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Characterization of antihistamines using biphasic cutaneous reaction in BALB/c mice.

机译:在BALB / c小鼠中使用双相皮肤反应表征抗组胺药。

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摘要

Effects of 11 histamine H1 receptor antagonists on IgE-mediated biphasic cutaneous reaction in mice were examined. The immediate phase reaction (IPR) assessed at 1 hour after antigen application was significantly inhibited by all antihistamines examined. The inhibition of IPR by cetirizine and mequitazine were potent, but those by cyproheptadine and diphenhydramine were weak. The later phase reaction (LPR) assessed at 24 hours after antigen application was inhibited by chlorpheniramine, oxatomide, ketotifen, mequitazine, emedastine, terfenadine and azelastine. The inhibition of LPR by emedastine was potent, but those by ketotifen and terfenadine were only partial. Emedastine inhibited both IPR and LPR comparably. Present results indicate that H1 receptor activation is involved in the IPR of the biphasic cutaneous reaction, and that the blockade of H1 receptors at IPR does not contribute to the attenuation of following LPR. Histamine H1 receptor antagonists inhibiting the LPR have a property distinct from H1 receptor antagonism, which may have an additional benefit for the treatment of allergic diseases.
机译:检查了11种组胺H1受体拮抗剂对IgE介导的小鼠双相皮肤反应的影响。抗原应用后1小时评估的即期反应(IPR)被所有检查的抗组胺药均显着抑制。西替利嗪和美喹他嗪对IPR的抑制作用强,但是赛庚啶和苯海拉明对IPR的抑制作用弱。氯苯那敏,奥沙米特,酮替芬,美喹他嗪,艾美他汀,特非那定和氮卓斯汀抑制了抗原应用后24小时评估的后期反应(LPR)。依米斯汀对LPR的抑制作用很强,但酮替芬和特非那定对LPR的抑制作用只是部分的。 Emedastine可同等地抑制IPR和LPR。目前的结果表明,H1受体的激活参与了双相皮肤反应的IPR,并且H1受体在IPR处的阻滞并没有促进随后LPR的减弱。抑制LPR的组胺H1受体拮抗剂具有与H1受体拮抗作用不同的性质,这可能对治疗过敏性疾病有额外的好处。

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