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Carbamoylcholine analogs as nicotinic acetylcholine receptor agonists—Structural modifications of 3-(dimethylamino)butyl dimethylcarbamate (DMABC)
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2008-11-07 , DOI: 10.1016/j.bmcl.2008.11.011 Camilla P. Hansen , Anders A. Jensen , Thomas Balle , Klaus Bitsch-Jensen , Mohamud M. Hassan , Tommy Liljefors , Bente Frølund
中文翻译:
氨基甲酰胆碱类似物作为烟碱乙酰胆碱受体激动剂—3-(二甲基氨基)丁基二甲基氨基甲酸酯(DMABC)的结构修饰
更新日期:2008-11-07
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2008-11-07 , DOI: 10.1016/j.bmcl.2008.11.011 Camilla P. Hansen , Anders A. Jensen , Thomas Balle , Klaus Bitsch-Jensen , Mohamud M. Hassan , Tommy Liljefors , Bente Frølund
Compounds based on the 3-(dimethylamino)butyl dimethylcarbamate (DMABC) scaffold were synthesized and pharmacologically characterized at the α4β2, α3β4, α4β4 and α7 neuronal nicotinic acetylcholine receptors (nAChRs). The carbamate functionality and a small hydrophobic substituent in the C-3 position were found to be vital for the binding affinity to the nAChRs, whereas the carbamate nitrogen substituents were important for nAChR subtype selectivity. Finally, the compounds were found to be agonists at the α3β4 nAChR.
中文翻译:
![](https://scdn.x-mol.com/jcss/images/paperTranslation.png)
氨基甲酰胆碱类似物作为烟碱乙酰胆碱受体激动剂—3-(二甲基氨基)丁基二甲基氨基甲酸酯(DMABC)的结构修饰
基于所述3-(二甲氨基)丁基二甲基氨基甲酸酯化合物(DMABC)支架的合成和药理学特征的α 4 β 2,α 3 β 4, α 4 β 4和α 7的神经元烟碱型乙酰胆碱受体(nAChRs)。发现氨基甲酸酯官能度和C-3位的小疏水取代基对于与nAChRs的结合亲和力至关重要,而氨基甲酸酯氮取代基对nAChR亚型选择性很重要。最后,发现化合物是在α激动剂3 β 4的nAChR。