Discovery of β-Arrestin-Biased 25CN-NBOH-Derived 5-HT2A Receptor Agonists
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.2c00702
Abstract: The serotonin 2A receptor (5-HT2AR) is the mediator of the psychedelic effects of serotonergic psychedelics, which have shown promising results in clinical studies for several neuropsychiatric indications. The 5-HT2AR is able to signal through the… read more here.
Keywords: discovery arrestin; arrestin biased; biased 25cn; receptor ... See more keywords
Introducing Conformational Restraints on 25CN-NBOH: A Selective 5-HT2A Receptor Agonist.
Sign Up to like & getrecommendations! Published in 2023 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.3c00014
Abstract: The N-benzylphenethylamines (NBOMes) are a class of ligands from which compounds with impressive selectivity for the serotonin 2A receptor (5-HT2AR) over the closely related serotonin 2C receptor (5-HT2CR) have emerged. These include 4-(2-((2-hydroxybenzyl)amino)ethyl)-2,5-dimethoxybenzonitrile (25CN-NBOH, 1)… read more here.
Keywords: nboh selective; restraints 25cn; conformational restraints; receptor ... See more keywords
Tolerance and Tachyphylaxis to Head Twitches Induced by the 5-HT2A Agonist 25CN-NBOH in Mice
Sign Up to like & getrecommendations! Published in 2018 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2018.00017
Abstract: The serotonin (5-HT) 2A receptor is the primary molecular target of serotonergic hallucinogens, which trigger large-scale perturbations of the cortex. Our understanding of how 5-HT2A activation may cause the effects of hallucinogens has been hampered… read more here.
Keywords: head; tolerance tachyphylaxis; tolerance; ht2a agonist ... See more keywords