25CN‐NBOH: A Selective Agonist for in vitro and in vivo Investigations of the Serotonin 2A Receptor. (21st August 2021)

• Record Type: Journal Article
• Authors: Märcher Rørsted, Emil; Jensen, Anders A.; Kristensen, Jesper L.
• Is Part Of: ChemMedChem. Volume 16:Number 21(2021)
• Page Start: 3263
• Page End: 3270
• Publication Date: 2021-08-21
• Subjects: Serotonin -- agonist -- 5-HT2A -- selectivity -- psychedelics; Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.1002/cmdc.202100395
• Languages: English
• ISSNs: 1860-7179

Abstract

Abstract: 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. Abstract : The highly subtype selective 5‐HT2AR agonist 25CN‐NBOH, has become widely used as a tool compound for various investigations, specifically as a comparator or token selective agonist in an array of studies investigating the implications of 5‐HT2A R activation and related effects. We here present a comprehensive overview of the synthesis, properties and reported applications of this interesting pharmacological tool.