School of Pharmaceutical Engineering & Life Science, Changzhou University, Changzhou, Jiangsu 213164, China.
Department of Medicine, Yangzhou Polytechnic College, Yangzhou, Jiangsu 225009, China.
Brain Res Bull. 2019 Nov;153:223-231. doi: 10.1016/j.brainresbull.2019.09.001. Epub 2019 Sep 4.
Alzheimer's disease (AD), characterized by a progressive impairment of memory and cognition, is a major health problem in both developing and developed countries. Currently, no drugs can reverse the progression of AD. Phosphodiesterase 5 (PDE5) is a critical component of the cyclic guanosine monophosphate/protein kinase G (cGMP/PKG) signaling pathway in neurons, the inhibition of which has produced neuroprotective effects, and PDE5 inhibitors have recently been thought to be potential therapeutic agents for AD. In this paper, we summarized the outstanding progress that has been made in PDE5 inhibitors as anti-AD agents with encouraging results in animal studies, clinical trials and the investigations on the underlying mechanisms. The novel PDE5 inhibitors reported recently in the treatment of AD were also reviewed and discussed.
阿尔茨海默病（AD），以记忆和认知能力的进行性损害为特征，是发展中国家和发达国家共同面临的主要健康问题。目前，尚无药物可以逆转 AD 的进展。磷酸二酯酶 5（PDE5）是神经元中环鸟苷酸单磷酸/蛋白激酶 G（cGMP/PKG）信号通路的关键组成部分，其抑制可产生神经保护作用，最近认为 PDE5 抑制剂可能是 AD 的潜在治疗药物。本文总结了 PDE5 抑制剂作为抗 AD 药物的突出进展，这些进展在动物研究、临床试验和潜在机制的研究中取得了令人鼓舞的结果。还对最近报道的用于治疗 AD 的新型 PDE5 抑制剂进行了综述和讨论。
