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25CN-NBOH:一种用于血清素 2A 受体的体外和体内研究的选择性激动剂。

25CN-NBOH: A Selective Agonist for in vitro and in vivo Investigations of the Serotonin 2A Receptor.

机构信息

Department of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2, 2100, Copenhagen Ø, Denmark.

出版信息

ChemMedChem. 2021 Nov 5;16(21):3263-3270. doi: 10.1002/cmdc.202100395. Epub 2021 Aug 21.

Abstract

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.

摘要

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。

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