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Serotonin 2A Receptor (5-HT<inf>2A</inf>R) Activation by 25H-NBOMe Positional Isomers: In Vitro Functional Evaluation and Molecular Docking

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dc.contributor.author Pottie E.
dc.contributor.author Kupriyanova O.V.
dc.contributor.author Brandt A.L.
dc.contributor.author Laprairie R.B.
dc.contributor.author Shevyrin V.A.
dc.contributor.author Stove C.P.
dc.date.accessioned 2022-02-09T20:45:19Z
dc.date.available 2022-02-09T20:45:19Z
dc.date.issued 2021
dc.identifier.uri https://dspace.kpfu.ru/xmlui/handle/net/170053
dc.description.abstract Serotonergic psychedelics are defined as compounds having serotonin 2A receptor (5-HT2AR) 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 proteins to the 5-HT2AR. Furthermore, molecular docking at the 5-HT2AR allowed estimation of which residues interact with the specific isomers' methoxy groups. Although the optimal substitution pattern of N-unsubstituted phenylalkylamines has been extensively studied, this is the first comparative evaluation of the functional effects of the positioning of the methoxy groups in the phenethylamine moiety of NBOMes.
dc.subject bioassay
dc.subject molecular docking
dc.subject new psychoactive substances
dc.subject psychedelic
dc.subject serotonin receptor
dc.subject structure-activity relationship
dc.title Serotonin 2A Receptor (5-HT<inf>2A</inf>R) Activation by 25H-NBOMe Positional Isomers: In Vitro Functional Evaluation and Molecular Docking
dc.type Article
dc.relation.ispartofseries-issue 2
dc.relation.ispartofseries-volume 4
dc.collection Публикации сотрудников КФУ
dc.relation.startpage 479
dc.source.id SCOPUS-2021-4-2-SID85103455365


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  • Публикации сотрудников КФУ Scopus [24551]
    Коллекция содержит публикации сотрудников Казанского федерального (до 2010 года Казанского государственного) университета, проиндексированные в БД Scopus, начиная с 1970г.

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