Inhibition of IgE-Mediated N-Acetylglucosaminidase and Serotonin Release from Rat Basophilic Leukemia Cells (RBL-2H3) by Tenidap: A Novel Anti-Inflammatory Agent

Abstract
Tenidap [(Z)-5-chloro-2,3-dihydro-3-(hydroxy-2-thienylmethylene)-2-oxo-1H-indole-1-carboxamide] is a novel anti-inflammatory compounds of the oxindole class that currently is undergoing clinical evaluation in man. Here we demonstrate that the tenidap inhibits (IC50 = .apprx.10 .mu.M) IgE-mediated secretion of granule constituents from the rat mast cell tumor line RBL-2H3. The inhibitory effect is rapid in onset, readily reversible, and appears to be unique when compared to a representative selection of other acidic (carboxylic acids, pyrazoles and oxicams) nonsteroidal anti-inflammatory compounds.

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