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Mechanism of inhibition of cyclo-oxygenase in human blood platelets by carbamate insecticides.

Biochem. J. 250, 103-110 (1988)
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Carbamates are a widely used class of insecticides and herbicides. They were tested for their ability to affect human blood platelet aggregation and arachidonic acid metabolism in platelets. (1) The herbicides of the carbamate type have no, or only little, influence up to a concentration of 100 μM; the carbamate insecticides, however, inhibit both aggregation and arachidonic acid metabolism in a dose- and time-dependent manner. (2) Carbaryl, the most effective compound, inhibits platelet aggregation and cyclo-oxygenase activity completely at 10 μM. The liberation of arachidonic acid from phospholipids and the lipoxygenase pathway are not affected, whereas the products of the cyclo-oxygenase pathway are drastically decreased. (3) By using [14C]carbaryl labelled in the carbamyl or in the ring moiety, it could be proved that the carbamyl residue binds covalently to platelet proteins. In contrast with acetylsalicylic acid, which acetylates only one protein, carbaryl carbamylates a multitude of platelet proteins. (4) One of the carbamylated proteins was found to be the platelet cyclo-oxygenase, indicating that carbaryl resembles in this respect acetylsalicylic acid, which is known to inhibit this enzyme specifically by acetylation.
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Publication type Article: Journal article
Document type Scientific Article
Language english
Publication Year 1988
HGF-reported in Year 0
ISSN (print) / ISBN 0264-6021
e-ISSN 1470-8728
Quellenangaben Volume: 250, Issue: 1, Pages: 103-110 Article Number: , Supplement: ,
Publisher Portland Press
Reviewing status Peer reviewed
Institute(s) Institut für Toxikologie und Biochemie
PubMed ID 3128272
Scopus ID 0023902811
Erfassungsdatum 1988-12-31