ono-4057 has been researched along with Inflammation* in 3 studies
3 other study(ies) available for ono-4057 and Inflammation
Article | Year |
---|---|
(E)-3-[[[[6-(2-carboxyethenyl)-5-[[8-(4- methoxyphenyl)octyl]oxy]-2-pyridinyl]-methyl]thio]methyl]benzoic acid: a novel high-affinity leukotriene B4 receptor antagonist.
Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Benzoates; Calcium; Humans; Inflammation; Leukotriene B4; Mice; Molecular Structure; Neutrophils; Pyridines; Receptors, Leukotriene B4 | 1993 |
ONO-4057, a novel, orally active leukotriene B4 antagonist: effects on LTB4-induced neutrophil functions.
ONO-4057(5-[2-(2-Carboxyethyl)-3-[6-(4-methoxyphenyl)-5E- hexenyl]oxyphenoxy]valeric acid), an orally active leukotriene B4(LTB4) antagonist, displaced the binding of [3H] LTB4 to the LTB4 receptor in human neutrophil (Ki = 3.7 +/- 0.9 nM). ONO-4057 inhibited the LTB4-induced rise in cytosolic free calcium (the concentration causing 50% inhibition (IC50) = 0.7 +/- 0.3 microM) and inhibited human neutrophil aggregation, chemotaxis or degranulation induced by LTB4 (IC50 = 3.0 +/- 0.1, 0.9 +/- 0.1 and 1.6 +/- 0.1 microM) without showing any agonist activity at concentration up to 30 microM. ONO-4057 did not inhibit fMLP or C5a-induced neutrophil activation at concentrations up to 30 microM. In the in vivo study, ONO-4057 given orally, prevented LTB4-induced transient neutropenia or intradermal neutrophil migration in guinea pig (the dose causing 50% efficacy (ED50) = 25.6mg/kg or 5.3mg/kg). Furthermore, ONO-4057 given topically, suppressed phorbol-12-myristate-13-acetate (PMA)-induced neutrophil infiltration in guinea pig ear (the effective dose = 1 mg/ear). These results indicate that ONO-4057 is a selective and orally active LTB4 antagonist and may be a potential candidate for the treatment of various inflammatory diseases. Topics: Animals; Calcium; Cell Aggregation; Chemotaxis, Leukocyte; Complement C5a; Cytoplasmic Granules; Guinea Pigs; Humans; Inflammation; Leukotriene B4; Male; N-Formylmethionine Leucyl-Phenylalanine; Neutropenia; Neutrophils; Phenylpropionates; Receptors, Immunologic; Receptors, Leukotriene B4; Tetradecanoylphorbol Acetate | 1992 |
Leukotriene C4 D4 antagonist markedly reduced inflammation in a rat model of inflammatory bowel disease.
Topics: Animals; Chromones; Colon; Inflammation; Inflammatory Bowel Diseases; Methacrylates; Phenylpropionates; Rats; SRS-A | 1992 |