abbott-41988 has been researched along with Shock* in 1 studies
1 other study(ies) available for abbott-41988 and Shock
Article | Year |
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Synthesis and structure-activity relationships of a series of novel benzopyran-containing platelet activating factor antagonists.
A class of N-substituted tetrahydrobenzopyrano[3,4-c]pyridines, I, have been identified as antagonists of platelet activating factor (PAF). The structural features essential for PAF binding were determined by systematic modification of three sites in the molecule. While O-alkyl analogues had little effect on binding potency, N-alkyl analogues exhibited a wide range of activity. Structural changes in the core ring system generally resulted in a loss of binding activity. Optimization of the N- and O-substituents resulted in the analogues 25-27 which exhibited Ki values ranging between 131 and 167 nM in a [3H]PAF binding assay. Compound 23 was also active in a model of PAF-induced shock in the mouse following intravenous administration. Topics: Alkylation; Animals; Benzopyrans; Binding Sites; Blood Platelets; Bridged Bicyclo Compounds; Cell Membrane; Cytoplasmic Granules; Male; Mice; Molecular Structure; Platelet Activating Factor; Platelet Membrane Glycoproteins; Pyridines; Rabbits; Receptors, Cell Surface; Receptors, G-Protein-Coupled; Shock; Structure-Activity Relationship | 1992 |