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【答案】应助回帖
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Mally89(金币+1): 再加一个！~专家辛苦了！~ 2011-07-23 21:22:05
411iloveyo(金币+300, 翻译EPI+1): 西西 谢谢。。。。。 2011-07-25 08:15:46
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Thus, compound 14{11} emerged as the most potent Sig-R binding candidate (Ki ¼ 867, 280 nM for sigma 1 and sigma 2, respectively) and compound 14{15} was found to possess the most potent κ opioid binding (Ki ¼ 407 nM) along with modest sigma 1 binding (Ki ¼ 1;158 nM). 由此发现作为最强Sig-R亲和性候选化合物14{11}和化合物14{15}具有最强的k阿片受体亲和性和中度的sigma 1受体亲和性。Sixteen of the 44 compounds were also evaluated for 5HT1A binding, with only compound 14{26} found to possess significant 5HT1A binding activity (Ki ¼ 431 nM).还评估了44种化合物中的16种对5HT1A受体的亲和性，发现只有化合物14{26}具有显著的5HT1A结合活性。 In addition, four compounds were screened against the full 43 GPCR assay panel as described previously for neostenine. 此外，还对4种化合物进行了如前所述对新斯替宁碱所进行的针对43种GPCR的组合筛选。The results showed this compound subset to be free from promiscuous binding, and compound 14{41} was discovered to possess selective adrenergic binding affinity (Ki ¼ 1;156, 7,588 nM for Alpha1A and Alpha1B, respectively). 结果显示这几个化合物缺乏各式各样的亲和性，化合物14{41}具有选择性肾上腺素能受体亲和性。Representative structures of this chemotype and associated binding activity are shown in Scheme 4 (for complete data on all compounds, see SI Appendix).此化学型种典型的结构及与之相联系的结合活性情况见示意图4.（所有化合物的完备资料，见附录SI。） |
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