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

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

Emil Märcher Rørsted  1 , Anders A Jensen  1 , Jesper L Kristensen  1
Affiliations
Review

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

Emil Märcher Rørsted et al. ChemMedChem. .

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.

Keywords: 5-HT2A; Serotonin; agonist; psychedelics; selectivity.

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