一种新型口服活性抗过敏药物：吡啶并[1,2-a]嘧啶，UCB L140（奇诺因1045）在大鼠体内的药理学

Pharmacology of a new orally active antiallergic: pyrido[1,2-a]pyrimidine, ucb L140 (CHINOIN 1045) in rats.

作者信息

De Vos C, Dessy F, Hermecz I, Meszaros Z, Breining T

出版信息

Int Arch Allergy Appl Immunol. 1982;67(4):362-8. doi: 10.1159/000233048.

Abstract

ucb L140 (CHINOIN 1045) has been tested in various rat anaphylaxis systems. In models of passive cutaneous anaphylaxis (PCA), passive peritoneal anaphylaxis (PPA) and anaphylactic bronchospasms, ucb L140 appears to be more potent than sodium cromoglycate (DSCG). Upon oral administration, ucb L140 exhibits a marked inhibition of these anaphylactic reactions. Sensitized rat mast cells in vitro display a decreased Nippostrongylus-induced histamine release when treated with a concentration of ucb L140 three times smaller than DSCG. In PCA testing after intravenous administration of ucb L140 a cross-tachyphylaxis with DSCG was observed. These results suggest that the action of ucb L140 is similar to that of DSCG in inhibiting the release of allergic mediators from mast cells and therefore may present antiallergic activity.

摘要

ucb L140（奇诺因1045）已在多种大鼠过敏反应系统中进行了测试。在被动皮肤过敏反应（PCA）、被动腹膜过敏反应（PPA）和过敏性支气管痉挛模型中，ucb L140似乎比色甘酸钠（DSCG）更有效。口服给药后，ucb L140对这些过敏反应表现出显著的抑制作用。体外致敏的大鼠肥大细胞在接受比DSCG小三倍浓度的ucb L140处理时，显示出由类圆线虫诱导的组胺释放减少。在静脉注射ucb L140后的PCA测试中，观察到与DSCG的交叉快速减敏现象。这些结果表明，ucb L140在抑制肥大细胞释放过敏介质方面的作用与DSCG相似，因此可能具有抗过敏活性。