Anti-inflammatory effects of two new methyl and morpholine derivatives of diphenhydramine on rats
作者:Abbas Ahmadi、Mohsen Khalili、Ramin Hajikhani、Narjes Safari、Babak Nahri-Niknafs
DOI:10.1007/s00044-011-9891-y
日期:2012.11
Diphenhydramines are one of the first-generation histamine H1-receptor antagonists of the ethanolamine class that demonstrate many pharmacological properties including anti-inflammatory effects. In this research, bromo (II) and two new tolyl derivatives of I, (Di [p-tolyl] [dimethylaminoethoxy] methane, III) and (Di [p-tolyl] [2-morpholinoethoxy] methane, IV) were synthesized. Their acute and chronic anti-inflammatory
苯海拉明是乙醇胺类的第一代组胺H 1受体拮抗剂之一,具有许多药理特性,包括抗炎作用。在这项研究中,溴(II)和I的两个新的甲苯基衍生物(Di [对甲苯基] [二甲基氨基乙氧基]甲烷(III)和(Di [对甲苯基] [2-吗啉代乙氧基]甲烷(IV))合成。用福尔马林和组胺诱导的大鼠爪水肿评估了它们的急性和慢性抗炎活性。还测量了福尔马林和组胺引起的足爪水肿,二甲苯引起的耳部水肿以及在腹膜腔涂乙酸后的腹膜炎中的血管通透性,并与II进行了比较。选择棉丸诱导的肉芽肿模型来诱导大鼠慢性炎症。新合成的苯海拉明类似物似乎可以有效减少急性炎症。结论是,新药的显着抗炎作用可能与其降低血管通透性机制或对H 1组胺受体的拮抗作用有关。