Preclinical and Clinical Activity of Zileuton and A-78773
| Autor: | Andrew O. Stewart, George W. Carter, P. Rubin, C. Lanni, Randy L. Bell, Robert S. Hansen, Dee W. Brooks, P. E. Malo |
|---|---|
| Rok vydání: | 2006 |
| Předmět: |
Male
Allergy Guinea Pigs Inflammation Pharmacology Leukotriene B4 Inflammatory bowel disease General Biochemistry Genetics and Molecular Biology Bronchospasm History and Philosophy of Science Edema medicine Animals Hydroxyurea Lipoxygenase Inhibitors Lung Whole blood Bronchial Spasm business.industry General Neuroscience Zileuton medicine.disease Rats Bronchoconstriction medicine.symptom business medicine.drug |
| Zdroj: | Annals of the New York Academy of Sciences. 696:205-215 |
| ISSN: | 1749-6632 0077-8923 |
| Popis: | The importance of leukotrienes as mediators of inflammation and bronchoconstriction was examined with two recently described 5-lipoxygenase inhibitors, zileuton and A-78773. Preclinical evaluation of these two molecules indicates that they are potent, selective, direct, reversible inhibitors of 5-lipoxygenase with activity in a variety of purified cells and in more complex biological systems such as whole blood, lung fragments, and tracheal tissues. In various animals models of inflammation and allergy, the molecules inhibited edema, inflammatory cell influx, and bronchospasm. These observations are consistent with the recent clinical success of zileuton in treating asthma and inflammatory bowel disease. In all preclinical systems tested thus far, A-78773 is more potent and longer acting than zileuton, indicating that the molecule could be even more effective in the clinic than zileuton and that both molecules are useful tools in defining the role of leukotrienes in preclinical and clinical settings. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Plný text