2-苯基组胺的Nα-烷基化衍生物：强效组胺H1受体激动剂的合成与体外活性
N alpha-alkylated derivatives of 2-phenylhistamines: synthesis and in vitro activity of potent histamine H1-receptor agonists.
作者信息
Kramer K, Elz S, Pertz H H, Schunack W
机构信息
Fachbereich Pharmazie, Freie Universität Berlin, Germany.
出版信息
Bioorg Med Chem Lett. 1998 Sep 22;8(18):2583-8. doi: 10.1016/s0960-894x(98)00461-2.
New potent N alpha-alkylated histamine H1-receptor agonists have been prepared and functionally evaluated for partial agonist potency and selectivity. N alpha-Methyl-2-(3-trifluoromethylphenyl)histamine contracts ileal segments and aortic rings of guinea-pig with a relative potency of 174% (95% confid. lim. 161-188%) and 217% (164-287%), respectively (histamine: 100%) and is the most potent H1 receptor agonist described so far.
新型强效Nα-烷基化组胺H1受体激动剂已被制备出来，并对其部分激动剂效力和选择性进行了功能评估。Nα-甲基-2-(3-三氟甲基苯基)组胺使豚鼠回肠段和主动脉环收缩，相对效力分别为174%（95%置信区间161 - 188%）和217%（164 - 287%）（组胺：100%），是迄今为止所描述的最有效的H1受体激动剂。
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