Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2021-07-23 , DOI: 10.1016/j.bmcl.2021.128275 Katarzyna Kucwaj-Brysz 1 , Hanna Baltrukevich 1 , Kinga Czarnota 1 , Jadwiga Handzlik 1
Despite the better understanding of the mechanisms underlying Alzheimer’s Disease (AD) and launched clinical trials, no AD-modifying treatment based on a synthetic drug has been introduced for almost twenty years. The serotonin 5-HT6 and 5-HT7 receptors turned out to be promising biological targets for modulation of central nervous system dysfunctions including cognitive impairment. Within this paper, we evaluate the pharmacological potency of both, 5-HT6R and 5-HT7R, agents in search for novel AD treatment. An overview of chemical structures of the 5-HTRs ligands with simultaneous procognitive action which have undergone preclinical and clinical studies within the last 10 years has been performed.
中文翻译:
血清素 5-HT6 和 5-HT7 受体药物治疗阿尔茨海默病的潜力的化学更新
尽管对阿尔茨海默病 (AD) 的潜在机制有了更好的了解并启动了临床试验,但近 20 年来没有引入基于合成药物的 AD 修饰治疗。5-羟色胺5-HT 6和5-HT 7受体被证明是用于调节中枢神经系统功能障碍包括认知障碍的有希望的生物靶标。在本文中,我们评估了 5-HT 6 R 和 5-HT 7 R这两种药物的药理学效力,以寻找新的 AD 治疗方法。对在过去 10 年内进行了临床前和临床研究的具有同步预认知作用的 5-HTR 配体的化学结构进行了概述。