PHARMACOLOGICAL PROPERTIES OF N-(3',4'-DIMETHOXYCINNAMOYL) ANTHRANILIC ACID (N-5'), A NEW ANTI-ATOPIC AGENT
PHARMACOLOGICAL PROPERTIES OF N-(3',4'-DIMETHOXYCINNAMOYL) ANTHRANILIC ACID (N-5'), A NEW ANTI-ATOPIC AGENT
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DOI：
10.1111/j.1476-5381.1976.tb08614.x
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发表时间：
1976-01-01
影响因子：
7.3
通讯作者：
YOSHIMURA, T
中科院分区：
文献类型：
--
作者：
AZUMA, H;BANNO, K;YOSHIMURA, T
1 N-(3‘-4’-二甲氧基肉桂酰基)邻氨基苯甲酸(N-5‘)对嗜同型细胞抗体(HTA)介导的被动皮肤过敏反应(PCA)有明显的抑制作用，且呈剂量依赖关系，但不受抗炎药苯丁酮、吲哚美辛和强的松龙的影响。联苯双胺和赛庚啶联合应用可显著抑制HTA诱导的PCa。2个剂量的N-5‘可有效抑制HTA诱导的PCA，但对抗牛血清白蛋白(BSA)兔血清产生的异种PCA仅有轻微抑制作用。苯丁酮、吲哚美辛和强的松龙可明显抑制这种异种PCA。苯乙双胺和赛庚啶单独或联合对异种前列腺癌的抑制作用较弱。3组胺和5-羟色胺引起的血管通透性增加可被二苯二胺或赛庚啶显著抑制，但N-5‘和所用抗炎药对此无明显影响。4N-5‘150 mg/kg灌胃对角叉菜胶致大鼠足肿胀的抑制作用约为26%，而苯丁酮、吲哚美辛和强的松龙对角叉菜胶致大鼠足肿胀有明显的抑制作用。5-N-5‘对HTA诱导的大鼠腹膜细胞组胺释放有明显的抑制作用(分别为52%和95%)，10umN-5’对HTA诱导的大鼠腹膜细胞组胺释放无明显影响。组胺释放在1000um时被苯丁酮或消炎痛抑制，而在100um时不受抑制。在所使用的任何浓度下，强的松龙对组胺释放都没有影响。6上述结果提示，N-5‘对HTA诱导的PCA的抑制作用可能与抑制组胺释放有关，与抗炎药苯丁酮、吲哚美辛和强的松龙的作用明显不同。
1 N-(3'-4'-dimethoxycinnamoyl) anthranilic acid (N-5') exhibited a dose-dependent, potent inhibition of the passive cutaneous anaphylaxis (PCA) mediated by homocytotropic antibodies (HTA), which was hardly affected by anti-inflammatory agents such as phenylbutazone, indomethacin and prednisolone at any dose used. The HTA-induced PCA was significantly inhibited by combined treatment with diphenydramine and cyproheptadine. 2 Doses of N-5' which potently inhibited HTA-induced PCA inhibited only slightly the heterologous PCA produced by anti-bovine serum albumin (BSA) rabbit serum. This heterologous PCA was clearly inhibited by phenylbutazone, indomethacin and prednisolone. Diphenydramine and cyproheptadine, singly or combined inhibited the heterologous PCA only slightly. 3 The increased vascular permeability caused by histamine and 5-hydroxytryptamine was significantly inhibited by diphenyldramine or cyproheptadine, but not by N-5' and the anti-inflammatory agents used. 4 N-5' 150 mg/kg orally inhibited rat paw oedema induced by carrageenin by about 26% while phenylbutazone, indomethacin and prednisolone produced significant inhibition. 5 N-5' at concentrations of 100 and 1000 muM significantly inhibited (by about 52% and 95%, respectively) the histamine release from rat peritoneal cells induced by HTA; 10 muM N-5' had little effect. Histamine release was inhibited by phenylbutazone or indomethacin at 1000 muM but not at 100 muM. Prednisolone had no effect on histamine release at any of the concentrations used. 6 These findings suggest that the inhibition of the HTA-induced PCA by N-5' may be due to inhibition of histamine release and is clearly different from the actions of anti-inflammatory agents such as phenylbutazone, indomethacin and prednisolone.