一种口服有效药剂[[3-(1H-四唑-5-基)-苯基]氨基]氧代乙酸正丁酯的抗过敏特性。

Antiallergic properties of an orally effective agent, [[3-(1H-tetrazol-5-yl)-phenyl] amino] oxoacetic acid n-butyl ester.

作者信息

Agata M, Goto H, Tsuriya Y, Tachibana K, Kuroda T

出版信息

Jpn J Pharmacol. 1982 Aug;32(4):689-97. doi: 10.1254/jjp.32.689.

DOI:10.1254/jjp.32.689

Abstract

A newly synthesized compound, [[3-(1H-tetrazol-5-yl)-phenyl] amino]oxoacetic acid n-butyl ester (MTB) has been demonstrated to be an orally active antiallergic agent. This compound inhibited the 48-hr passive cutaneous anaphylaxis (48-hr PCA) induced by IgE in rats. In guinea pigs, MTB also inhibited the 8-day passive cutaneous anaphylaxis (8-day PCA) and the 8-day passive systemic anaphylaxis induced by IgE. The compound partially inhibited the IgG-mediated 3-hr PCA in rats and guinea pigs, but failed to have any effect on the rabbit IgG-mediated 3-hr PCA in these animals. In the rat, MTB was not an antagonist of histamine or serotonin. The antiallergic effect of MTB was not mediated via any adrenergic mechanisms. MTB significantly inhibited histamine release from rat peritoneal cells induced by rat IgE in vitro.

摘要

一种新合成的化合物，[[3-(1H-四唑-5-基)-苯基]氨基]氧代乙酸正丁酯（MTB）已被证明是一种口服活性抗过敏剂。该化合物抑制了大鼠中由IgE诱导的48小时被动皮肤过敏反应（48小时PCA）。在豚鼠中，MTB还抑制了由IgE诱导的8天被动皮肤过敏反应（8天PCA）和8天被动全身过敏反应。该化合物部分抑制了大鼠和豚鼠中IgG介导的3小时PCA，但对这些动物中兔IgG介导的3小时PCA没有任何影响。在大鼠中，MTB不是组胺或5-羟色胺的拮抗剂。MTB的抗过敏作用不是通过任何肾上腺素能机制介导的。MTB显著抑制了体外大鼠IgE诱导的大鼠腹膜细胞组胺释放。