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Journals and Conferences
A series of 4,5-diarylimidazoline libraries were prepared using high-throughput solid-phase and microwave techniques. The compounds were evaluated as P2X(7) antagonists and their SAR is described.
This article describes the novel pharmacological activity of MDL 28,753, a compound designed as a potential receptor antagonist of the peptidoleukotrienes. In the isolated longitudinal muscle of the guinea pig ileum, MDL 28,753 was a full agonist at the leukotriene (LT) D4 receptor and had a pD2 of 8.9 compared with a pD2 of 9.2 for LTD4. The contraction… (More)
A series of azachalcones was evaluated for ability to affect secretion of myeloperoxidase by rat polymorphonuclear leukocytes stimulated by fMLP. The compounds were found to interfere with cellular uptake of extracellular calcium. Structure-activity relationships are discussed.
[(Octahydro-2-oxo-7-tetradecylidene-2H-1-benzopyran-8-yl)thio]acet ic acid (MDL 43,291) is a novel leukotriene (LT) receptor antagonist. It is a competitive antagonist of LTD4 (pA2 = 6.7) and LTE4 (pA2 = 6.7) and an apparent noncompetitive inhibitor of LTC4 ('pseudo' pA2 = 6.8) in the longitudinal muscle of the guinea pig ileum. At concentrations that… (More)