Department of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2, 2100, Copenhagen Ø, Denmark.
ChemMedChem. 2021 Nov 5;16(21):3263-3270. doi: 10.1002/cmdc.202100395. Epub 2021 Aug 21.
4-(2-((2-hydroxybenzyl)amino)ethyl)-2,5-dimethoxybenzonitrile (25CN-NBOH) was first reported as a potent and selective serotonin 2A receptor (5-HT R) agonist in 2014, and it has since found extensive use as a pharmacological tool in a variety of in vitro, ex vivo and in vivo studies. 25CN-NBOH is readily available from a synthetic perspective using standard chemical transformations, and displays favorable physiochemical properties in terms of stability and solubility. Due to its superior selectivity for 5-HT R, 25CN-NBOH has been used to investigate the effects of selective 5-HT R activation in vivo, and has thus become an important pharmacological tool for the exploration of 5-HT R signaling in a range of animal models. In the present review, we outline the discovery of 25CN-NBOH, its pharmacological profile and major findings from studies where it has been used.
4-(2-((2-羟基苄基)氨基)乙基)-2,5-二甲氧基苯甲腈(25CN-NBOH)于 2014 年首次被报道为一种强效且选择性的 5-羟色胺 2A 受体(5-HT R)激动剂,此后,它已被广泛用作各种体外、离体和体内研究的药理学工具。从合成的角度来看,25CN-NBOH 很容易通过标准的化学转化得到,并且在稳定性和溶解度方面表现出良好的物理化学性质。由于其对 5-HT R 的高选择性,25CN-NBOH 已被用于研究选择性 5-HT R 激活在体内的作用,因此成为探索一系列动物模型中 5-HT R 信号的重要药理学工具。在本综述中,我们概述了 25CN-NBOH 的发现、其药理学特征以及在使用它的研究中的主要发现。