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 Pharmacoljournal_title
Biochemical pharmacologyauthors
Ahnfelt-Rønne I,Arrigoni-Martelli Edoi
10.1016/0006-2952(82)90708-0subject
Has Abstractpub_date
1982-08-15 00:00:00pages
2619-24issue
16eissn
0006-2952issn
1873-2968pii
0006-2952(82)90708-0journal_volume
31pub_type
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