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【答案】应助回帖
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sltmac(金币+1): 谢谢应助，欢迎常来~~ 2011-07-22 16:11:22
烟云听雨(金币+15, 翻译EPI+1): 谢谢 2011-07-24 19:18:07
Binding Studies of the Initial Library Against a Panel of CNS Targets. 初步文库对一组中枢神经系统靶标的亲和性研究
Because other naturally occurring antitussive agents have potent function at one or more CNS receptors (i.e., codeine, along with numerous related agents) (40), we sought to determine if neostenine bound to such targets.由于其它天然存在的镇咳剂在一个或多个中枢神经系统受体具有强的功能，我们试图确定新斯替宁是否与这些受体具有亲和性。 Thus, synthetic ( )-neostenine and ( )-13-epineostenine were screened against 40 individual GPCR and other molecular targets (Fig. 2). 因此对合成的( )-neostenine和( )-13-epineostenine进行了针对40个GPCR和其它分子靶标的筛选。 The compounds were initially screened at a constant concentration (10 μM) to identify possible activity of the compound. 初步筛选采用固定的浓度以确定化合物可能的活性。Results showing significant activity in the initial screen were selected for κi determinations using radioligand binding assays.在初步筛选中显示显著活性的被选出来以放射性配体结合测定确定Ki。 It was determined that ( )- neostenine and ( )-13-epineostenine only showed binding at the muscarinic M5 receptor and Sig-Rs, respectively, as shown. 结果显示( )-neostenine和( )-13-epineostenine只分别对毒蕈碱M5受体和Sig-R显示亲和性。 The somewhat surprising binding differences observed between the epimers suggest a key role for the C-13 substituent.差向异构体之间这种多少令人惊异的亲和性差别提示C-13取代基的关键作用。 |
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