5-羟色胺(5-HT)是重要的神经递质,5-HT受体(5-HTR)在认知、情感等众多神经活动中发挥着重要作用,是重要的药物靶标。5-HT1A受体(5-HT1AR)是众多5-HTR亚型中研究最为广泛和深入的一类受体,研究5-HT1A受体配体(5-HT1ARL)对于临床上治疗焦虑、抑郁、疼痛等疾病都具有重要的价值。该文主要从5-HT1ARL结构类型的角度综述5-HT1ARL的最新研究进展,并简要介绍定向多靶标配体的研究成果,展望5-HT1ARL药物的开发前景。
5-HT is an important neurotransmitter. 5-HT receptors(5-HTRs) play significant functions in most of human nervous activities such as cognition, affection and are crucial medicinal targets. Among 5- HTRs, 5-HT1A receptor(5-HT1AR) subtype is the best studied. The research of 5-HT1A receptor ligands (5- HT1ARL) is beneficial to treat anxiety, depression, pain, etc. In this review, the latest progress on the different chemical types of the 5-HT1ARL were overviewed. Meanwhile, the development of multi-target-directed ligands and the investigation prospect of 5-HT1ARL drug were described.