Biochemical and pharmacological properties of a new topical anti-inflammatory compound, 9-phenylnonanohydroxamic acid (BMY 30094)
| Autor: | Paul L. Stanley, Kenneth M. Tramposch, Fred Christopher Zusi, Steiner Stephen A, J. W. Quigley, Suresh A. Marathe, Xina Nair |
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| Rok vydání: | 1990 |
| Předmět: |
Male
Immunology Inflammation Arachidonic Acids Pharmacology Administration Cutaneous Arachidonate 12-Lipoxygenase Carrageenan Hydroxamic Acids Toxicology Mice chemistry.chemical_compound Lipoxygenase Psoriasis medicine Animals Pharmacology (medical) IC50 Chromatography High Pressure Liquid ED50 Arachidonate 5-Lipoxygenase Arachidonic Acid Molecular Structure biology Anti-Inflammatory Agents Non-Steroidal Rats Inbred Strains Exudates and Transudates medicine.disease Rats chemistry Prostaglandin-Endoperoxide Synthases biology.protein Eicosanoids Tetradecanoylphorbol Acetate Female Arachidonic acid Cyclooxygenase medicine.symptom |
| Zdroj: | Agents and Actions. 30:443-450 |
| ISSN: | 1420-908X 0065-4299 |
| DOI: | 10.1007/bf01966310 |
| Popis: | 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: | OpenAIRE |
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