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Acute behavioral and Neurochemical Effects of Novel N-Benzyl-2-Phenylethylamine Derivatives in Adult Zebrafish
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    Research Article

    Acute behavioral and Neurochemical Effects of Novel N-Benzyl-2-Phenylethylamine Derivatives in Adult Zebrafish
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    • Konstantin A. Demin*
      Konstantin A. Demin
      Institute of Translational Biomedicine, St. Petersburg State University, St. Petersburg 199034, Russia
      Almazov National Medical Research Centre, St. Petersburg 197341, Russia
      *Email: [email protected]
    • Olga V. Kupriyanova
      Olga V. Kupriyanova
      Institute of Fundamental Medicine and Biology, Kazan Volga Region Federal University, Kazan 420008, Russia
      Kazan State Medical University, Kazan 420012, Russia
    • Vadim A. Shevyrin*
      Vadim A. Shevyrin
      Institute of Chemistry and Technology, Ural Federal University, 19 Mira Str., Ekaterinburg 620002, Russia
      *Email: [email protected]
    • Ksenia A. Derzhavina
      Ksenia A. Derzhavina
      Institute of Translational Biomedicine, St. Petersburg State University, St. Petersburg 199034, Russia
      Almazov National Medical Research Centre, St. Petersburg 197341, Russia
    • Nataliya A. Krotova
      Nataliya A. Krotova
      Institute of Translational Biomedicine, St. Petersburg State University, St. Petersburg 199034, Russia
      Almazov National Medical Research Centre, St. Petersburg 197341, Russia
    • Nikita P. Ilyin
      Nikita P. Ilyin
      Institute of Translational Biomedicine, St. Petersburg State University, St. Petersburg 199034, Russia
      Almazov National Medical Research Centre, St. Petersburg 197341, Russia
    • Tatiana O. Kolesnikova
      Tatiana O. Kolesnikova
      Institute of Translational Biomedicine, St. Petersburg State University, St. Petersburg 199034, Russia
      Neurobiology Program, Sirius University of Science and Technology, Sochi 354340, Russia
    • David S. Galstyan
      David S. Galstyan
      Institute of Translational Biomedicine, St. Petersburg State University, St. Petersburg 199034, Russia
      Laboratory of Preclinical Bioscreening, Granov Russian Research Center of Radiology and Surgical Technologies, Ministry of Healthcare of Russian Federation, Pesochny 197758, Russia
    • Yurii M. Kositsyn
      Yurii M. Kositsyn
      Institute of Translational Biomedicine, St. Petersburg State University, St. Petersburg 199034, Russia
    • Abubakar-Askhab S. Khaybaev
      Abubakar-Askhab S. Khaybaev
      Almazov National Medical Research Centre, St. Petersburg 197341, Russia
    • Maria V. Seredinskaya
      Maria V. Seredinskaya
      Institute of Translational Biomedicine, St. Petersburg State University, St. Petersburg 199034, Russia
    • Yaroslav Dubrovskii
      Yaroslav Dubrovskii
      Almazov National Medical Research Centre, St. Petersburg 197341, Russia
      Institute of Chemistry, St. Petersburg State University, St. Petersburg 199034, Russia
      St. Petersburg State Chemical Pharmaceutical University, St. Petersburg 197022, Russia
    • Raziya G. Sadykova
      Raziya G. Sadykova
      Kazan State Medical University, Kazan 420012, Russia
    • Maria O. Nerush
      Maria O. Nerush
      Almazov National Medical Research Centre, St. Petersburg 197341, Russia
    • Mikael S. Mor
      Mikael S. Mor
      Institute of Translational Biomedicine, St. Petersburg State University, St. Petersburg 199034, Russia
    • Elena V. Petersen
      Elena V. Petersen
      Moscow Institute of Physics and Technology, Moscow 141701, Russia
    • Tatyana Strekalova
      Tatyana Strekalova
      Maastricht University, NL Postbus 616, Maastricht 62, Netherlands
    • Evgeniya V. Efimova
      Evgeniya V. Efimova
      Institute of Translational Biomedicine, St. Petersburg State University, St. Petersburg 199034, Russia
    • Savelii R. Kuvarzin
      Savelii R. Kuvarzin
      Institute of Translational Biomedicine, St. Petersburg State University, St. Petersburg 199034, Russia
    • Konstantin B. Yenkoyan
      Konstantin B. Yenkoyan
      Neuroscience Laboratory, COBRAIN Center, M. Heratsi Yerevan State Medical University, Yerevan AM 0025, Armenia
      COBRAIN Scientific Educational Center for Fundamental Brain Research, Yerevan AM 0025, Armenia
    • Dmitrii V. Bozhko
      Dmitrii V. Bozhko
      ZebraML, Inc., Houston 77001 Texas, United States
    • Vladislav O. Myrov
      Vladislav O. Myrov
      ZebraML, Inc., Houston 77001 Texas, United States
    • Sofia M. Kolchanova
      Sofia M. Kolchanova
      ZebraML, Inc., Houston 77001 Texas, United States
    • Aleksander I. Polovian
      Aleksander I. Polovian
      ZebraML, Inc., Houston 77001 Texas, United States
    • Georgii K. Galumov
      Georgii K. Galumov
      ZebraML, Inc., Houston 77001 Texas, United States
    • Allan V. Kalueff*
      Allan V. Kalueff
      Institute of Translational Biomedicine, St. Petersburg State University, St. Petersburg 199034, Russia
      Almazov National Medical Research Centre, St. Petersburg 197341, Russia
      Ural Federal University, Ekaterinburg 620075, Russia
      Granov Russian Research Center of Radiology and Surgical Technologies, Ministry of Healthcare of Russian Federation, Pesochny 197758, Russia
      Moscow Institute of Physics and Technology, Moscow 141701, Russia
      COBRAIN Scientific Educational Center for Fundamental Brain Research, Yerevan AM 0025, Armenia
      Scientific Research Institute of Neuroscience and Medicine, Novosibirsk, 630117, Russia
      *Email: [email protected]. Phone: +1-240-899-9571.
    Other Access OptionsSupporting Information (1)

    ACS Chemical Neuroscience

    Cite this: ACS Chem. Neurosci. 2022, 13, 13, 1902–1922
    Click to copy citationCitation copied!
    https://doi.org/10.1021/acschemneuro.2c00123
    Published June 7, 2022
    Copyright © 2022 American Chemical Society

    Abstract

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    Hallucinogenic drugs potently affect brain and behavior and have also recently emerged as potentially promising agents in pharmacotherapy. Complementing laboratory rodents, the zebrafish (Danio rerio) is a powerful animal model organism for screening neuroactive drugs, including hallucinogens. Here, we test a battery of ten novel N-benzyl-2-phenylethylamine (NBPEA) derivatives with the 2,4- and 3,4-dimethoxy substitutions in the phenethylamine moiety and the −OCH3, −OCF3, −F, −Cl, and −Br substitutions in the ortho position of the phenyl ring of the N-benzyl moiety, assessing their acute behavioral and neurochemical effects in the adult zebrafish. Overall, substitutions in the Overall, substitutions in the N-benzyl moiety modulate locomotion, and substitutions in the phenethylamine moiety alter zebrafish anxiety-like behavior, also affecting the brain serotonin and/or dopamine turnover. The 24H–NBOMe(F) and 34H–NBOMe(F) treatment also reduced zebrafish despair-like behavior. Computational analyses of zebrafish behavioral data by artificial intelligence identified several distinct clusters for these agents, including anxiogenic/hypolocomotor (24H–NBF, 24H–NBOMe, and 34H–NBF), behaviorally inert (34H–NBBr, 34H–NBCl, and 34H–NBOMe), anxiogenic/hallucinogenic-like (24H–NBBr, 24H–NBCl, and 24H–NBOMe(F)), and anxiolytic/hallucinogenic-like (34H–NBOMe(F)) drugs. Our computational analyses also revealed phenotypic similarity of the behavioral activity of some NBPEAs to that of selected conventional serotonergic and antiglutamatergic hallucinogens. In silico functional molecular activity modeling further supported the overlap of the drug targets for NBPEAs tested here and the conventional serotonergic and antiglutamatergic hallucinogens. Overall, these findings suggest potent neuroactive properties of several novel synthetic NBPEAs, detected in a sensitive in vivo vertebrate model system, the zebrafish, raising the possibility of their potential clinical use and abuse.

    Copyright © 2022 American Chemical Society

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    Supporting Information

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    The Supporting Information is available free of charge at https://pubs.acs.org/doi/10.1021/acschemneuro.2c00123.

    • Statistical data for behavioral and neurochemical analyses and figures with analytical data for the studied compounds (PDF)

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    Cited By

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    This article is cited by 2 publications.

    1. Nikita P. Ilyin, Arslan D. Nabiullin, Anna D. Kozlova, Olga V. Kupriyanova, Vadim A. Shevyrin, Tatyana Gloriozova, Dmitry Filimonov, Alexey Lagunin, David S. Galstyan, Tatiana O. Kolesnikova, Mikael S. Mor, Evgeniya V. Efimova, Vladimir Poroikov, Konstantin B. Yenkoyan, Murilo S. de Abreu, Konstantin A. Demin, Allan V. Kalueff. Chronic Behavioral and Neurochemical Effects of Four Novel N-Benzyl-2-phenylethylamine Derivatives Recently Identified as “Psychoactive” in Adult Zebrafish Screens. ACS Chemical Neuroscience 2024, 15 (10) , 2006-2017. https://doi.org/10.1021/acschemneuro.4c00017
    2. Binjie Wang, Jiale Chen, Zhong Sheng, Wanting Lian, Yuanzhao Wu, Meng Liu. Embryonic exposure to fentanyl induces behavioral changes and neurotoxicity in zebrafish larvae. PeerJ 2022, 10 , e14524. https://doi.org/10.7717/peerj.14524

    ACS Chemical Neuroscience

    Cite this: ACS Chem. Neurosci. 2022, 13, 13, 1902–1922
    Click to copy citationCitation copied!
    https://doi.org/10.1021/acschemneuro.2c00123
    Published June 7, 2022
    Copyright © 2022 American Chemical Society

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