Preclinical and clinical evidence support the effectiveness of neurotrophins in Alzheimer's disease (AD) and neurodegenerative diseases. Delivery of neurotrophins to target sites in the brain remains a major obstacle for their use in humans. Development of orally active agents that mimic the effects of nerve growth factor and other neurotrophins provides a promising alternative therapeutic strategy. AIT-082, a purine analogue, has been shown to reverse age-induced memory deficits in mice and is a growth factor-mimetic agent. It is orally active, rapidly penetrates the blood-brain barrier and induces the production of multiple growth factors at the appropriate target site in the central nervous system (CNS).

译文

临床前和临床证据支持神经营养蛋白在阿尔茨海默氏病 (AD) 和神经退行性疾病中的有效性。将神经营养蛋白递送到大脑的靶位点仍然是其在人类中使用的主要障碍。模拟神经生长因子和其他神经营养蛋白作用的口服活性剂的开发提供了一种有前途的替代治疗策略。AIT-082,一种嘌呤类似物,已被证明可以逆转小鼠中年龄诱导的记忆缺陷,并且是一种生长因子模拟剂。它具有口服活性,可迅速穿透血脑屏障,并在中枢神经系统 (CNS) 的适当靶位点诱导多种生长因子的产生。

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