Wåhlin-Boll; I Odar-Cederlöf; L Lindholm; A Melander
Journal:  Eur J Clin Pharmacol       Date:  1989       Impact factor: 2.953

8.  Group A streptococcal pyrogenic exotoxin: pyrogenicity, alteration of blood-brain barrier, and separation of sites for pyrogenicity and enhancement of lethal endotoxin shock.

Authors:  P M Schlievert; D W Watson
Journal:  Infect Immun       Date:  1978-09       Impact factor: 3.441

9.  Different sensitivities of prostaglandin-cyclooxygenases in blood platelets and coronary arteries against non-steroidal antiinflammatory drugs.

Authors:  K Schrör; S Sauerland; A Kuhn; R Rösen
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1980-08       Impact factor: 3.000

10.  Diflunisal in rheumatoid arthritis.

Authors:  B Fishel; S Weiss; M Yaron
Journal:  Inflammation       Date:  1981-09       Impact factor: 4.092

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