Serotonin 2A Receptor (5-HT_2AR) Activation by 25H-NBOMe Positional Isomers: In Vitro Functional Evaluation and Molecular Docking.

ABSTRACT: Serotonergic psychedelics are defined as compounds having serotonin 2A receptor (5-HT_2AR) activation as an important pharmacological mechanism. These compounds include the phenylalkylamine class, containing substances with e.g. 2C-X structures (phenethylamines) or their N-methoxybenzyl analogues (NBOMes). Besides their abuse potential, psychedelics are increasingly recognized for having therapeutic benefits. However, many psychedelics remain incompletely characterized, even concerning their structure-activity relationships. Here, five positional isomers of 25H-NBOMe, with two methoxy groups on the different positions of the phenyl ring of the phenethylamine moiety, were subjected to split-nanoluciferase assays assessing the in vitro recruitment of cytosolic protein

SUBMITTER: Pottie E 

PROVIDER: S-EPMC8033611 | biostudies-literature | 2021 Apr

REPOSITORIES: biostudies-literature