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

Autor: Märcher Rørsted E; Department of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2, 2100, Copenhagen Ø, Denmark., Jensen AA; Department of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2, 2100, Copenhagen Ø, Denmark., Kristensen JL; Department of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2, 2100, Copenhagen Ø, Denmark.
Jazyk: angličtina
Zdroj: ChemMedChem [ChemMedChem] 2021 Nov 05; Vol. 16 (21), pp. 3263-3270. Date of Electronic Publication: 2021 Aug 21.
DOI: 10.1002/cmdc.202100395
Abstrakt: 4-(2-((2-hydroxybenzyl)amino)ethyl)-2,5-dimethoxybenzonitrile (25CN-NBOH) was first reported as a potent and selective serotonin 2A receptor (5-HT 2A 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 2A R, 25CN-NBOH has been used to investigate the effects of selective 5-HT 2A R activation in vivo, and has thus become an important pharmacological tool for the exploration of 5-HT 2A 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.
(© 2021 Wiley-VCH GmbH.)
Databáze: MEDLINE