Hughes Alexander J, Talbert Julie A, Townsend Steven D
Department of Chemistry, Vanderbilt University, Nashville, Tennessee 37235, United States.
ACS Bio Med Chem Au. 2025 May 12;5(3):379-386. doi: 10.1021/acsbiomedchemau.5c00011. eCollection 2025 Jun 18.
Substance use disorder (SUD) is a mental condition that affects a person's brain and behavior, leading to a lack of control with alcohol, drug, and medication use. The lack of efficacious and novel treatments for SUD is a growing concern. As such, we have synthesized a series of iboga alkaloid derivatives and evaluated their receptor binding profiles against a panel of CNS-based proteins, which were performed at the National Institute of Mental Health Psychoactive Drug Screening Program. These studies revealed two compounds that exhibit high affinity for the sigma-2 receptor and introduce the iboga alkaloid framework as a new scaffold for the development of sigma-2 ligands.
物质使用障碍（SUD）是一种影响人的大脑和行为的精神疾病，会导致对酒精、药物和药物使用失去控制。缺乏针对SUD的有效和新型治疗方法日益受到关注。因此，我们合成了一系列伊博格生物碱衍生物，并在美国国立精神卫生研究所精神活性药物筛选项目中，评估了它们与一组基于中枢神经系统的蛋白质的受体结合情况。这些研究揭示了两种对sigma-2受体具有高亲和力的化合物，并引入了伊博格生物碱框架作为开发sigma-2配体的新支架。
