Ramachers U, Amon U, Wolff H H
Department of Dermatology, Medical University of Lübeck, Germany.
Agents Actions. 1994 Jun;41 Spec No:C45-6. doi: 10.1007/BF02007760.
The present study was performed to investigate the putative suppressive effects of H1-receptor antagonists (HRA) of the second generation (astemizole (AS), cetirizine (CT), loratadine (LO), oxatomide (OX) and terfenadine (TF)) on the mediator release from human basophils activated by two classical stimuli. Anti-IgE-mediated histamine release was inhibited in a dose-dependent fashion by TF (maximum inhibitory value: 33.8 +/- 7.6%, 100 microM, n = 7), whereas the other HRA exhibited weaker activity. The anti-IgE-induced LTC4 production was strongly suppressed by TF, LO and OX (92.4 +/- 6.3%, 90.8 +/- 6.0% and 88.5 +/- 5.6%, 100 microM, n = 4-5), while AS was less active (56.4 +/- 4.1%, 100 microM, n = 5). Histamine release induced by incubation with grass pollen antigen (0.01%) was inhibited by TF (40.7 +/- 4.1%, 50 microM, n = 4), but the other HRA showed only low activity. The present findings suggest that some HRA might exhibit direct inhibitory effects on activation of IgE-receptor bearing cells.
本研究旨在探讨第二代H1受体拮抗剂（HRA）（阿司咪唑（AS）、西替利嗪（CT）、氯雷他定（LO）、奥沙米特（OX）和特非那定（TF））对两种经典刺激激活的人嗜碱性粒细胞介质释放的假定抑制作用。TF以剂量依赖方式抑制抗IgE介导的组胺释放（最大抑制值：33.8±7.6%，100μM，n = 7），而其他HRA活性较弱。TF、LO和OX强烈抑制抗IgE诱导的LTC4产生（92.4±6.3%、90.8±6.0%和88.5±5.6%，100μM，n = 4 - 5），而AS活性较低（56.4±4.1%，100μM，n = 5）。与草花粉抗原（0.01%）孵育诱导的组胺释放被TF抑制（40.7±4.1%，50μM，n = 4），但其他HRA仅显示低活性。本研究结果表明，一些HRA可能对携带IgE受体的细胞激活具有直接抑制作用。
