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

4-(2-((2-hydroxybenzyl)amino)ethyl)-2,5-dimethoxybenzonitrile (25CN-NBOH) was first reported as a potent and selective serotonin 2A receptor (5-HT2AR) 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-HT2AR, 25CN-NBOH has been used to investigate the effects of selective 5-HT2AR activation in vivo, and has thus become an important pharmacological tool for the exploration of 5-HT2AR 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.

Automated summary

25CN-NBOH, a potent and selective serotonin 2A receptor agonist, has been widely used in various studies due to its favorable physiochemical properties and superior selectivity. It has become an important pharmacological tool for exploring 5-HT2AR signaling in different animal models.