体内
兴奋剂
血清素
药理学
化学
离体
5-羟色胺受体
受体
功能选择性
体外
生物化学
生物
生物技术
作者
Emil Märcher-Rørsted,Anders A. Jensen,Jesper L. Kristensen
出处
期刊:ChemMedChem
[Wiley]
日期:2021-07-20
卷期号:16 (21): 3263-3270
被引量:15
标识
DOI:10.1002/cmdc.202100395
摘要
4-(2-((2-hydroxybenzyl)amino)ethyl)-2,5-dimethoxybenzonitrile (25CN-NBOH) was first reported as a potent and selective serotonin 2A receptor (5-HT2A 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-HT2A R, 25CN-NBOH has been used to investigate the effects of selective 5-HT2A R activation in vivo, and has thus become an important pharmacological tool for the exploration of 5-HT2A 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.
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