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5-羟色胺是吲哚类脑内神经递质,参与脑内痛觉的调节。我们曾证实次甲二氧-3-(1-β-乙基-4-甲基哌嗪)吲哚衍生物有较强的抗电休克及镇痛活性。在吲哚母核的2位氢以甲基、苯基取代或不取代,得3个系列衍生物;在吲哚母核3位上带有碱性醚链的末端氨基氮上,以不同基团取代,共得21个化合物。本文对这些化合物进行了镇痛及抗电休克活性的筛选,并对它们进行了构效关系的分析。
Serotonin is indole brain neurotransmitter, involved in the regulation of intracerebral pain. We have demonstrated that methylenedioxy-3- (1-β-ethyl-4-methylpiperazine) indole derivatives have strong anti-shock and analgesic activities. In the indole nucleus 2 hydrogen to methyl, phenyl substituted or not, have 3 series of derivatives; indole mother nucleus with a basic ether chain at the terminal amino nitrogen, with different groups Group replacement, a total of 21 compounds. In this paper, the compounds were analgesic and anti-shock activity screening, and their structure-activity relationship analysis.