Pharmacological properties of N- (3',4'-dimethoxycinnamoyl) anthranilic acid (N-5') , a new anti-atopic agent. (5) .--Influence of N-5' on the histamine release from peritoneal exudate cells
Nakazawa, M.; Yoshimura, T.; Naito, J.; Azuma, H.
Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica 74(4): 483-490
1978
ISSN/ISBN: 0015-5691 PMID: 81163 Document Number: 133478
The allergic histamine release mediated by homocytotropic antibody (HTA) was significantly inhibited by 100 and 1000 .mu.M N-5', but was affected little by the drug at 1 and 10 .mu.M. Disodium cromoglycate (DSCG) showed a potent inhibition of histamine release at concentrations of 10 and 100 .mu.M in a concentration-dependent manner. Although a significant inhibition of histamine release was elicited by 1000 .mu.M DSCG, the effect was less potent than that by 100 .mu.M of the drug. One .mu.M DSCG had no effect. Allergic histamine release and spontaneous histamine release (without antigen) was significantly potentiated by addition of 1 .mu.M 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 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 peritoneal exudate cells. The release was significantly potentiated by the combined treatment with phosphatidylserine and dextran. N-5' (10-100 .mu.M) 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 .mu.M, the action did not increase with an increase in concentration of the drug. N-5' was more potent than DSCG. Approximately 25% histamine release was induced by phospholipase-A (10 .mu.g/ml). N-5' at concentrations of 100 and 1000 .mu.M showed a significant inhibition (42.0% and 62.6%, respectively) of the release. In the case of DSCG, the inhibition 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, while N-5' at a concentration of 1000 .mu.M showed a significant inhibition (23%).