Khandwala A, Coutts S M, Dally-Meade V, Jariwala N, Huang F C
Int Arch Allergy Appl Immunol. 1983;70(4):311-20. doi: 10.1159/000233342.
RHC 3024 has been investigated for its antiallergic activity in three in vitro models of anaphylaxis. We have also compared its activity profile in these models with that of disodium cromoglycate (DSCG) and other antiallergic agents. As an inhibitor of antigen-induced release of histamine from rat mast cells RHC 3024 was 4 times more potent than DSCG. In the same model the activity profile of RHC 3024 was identical to that of DSCG in the following respects: loss of inhibitory activity with increasing preincubation time, reversibility of the inhibition, tachyphylaxis and cross-tachyphylaxis to each other and inability to inhibit histamine release stimulated by Ca++ ionophore, dextran/phosphatidyl serine and compound 48/80. Both drugs had no effect in the other two models, IgG1-mediated histamine release from guinea pig lung and anti-IgE-induced histamine release from human basophils. We conclude: (1) RHC 3024 is a potent inhibitor of mediator release with a mechanism of action similar to that of DSCG, M&B 22,948, PRD-92-Ea and AH-7725 and (2) the in vitro activity profiles of proxicromil, doxantrazole, ICI 74,917 and WY-16,922 are different from DSCG and RHC 3024.
已在三种过敏性反应体外模型中研究了RHC 3024的抗过敏活性。我们还将其在这些模型中的活性概况与色甘酸二钠(DSCG)和其他抗过敏药物进行了比较。作为大鼠肥大细胞中抗原诱导的组胺释放抑制剂,RHC 3024的效力比DSCG高4倍。在同一模型中,RHC 3024的活性概况在以下方面与DSCG相同:随着预孵育时间增加抑制活性丧失、抑制作用的可逆性、快速耐受性以及相互间的交叉快速耐受性,并且无法抑制由钙离子载体、葡聚糖/磷脂酰丝氨酸和化合物48/80刺激的组胺释放。两种药物在另外两种模型中均无作用,即IgG1介导的豚鼠肺组胺释放和抗IgE诱导的人嗜碱性粒细胞组胺释放。我们得出结论:(1)RHC 3024是一种有效的介质释放抑制剂,其作用机制与DSCG、M&B 22,948、PRD - 92 - Ea和AH - 7725相似;(2)丙氧米特、多克替唑、ICI 74,917和WY - 16,922的体外活性概况与DSCG和RHC 3024不同。