Grupe R, Pietzsch W
Institute of Pharmacological Research, VEB of the Pharmaceutical Kombinat GERMED, Berlin-Friedrichsfelde, GDR.
Agents Actions. 1988 Apr;23(3-4):324-7. doi: 10.1007/BF02142577.
Different types of anti-allergic agents have been compared for their ability to inhibit the antigen-induced contraction of isolated lung parenchymal strips and ilea of guinea pigs. Extremely low concentrations of the lipoxygenase inhibitor NDGA inhibit the contraction of the lung parenchymal strips and higher concentrations block the ileal phase II-contraction (both predominantly caused by the developing SRS-A), but do not inhibit ileal phase I-contraction (caused by released histamine). The H1-antihistamine clemastine predominantly antagonizes phase I of the ileum contraction, and the anti-allergic drug oxatomide reduces all three types of contraction. The degranulation inhibitor DSCG does not influence the contraction of the lung strip, but produces a slight inhibition of both ileal contractions. The PAF-antagonist BN 52021 influences these three contractions in the opposite way to DSCG. As these various types of anti-allergic agents influence these three contractions in a different manner, the models can be used for judging the mechanism of action of a new anti-allergic compound.
已对不同类型的抗过敏药物抑制豚鼠离体肺实质条和回肠抗原诱导收缩的能力进行了比较。极低浓度的脂氧合酶抑制剂去甲二氢愈创木酸可抑制肺实质条的收缩,较高浓度则可阻断回肠的II期收缩(两者主要由正在形成的慢反应物质A引起),但不抑制回肠的I期收缩(由释放的组胺引起)。H1抗组胺药氯马斯汀主要拮抗回肠收缩的I期,而抗过敏药物奥沙米特可减少所有三种类型的收缩。脱颗粒抑制剂色甘酸钠不影响肺条的收缩,但对回肠的两种收缩均有轻微抑制作用。血小板活化因子拮抗剂BN 52021对这三种收缩的影响与色甘酸钠相反。由于这些不同类型的抗过敏药物以不同方式影响这三种收缩,因此这些模型可用于判断新抗过敏化合物的作用机制。