Design, synthesis, and pharmacological evaluation of multitarget-directed ligands with both serotonergic subtype 4 receptor (5-HT4R) partial agonist and 5-HT6R antagonist activities, as potential treatment of Alzheimer’s disease
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- 作者：Samir Yahiaouia ; Katia Hamidoucheb ; Cé ; line Ballandonnea ; Audrey Davisa ; Jana Sopkova de Oliveira Santosa ; Thomas Freretb ; Michel Boulouardb ; Christophe Rochaisa ; christophe.rochais@unicaen.fr" class="auth_mail" title="E-mail the corresponding author ; Patrick Dallemagnea ; patrick.dallemagne@unicaen.fr" class="auth_mail" title="E-mail the corresponding author
- 关键词：Alzheimer&rsquo ; s disease ; MTDL ; 5-HT4 receptors agonists ; 5-HT6 receptors antagonists
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：4 October 2016
- 年：2016
- 卷：121
- 期：Complete
- 页码：283-293
- 全文大小：688 K
文摘
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Seventeen novel derivatives of RS67333 were synthesized.
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5">Some of them showed nanomolar and submicromolar affinities toward 5-HT4R and 5-HT6R respectively.
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One of these MTDL showed an antiamnesic effect in the mouse at 1 mg/kg ip.
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5">It could represent a potential novel therapeutic avenue within AD treatment.