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GEBR-7b a novel PDE4D selective inhibitor that improves memory in rodents at non-emetic doses

机译:GEBR-7b一种新颖的PDE4D选择性抑制剂可在非催吐剂量下提高啮齿动物的记忆力

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摘要

BACKGROUND AND PURPOSEStrategies designed to enhance cerebral cAMP have been proposed as symptomatic treatments to counteract cognitive deficits. However, pharmacological therapies aimed at reducing PDE4, the main class of cAMP catabolizing enzymes in the brain, produce severe emetic side effects. We have recently synthesized a 3-cyclopentyloxy-4-methoxybenzaldehyde derivative, structurally related to rolipram, and endowed with selective PDE4D inhibitory activity. The aim of the present study was to investigate the effect of the new drug, namely GEBR-7b, on memory performance, nausea, hippocampal cAMP and amyloid-β (Aβ) levels.
机译:背景和目的已提出了旨在增强脑部cAMP的策略,作为对付认知缺陷的对症治疗。但是,旨在减少PDE4(脑中cAMP分解代谢的主要酶)的药物疗法会产生严重的催吐作用。我们最近合成了一种3-羟基戊氧基-4-甲氧基苯甲醛衍生物,其结构与咯利普兰有关,并具有选择性的PDE4D抑制活性。本研究的目的是研究新药GEBR-7b对记忆性能,恶心,海马cAMP和淀粉样β(Aβ)水平的影响。

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