新しいアトピ-性疾患治療剤,N-(3′,4′-dimethoxycinnamoyl)anthranilic acid(N-5′)の薬理学的性質-5-分離ラット腹腔細胞からのHistamine遊離におよぼす影響

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The allergic histamine release mediated by homocytotropic antibody (HTA) was significantly inhibited by 100 and 1, 000 μM N-5', but was little affected by the drug at concentrations of 1 and 10, μM. Disodium cromoglycate (DSCG) showed a potent inhibition of the histamine release at concentrations of 10 and 100 μM, in a concentration dependent manner. Although a significant inhibition of histamine release was elicited by 1, 000 μM DSCG, the effect was less potent than that by 100 μM of the drug. One μM DSCG had no effect. Allergic histamine release as well as a spontaneous one without antigen was significantly potentiated by addition of 1 μM phosphatidylserine. The inhibitory activity of N-5' was unchanged by phosphatidylserine, while the activity of DSCG was significantly reduced in the presence of phosphatidylserine. The inhibitory activity of N-5' on the allergic histamine release was unchanged by glucose, while the activity of papaverine was significantly enhanced in the absence of glucose. N-5' showed little effect on the histamine release induced by compound 48/80, while DSCG showed a concentration dependent inhibition of the release. Phosphatidylserine or dextran alon induced only slight release of histamine from peritoneal exudate cells. However, the release was significantly potentiated by the combined treatment with phosphatidylserine and dextran. N-5' (10 to 100 μM) showed a significant inhibition of the release, in a concentration dependent manner. Although the inhibitory action of DSCG was significant even at a concentration of 1 μM, the action did not increasewith an increase in concentration of the drug. N-5' was more potent than DSCG. Approximately 25% histamine release was induced by phospholipase-A (10, μg/ml). N-5' at concentrations of 100 and 1, 000 μMshowed a significant inhibition (42.0 and 62.6%, respectively) of the release. In the case of DSCG, the inhibition percent was calculated to be 30.5 and 37.9% at the same levels of concentration as N-5'. DSCG had no effect on the phospholipase-A activity at any concentration tested herein, while N-5' at a concentration of 1, 000 μM showed a significant inhibition (23%).

新しいアトピ-性疾患治療剤,N-(3′,4′-dimethoxycinnamoyl)anthranilic acid(N-5′)の薬理学的性質-5-分離ラット腹腔細胞からのHistamine遊離におよぼす影響

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