Syracuse University, Department of Chemistry, 111 College Pl., Syracuse, NY 13244, USA.
Chem Commun (Camb). 2024 Oct 15;60(83):11956-11959. doi: 10.1039/d4cc03892d.
Therapies that target the serotonin 2A receptor (5-HTR) are promising. However, probes are needed to better understand the role of 5-HTR. Here, we design and synthesize a photoswitch and photoswitchable 5-HTR ligand based on highly potent agonist TCB-2 and arylazopyrazole, which also boasts photoswitchable G protein β-arrestin pathway bias.
靶向血清素 2A 受体(5-HTR)的治疗方法很有前途。然而,需要探针来更好地了解 5-HTR 的作用。在这里,我们设计并合成了一种基于高效激动剂 TCB-2 和芳基偶氮吡唑的光开关和可光开关的 5-HTR 配体,它还具有可光开关的 G 蛋白β-arrestin 途径偏倚。