Abstract:
:Three grams of nafazatrom (Bay g 6575), given orally to healthy male volunteers in a single dose, significantly reduce the formation of leukotriene B4 in polymorphonuclear leukocytes. LTB4 synthesis fell from 57.1 +/- 17.0 ng/10(7) PMNL, mean +/- S.D., in control to 34.3 +/- 14.4 ng/10(7) PMNL 3 hr after nafazatrom (2 P less than 0.001). In vitro, nafazatrom inhibited LTB4 formation in human PMNL in a dose dependent manner. At 1 microM nafazatrom LTB4 formation was reduced to 65% of the control value. Nafazatrom had no effect on the excretion of 2,3-dinor-6-keto-PGF1 alpha and 2,3-dinor-TXB2, the major urinary metabolites of endogenously synthesized PGI2 and TXA2, respectively. Serum levels of TXB2 in clotted whole blood also remained unchanged. The inhibitory effect of nafazatrom on leukotriene biosynthesis in human PMNL suggests a therapeutic potential of this drug in processes like allergy and chronic inflammation, where leukotrienes play a pathogenetic role.
journal_name
Biochem Pharmacoljournal_title
Biochemical pharmacologyauthors
Strasser T,Fischer S,Weber PCdoi
10.1016/0006-2952(85)90304-1subject
Has Abstractpub_date
1985-06-01 00:00:00pages
1891-4issue
11eissn
0006-2952issn
1873-2968pii
0006-2952(85)90304-1journal_volume
34pub_type
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journal_title:Biochemical pharmacology
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journal_title:Biochemical pharmacology
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journal_title:Biochemical pharmacology
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更新日期:2003-12-01 00:00:00