| Autor: |
Tramposch KM; Bristol-Myers Squibb Co., Pharmaceutical Research and Development Division, Buffalo, New York 14213., Zusi FC, Marathe SA, Stanley PL, Nair X, Steiner SA, Quigley JW |
| Jazyk: |
angličtina |
| Zdroj: |
Agents and actions [Agents Actions] 1990 Jun; Vol. 30 (3-4), pp. 443-50. |
| DOI: |
10.1007/BF01966310 |
| Abstrakt: |
Drugs which block the biosynthesis of leukotrienes and prostaglandins may have potential in the treatment of psoriasis and other skin diseases. The biochemical and anti-inflammatory activity of 9-phenylnonanohydroxamic acid (BMY 30094) is described. BMY 30094 inhibited human neutrophil 5-lipoxygenase with an IC50 of 5.7 microM. BMY 30094 also blocked human platelet cyclooxygenase and lipoxygenase with IC50 values of 15.2 and 15.0 microM, respectively. Topical application of this compound blocked arachidonic acid and 12-O-tetradecanoylphorbol ester-induced mouse skin inflammation with activity comparable to that observed for lonapalene. The topical ED50 for BMY 30094 in the arachidonic acid-induced inflammation model is 2.2 mumoles/ear. In the sub-cutaneous carrageenan sponge assay in rats, BMY 30094 blocked LTB4 and PGE2 production and inhibited neutrophil migration. This compound would be a useful tool to determine the role of arachidonic acid metabolites in the etiology of inflammatory dermatoses. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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