Literature DB >> 291066

13-Azaprostanoic acid: a specific antagonist of the human blood platelet thromboxane/endoperoxide receptor.

G C Le Breton, D L Venton, S E Enke, P V Halushka.   

Abstract

A newly synthesized 13-aza derivative of prostanoic acid (13-APA) specifically inhibited human platelet aggregation induced by arachidonic acid, prostaglandin H2, or the stable endoperoxide analog (15S)-hydroxy-9 alpha,11 alpha-)epoxymethano)-prosta-5Z,13E-dienoic acid. 13-APA also inhibited [14C]serotonin release in response to arachidonic acid, ADP, or thrombin, but did not inhibit primary aggregation induced by ADP or thrombin. 13-APA completely blocked prostaglandin H2-induced aggregation in indomethacin-treated resuspended platelets but did not inhibit thromboxane synthesis. We therefore conclude that 13-APA acts as a direct antagonist of the platelet thromboxane/endoperoxide receptor.

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Year:  1979        PMID： 291066      PMCID： PMC383985          DOI： 10.1073/pnas.76.8.4097

Source DB:  PubMed          Journal:  Proc Natl Acad Sci U S A        ISSN： 0027-8424            Impact factor:   11.205


  42 in total

1.  STRONG INHIBITION BY 2-CHLOROADENOSINE OF THE AGGREGATION OF BLOOD PLATELETS BY ADENOSINE DIPHOSPHATE.

Authors:  G V BORN
Journal:  Nature       Date:  1964-04-04       Impact factor: 49.962

2.  Aggregation of blood platelets by adenosine diphosphate and its reversal.

Authors:  G V BORN
Journal:  Nature       Date:  1962-06-09       Impact factor: 49.962

3.  Prostacyclin increases cyclic AMP levels and adenylate cyclase activity in platelets.

Authors:  L C Best; T J Martin; R G Russell; F E Preston
Journal:  Nature       Date:  1977-06-30       Impact factor: 49.962

4.  Inhibitors of thromboxane synthase in human platelets.

Authors:  U D Alusy; S Hammarström
Journal:  FEBS Lett       Date:  1977-10-01       Impact factor: 4.124

5.  Azaprostanoic acid derivatives. Inhibitors of arachidonic acid induced platelet aggregation.

Authors:  D L Venton; S E Enke; G C Le Breton
Journal:  J Med Chem       Date:  1979-07       Impact factor: 7.446

6.  Controlled trial of aspirin in cerebral ischemia.

Authors:  W S Fields; N A Lemak; R F Frankowski; R J Hardy
Journal:  Stroke       Date:  1977 May-Jun       Impact factor: 7.914

7.  A comparison of imidazole and 9,11-azoprosta-5,13-dienoic acid. Two selective thromboxane synthetase inhibitors.

Authors:  F A Fitzpatrick; R R Gorman
Journal:  Biochim Biophys Acta       Date:  1978-03-01

8.  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

9.  Diversion of prostaglandin endoperoxide metabolism by selective inhibition of thromboxane A2 biosynthesis in lung, spleen or platelets.

Authors:  F P Nijkamp; S Moncada; H L White; J R Vane
Journal:  Eur J Pharmacol       Date:  1977-07-15       Impact factor: 4.432

10.  Inhibition of human platelet thromboxane synthetase by 9,11-azoprosta-5,13-dienoic acid.

Authors:  R R Gorman; G L Bundy; D C Peterson; F F Sun; O V Miller; F A Fitzpatrick
Journal:  Proc Natl Acad Sci U S A       Date:  1977-09       Impact factor: 11.205
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  19 in total

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Authors:  Harold J Ting; Wallace J Murray; Fadi T Khasawneh
Journal:  Acta Pharmacol Sin       Date:  2010-02       Impact factor: 6.150

Review 2.  Current concepts for a drug-induced inhibition of formation and action of thromboxane A2.

Authors:  H Patscheke
Journal:  Blut       Date:  1990-05

3.  Solubilization of a thromboxane A2/prostaglandin H2 antagonist binding site from human platelets.

Authors:  R M Burch; D E Mais; D L Saussy; P V Halushka
Journal:  Proc Natl Acad Sci U S A       Date:  1985-11       Impact factor: 11.205

4.  Pinane thromboxane A2 analogues are non-selective prostanoid antagonists in rat and human stomach muscle.

Authors:  A Bennett; G J Sanger
Journal:  Br J Pharmacol       Date:  1982-12       Impact factor: 8.739

5.  Triggering by Paf-acether and adrenaline of cyclo-oxygenase-independent platelet aggregation.

Authors:  F Fouque; B B Vargaftig
Journal:  Br J Pharmacol       Date:  1984-11       Impact factor: 8.739

Review 6.  Current issues in thrombosis prevention with antiplatelet drugs.

Authors:  G de Gaetano; C Cerletti; E Dejana; J Vermylen
Journal:  Drugs       Date:  1986-06       Impact factor: 9.546

7.  Acetyl glyceryl ether phosphorylcholine-stimulated human platelets cause pulmonary hypertension and edema in isolated rabbit lungs. Role of thromboxane A2.

Authors:  J E Heffner; S A Shoemaker; E M Canham; M Patel; I F McMurtry; H G Morris; J E Repine
Journal:  J Clin Invest       Date:  1983-02       Impact factor: 14.808

8.  Binding of a radioiodinated 13-azapinane thromboxane antagonist to platelets: correlation with antiaggregatory activity in different species.

Authors:  S Narumiya; M Okuma; F Ushikubi
Journal:  Br J Pharmacol       Date:  1986-06       Impact factor: 8.739

9.  Gram-positive bacteria-induced granulocytopenia and pulmonary leukostasis in rabbits.

Authors:  S E Goldblum; W P Reed
Journal:  Infect Immun       Date:  1982-07       Impact factor: 3.441

10.  Elevated thromboxane levels in the rat during endotoxic shock: protective effects of imidazole, 13-azaprostanoic acid, or essential fatty acid deficiency.

Authors:  J A Cook; W C Wise; P V Halushka
Journal:  J Clin Invest       Date:  1980-01       Impact factor: 14.808
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