Modification of the anabaseine pyridine nucleus allows achieving binding and functional selectivity for the α3β4 nicotinic acetylcholine receptor subtype
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- 作者：Carlo Materaa ; Marta Quadria ; Miriam Sciaccalugab ; Diego Yuri Pomè ; a ; Francesca Fasolid ; e ; Marco De Amicia ; Sergio Fucileb ; c ; Cecilia Gottid ; e ; Clelia Dallanocea ; clelia.dallanoce@unimi.it" class="auth_mail" title="E-mail the corresponding author ; Giovanni Graziosoa
- 关键词：Neuronal nicotinic acetylcholine receptors ; Molecular modeling ; Design ; Anabaseine-related derivatives ; α3β4 nicotinic ligands ; Binding affinity ; Functional activity/selectivity
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：27 January 2016
- 年：2016
- 卷：108
- 期：Complete
- 页码：392-405
- 全文大小：1539 K
文摘
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Novel anabaseine-related derivatives were designed, synthesized and tested.
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Substituents on the 3-position of the benzene ring engendered binding selectivity.
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Electrophysiological assays evidenced functional selectivity among nAChRs.
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The 3-iodo derivative 12 behaved as a selective α3β4 partial agonist.