Pulmonary actions of LY255283, a leukotriene B4 receptor antagonist
| Autor: | David K. Herron, Steven A. Silbaugh, Theodore Goodson, Carlos R. Roman, Jerome H. Fleisch, Stephen M. Spaethe, Sandra L. Cockerham, David L. Saussy, Peter W. Stengel |
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| Rok vydání: | 1992 |
| Předmět: |
Male
medicine.medical_specialty Thromboxane medicine.drug_class Leukotriene B4 Guinea Pigs Receptors Leukotriene B4 Tetrazoles In Vitro Techniques Biology Dinoprostone Radioligand Assay Thromboxane A2 chemistry.chemical_compound Internal medicine medicine Animals Receptors Immunologic Lung Pharmacology Analgesics Leukotriene Membranes Pulmonary Gas Exchange Leukotriene B4 receptor Antagonist respiratory system Receptor antagonist Prostaglandin Endoperoxides Synthetic respiratory tract diseases Airway Obstruction Endocrinology chemistry 15-Hydroxy-11 alpha 9 alpha-(epoxymethano)prosta-5 13-dienoic Acid lipids (amino acids peptides and proteins) Lung Volume Measurements Histamine Muscle Contraction |
| Zdroj: | European Journal of Pharmacology. 223:57-64 |
| ISSN: | 0014-2999 |
| DOI: | 10.1016/0014-2999(92)90818-o |
| Popis: | The actions of LY255283, a leukotriene (LT) B4 receptor antagonist, were examined on guinea pig lung. LTB4 and LY255283 displaced [3H]LTB4 from its binding site on lung membranes with pKi values of 9.9 and 7.0, respectively. In the functional correlate of the binding studies, LY255283 competitively reduced contractile responses of lung parenchyma to LTB4 (pA2 = 7.2). LTB4 produced airway obstruction which was reduced by LY255283 administered i.v. (ED50 = 2.8 mg/kg) or orally (ED50 = 11.0 mg/kg). Contractile responses to histamine, LTD4 and the thromboxane mimetic, U46619, were not reduced by LY255283. The compound also did not inhibit cyclooxygenase or 5-lipoxygenase enzymes. We conclude that LY255283 selectively antagonized pharmacologic responses to LTB4 on lung tissue and appears to be a useful tool to investigate the role of LTB4 in pulmonary disease. |
| Databáze: | OpenAIRE |
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