Literature DB >> 558637

Imidazole: a selective inhibitor of thromboxane synthetase.

S Moncada, S Bunting, K Mullane, P Thorogood, J R Vane, A Raz, P Needleman.   

Abstract

Imidazole inhibits the enzymic conversion of the endoperoxides (PGG2 and PGH2) to thromboxane A2 by platelet microsomes (IC50: 22 MICRONG/ML; DETERMINED BY BIOASSAY). The inhibitor is selective, for prostaglandin cyclo-oxygenase is only affected at high doses. Radiochemical data confirms that imidazole blocks the formation of 14C-thromboxane B2 from 14C-PGH2. Several imidazole analogues and other substances were tested but only 1-methyl-imidazole was more potent than imidazole itself. The use of imidazole to inhibit thromboxane formation could help to elucidate the role of thromboxanes in physiology or pathophysiology.

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Year:  1977        PMID: 558637     DOI: 10.1016/0090-6980(77)90232-5

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


  45 in total

Review 1.  Thromboxane synthase inhibitors and receptor antagonists.

Authors:  J Vermylen; H Deckmyn
Journal:  Cardiovasc Drugs Ther       Date:  1992-02       Impact factor: 3.727

Review 2.  Adventures in vascular biology: a tale of two mediators.

Authors:  S Moncada
Journal:  Philos Trans R Soc Lond B Biol Sci       Date:  2006-05-29       Impact factor: 6.237

3.  The effects of the protein synthesis inhibitor anisomycin on the febrile responses to intracerebroventricular injections of bacterial pyrogen, arachidonic acid and prostaglandin E2.

Authors:  A S Milton; V K Sawhney
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1987-09       Impact factor: 3.000

4.  Hypersensitivity to methoxamine in atria isolated from streptozotocin-induced diabetic rats.

Authors:  L Canga; L Sterin-Borda
Journal:  Br J Pharmacol       Date:  1986-01       Impact factor: 8.739

5.  Pharmacologic characterization of immune complex induced bronchoconstriction in guinea pigs.

Authors:  Z E Mielens; E W Ferguson; R A Ferrari
Journal:  Agents Actions       Date:  1981-12

6.  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

7.  Prostaglandin biosynthesis in pulmonary macrophages.

Authors:  W Hsueh
Journal:  Am J Pathol       Date:  1979-10       Impact factor: 4.307

8.  Platelet and blood vessel arachidonate metabolism and interactions.

Authors:  P Needleman; A Wyche; A Raz
Journal:  J Clin Invest       Date:  1979-02       Impact factor: 14.808

9.  13-Azaprostanoic acid: a specific antagonist of the human blood platelet thromboxane/endoperoxide receptor.

Authors:  G C Le Breton; D L Venton; S E Enke; P V Halushka
Journal:  Proc Natl Acad Sci U S A       Date:  1979-08       Impact factor: 11.205

10.  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

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