| 查看: 510 | 回复: 1 | ||
| 本帖产生 1 个 翻译EPI ，点击这里进行查看 | ||
| 当前只显示满足指定条件的回帖，点击这里查看本话题的所有回帖 | ||
txy5207铁杆木虫 (正式写手)
|
[求助]
求英文翻译一段（药物）
|
|
|
Following selective secondary binding evaluation for κ opioid and sigma binding, we noted that many compounds of this chemotype possessed potent sigma 1 receptor binding. Although full panel GPCR screening was not completed for this chemotype,six compounds (entries 1–3, 5, 6, and 14 in Table 1) were found to lack submicromolar binding against 5HT6 and D4 (arbitrarily chosen as representative countertargets). Five individual examples of compounds with a single digit nanomolar sigma 1 Kivalue were found (entries 2, 3, 7, 15, and 20). In particular, entry 20 was an exciting result, due to both potency (2 nM Ki) and selectivity (sigma 1:sigma 2:KOR binding ratio of 1∶88∶558). Also of note was that the stereochemistry of the ethyl side chain has little effect on this potent sigma binding because derivatives of both epimers were similarly tight-binding. The sigma 1 secondary binding curves for the compounds in entries 19, 20, and the control compound, haloperidol, are shown in Fig. 5. The binding curves illustrate the dramatic link between activity and basic nitrogen incorporation with compound 10{20}, found to be of comparable potency to haloperidol, and compound 10{19},found to be inactive. An analogous trend was observed for the sigma 2 binding between these compounds, although with a less drastic dependence on basic nitrogen incorporation. Although the structures of 10{20} and haloperidol differ substantially in connectivity, both contain a phenyl group tethered to the basic nitrogen. To assess whether the tricyclic scaffold is contributing significantly to the observed binding activity, the alkyl chain analogue was synthesized (entry 22). Gratifyingly, this analogue retained marked sigma binding affinity, thus dispelling any speculation that an aromatic moiety tethered amine is responsible for the activity. [ Last edited by txy5207 on 2011-7-20 at 20:40 ] |
回复此楼» 猜你喜欢
论文终于录用啦！满足毕业条件了
已经有5人回复
-
2025年遐想
已经有4人回复
-
投稿Elsevier的杂志（返修），总是在选择OA和subscription界面被踢皮球
已经有8人回复
-
自然科学基金委宣布启动申请书“瘦身提质”行动
已经有4人回复
-
求个博导看看
已经有18人回复