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- W218205731 abstract "The allergic mediator release inhibitor CI-922 (3,7-dimethoxy-4-phenyl-N-1H-tetrazol-5-yl-4H-furo(3,2-b)indole-2-carboxamide) is a potent inhibitor of human neutrophil (PMN) respiratory and secretory responses in vitro. At concentrations from 1 to 100 micromolar, CI-922 inhibits activation of PMNs by agents which stimulate phospholipase C-dependent phosphoinositide hydrolysis to generate the second messengers inositol 1,4,5 trisphosphate and diacylglycerol, including: the plasma membrane receptor-specific ligands fMet-Leu-Phe and C5a; concanavalin A; and the guanine nucleotide regulatory protein-specific stimulus GTPgammaS. In contrast, CI-922 does not inhibit PMN responses to protein kinase C-specific stimuli such as phorbol myristate acetate (PMA) or sn-1,2-dioctanoyl-glycerol. CI-922 is also unable to inhibit the synergistic activation of PMNs by suboptimal concentrations of PMA and calcium ionophore A23187. These results suggest that CI-922 inhibits PMN activation at a site distal to signal transduction through the guanine nucleotide regulatory protein required for second messenger generation but proximal cophosphorylation reactions mediated by protein kinase C and calcium/calmodulin-dependent protein kinases." @default.
- W218205731 created "2016-06-24" @default.
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- W218205731 date "1986-03-05" @default.
- W218205731 modified "2023-09-24" @default.
- W218205731 title "Mechanism of inhibition of human neutrophil activation by the allergic mediator release inhibitor, CI-922" @default.
- W218205731 hasPublicationYear "1986" @default.
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