Literature DB >> 968048

Prostaglandin endoperoxide and thromboxane generating systems and their selective inhibition.

S Moncada, P Needleman, S Bunting, J R Vane.   

Abstract

Two enzyme systems and their selective inhibition are described. Microsomes from ram seminal vesicles (RSV) incubated with arachidonic acid at 22 degrees C generated a rabbit aorta contracting substance which, after rapid ether extraction, had characteristics similar to purified standard endoperoxides. Incubation of either purified endoperoxide or the product from RSV and arachidonic acid with horse platelet microsomes (HPM) yielded a more potent rabbit aorta contracting substance characterized as thromboxane A2, with a half life of 35.9 +/- 2.2 s at 37 degrees C after ether extraction. Two inhibitors, indomethacin and benzydamine exhibited selectivity for the two enzyme systems. The IC50 for benzydamine against thromboxane synthetase was 100 mug/ml and 250 mug/ml against RSV. Indomethacin showed a greater degree of selectivity with an IC50 of 5 mug/ml for the ram seminal vesicle cyclo-oxygenase compared to 100 mug/ml for thromboxane synthetase.

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Year:  1976        PMID： 968048     DOI： 10.1016/0090-6980(76)90014-9

Source DB:  PubMed          Journal:  Prostaglandins        ISSN： 0090-6980


  28 in total

1.  Selective inhibitory actions of sodium-p-benzyl-4-[1-oxo-2-(4-chlorobenzyl)-3-phenyl propyl] phenyl phosphonate (N-0161) and indomethacin on the biosynthesis of prostaglandins and thromboxanes from arachidonic acid.

Authors:  K E Eakins; P S Kulkarni
Journal:  Br J Pharmacol       Date:  1977-05       Impact factor: 8.739

2.  Tracks of a non-main path traveler: 2011 Thomas Willis Lecture.

Authors:  John M Hallenbeck
Journal:  Stroke       Date:  2012-01-12       Impact factor: 7.914

3.  Delta6-desaturase (FADS2) deficiency unveils the role of omega3- and omega6-polyunsaturated fatty acids.

Authors:  Wilhelm Stoffel; Barbara Holz; Britta Jenke; Erika Binczek; Robert Heinz Günter; Christine Kiss; Iakowos Karakesisoglou; Mario Thevis; Artur-Aron Weber; Stephan Arnhold; Klaus Addicks
Journal:  EMBO J       Date:  2008-09-03       Impact factor: 11.598

4.  Prostacyclin and thromboxanes in carrageenan-induced pleurisy in the rat.

Authors:  M Tissot; C Bonne; B Martin; M Solier; J P Giroud
Journal:  Agents Actions       Date:  1984-01

5.  Comparison of the actions of U-46619, a prostaglandin H2-analogue, with those of prostaglandin H2 and thromboxane A2 on some isolated smooth muscle preparations.

Authors:  R A Coleman; P P Humphrey; I Kennedy; G P Levy; P Lumley
Journal:  Br J Pharmacol       Date:  1981-07       Impact factor: 8.739

6.  Staphylococcal alpha-toxin elicits hypertension in isolated rabbit lungs. Evidence for thromboxane formation and the role of extracellular calcium.

Authors:  W Seeger; M Bauer; S Bhakdi
Journal:  J Clin Invest       Date:  1984-09       Impact factor: 14.808

Review 7.  Steroids, aspirin, and inflammation.

Authors:  E Katler; G Weissmann
Journal:  Inflammation       Date:  1977-12       Impact factor: 4.092

8.  Modification of cholesterol crystal-induced inflammation.

Authors:  C W Denko; M Petricevic
Journal:  Agents Actions       Date:  1980-09

9.  Application of imidazole as a selective inhibitor thromboxane synthetase in human platelets.

Authors:  P Needleman; A Raz; J A Ferrendelli; M Minkes
Journal:  Proc Natl Acad Sci U S A       Date:  1977-04       Impact factor: 11.205

10.  Lipopolysaccharide augments HLA-A,B,C molecule expression but inhibits interferon-gamma-induced HLA-DR molecule expression on cultured human endothelial cells.

Authors:  A Otsuka; T Hanafusa; N Kono; S Tarui
Journal:  Immunology       Date:  1991-08       Impact factor: 7.397
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