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C. Stove

2 papers in the library · publishing 2020-2021

Papers

Serotonin 2A Receptor (5-HT2AR) Activation by 25H-NBOMe Positional Isomers: In Vitro Functional Evaluation and Molecular Docking.

ACS Pharmacology & Translational Science February 25, 2021 E. Pottie, O. Kupriyanova, Asher L. Brandt et al.

Five positional isomers of the psychedelic compound 25H-NBOMe, each differing in the placement of two methoxy groups on the phenyl ring of the phenethylamine moiety, were tested in split-nanoluciferase assays to measure their ability to recruit cytosolic proteins to the serotonin 2A receptor. Molecular docking simulations estimated which receptor residues interact with each isomer's methoxy groups. This is the first comparative evaluation of how the positioning of methoxy groups in the phenethylamine moiety of NBOMes affects functional activity at the receptor.

Identification of psychedelic new psychoactive substances (NPS) showing biased agonism at the 5-HT2AR through simultaneous use of β-arrestin 2 and miniGαq bioassays.

Biochemical Pharmacology September 27, 2020 E. Pottie, P. Dedecker, C. Stove

Psychedelic new psychoactive substances (NPS) that activate the serotonin 2A receptor (5-HT2AR) remain a large share of reported NPS, but their exact mechanisms—especially what distinguishes them from non-psychedelic 5-HT2AR agonists—need more study. A new bioassay was developed to monitor recruitment of an engineered miniGαq protein to the activated 5-HT2AR, designed to parallel an existing assay for β-arrestin 2 recruitment. This allowed estimation of a substance's preference for triggering one protein over the other (biased agonism).