Multiple effects of a new anti-inflammatory agent, timegadine, on arachidonic acid release and metabolism in neutrophils and platelets.

Abstract:

:Casein-elicited rat peritoneal polymorphonuclear leukocytes (PMNL) and rabbit platelets were prelabelled with [1-14C]arachidonic acid, and the effect of timegadine, a new anti-inflammatory agent, on the release and metabolism of arachidonic acid induced by A23187 (PMNL) and thrombin (platelets) was studied and compared with the effect of other compounds reported to affect these enzymatic mechanisms. Timegadine inhibited arachidonic acid release from both cells (IC50 = 2.7 X 10(-5) M), the lipoxygenase activity in PMNL (IC50 = 4.1 X 10(-5) M) and the cyclooxygenase activity in platelets (IC50 = 3.1 X 10(-8) M). By these mechanisms, PMNL leukotriene B4 formation was inhibited by 50% at 2.0 X 10(-5) M, platelet thromboxane B2 at 3.2 X 10(-8) M, and platelet 12-HETE at 4.9 X 10(-5) M. These effects might add to the understanding of the anti-inflammatory properties of timegadine.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Ahnfelt-Rønne I,Arrigoni-Martelli E

doi

10.1016/0006-2952(82)90708-0

subject

Has Abstract

pub_date

1982-08-15 00:00:00

pages

2619-24

issue

16

eissn

0006-2952

issn

1873-2968

pii

0006-2952(82)90708-0

journal_volume

31

pub_type

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