This experiment was an attempt to investigate the influence of N-(3′, 4′-dimethoxycinnamoyl) anthranilic acid (N-5′) on the synthesis, release and degradation of histamine, and following results were obtained. 1) N-5′only at a concentration of 1000μM showed about 58% inhibition on histamine formation mediated by crude gastric histidine decarboxylase of rats. However, the enzyme activity was unaffected by an I.p. injection of N-5′at a dose of 200mg/kg or less. 2) N-5′at concentrations of 100 and 1000μM showed a significant inhibition (about 51 and 95%, respectively) of the histamine release from peritoneal cells mediated by HTA, while the drug did not affect the spontaneous histamine release and that by compound 48/80 at a concentration sufficient to elicit an inhibition of the allergic histamine release. 3) N-5′only at a concentration of 1000μM showed about 44% inhibition on histamine degradation mediated by crude histaminase from rat duodenum. 4) Histamine levels in whole blood, peritoneal cells, lung, trachea and spleen of rat were hardly changed by an oral administration of N-5′at a dose of 600mg/kg or less.
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