Synthesis and neuropharmacological characterization of 2-O-substituted apomorphines

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• 作者：Attila Sipos ; Csaba Csutorá ; s ; Sá ; ndor Beré ; nyi ; Ain Uustare ; Ago Rinken
• 关键词：Apomorphine ; 2-Alkoxyapomorphines ; Alkyl-type hydroxyl ; Bis-apomorphines ; Dopamine receptor binding activity ; D₂/D₁ receptor selectivity
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2008
• 期刊代码：9_09680896
• 类别：ch
• 出版时间：15 April 2008
• 卷：16
• 期：8
• 页码：4563-4568
• 文件大小：157 K

摘要

We have synthesized novel 2-O-substituted apomorphines with both different lengths of lipophilic alkyl chains and alkyl chains carrying free hydroxyl groups. Two bis-apomorphines formed as side products of the reactions with diols were isolated and characterized as well. The neuropharmacological profile of all these new compounds were investigated with respect to their binding affinities and activities to dopamine D₂ and D₁ receptors. The obtained data pointed to the fact that, in the examination of dopaminergic activities of 2-substituted apomorphines, the lipophilicity of the substituent is more important than its spatial parameters.