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    The blood-to-plasma ratio and predicted GABAA-binding affinity of designer benzodiazepines

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    Manchester_et_al_Forensic_Toxicology (538.1Kb)
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    Publication date
    2022-03
    Author
    Manchester, Kieran R.
    Waters, L.
    Haider, S.
    Maskell, P.D.
    Keyword
    QSAR
    Designer benzodiazepines
    New psychoactive substances
    Blood-to-plasma ratio
    GABAA receptor
    Research Development Fund Publication Prize Award
    Rights
    © The Author(s) 2022. Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. The images or other third party material in this article are included in the article's Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article's Creative Commons licence and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this licence, visit http://creativecommons.org/licenses/by/4.0/.
    Peer-Reviewed
    Yes
    Open Access status
    openAccess
    
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    Abstract
    Purpose: The number of benzodiazepines appearing as new psychoactive substances (NPS) is continually increasing. Information about the pharmacological parameters of these compounds is required to fully understand their potential effects and harms. One parameter that has yet to be described is the blood-to-plasma ratio. Knowledge of the pharmacodynamics of designer benzodiazepines is also important, and the use of quantitative structure–activity relationship (QSAR) modelling provides a fast and inexpensive method of predicting binding affinity to the GABAA receptor. Methods: In this work, the blood-to-plasma ratios for six designer benzodiazepines (deschloroetizolam, diclazepam, etizolam, meclonazepam, phenazepam, and pyrazolam) were determined. A previously developed QSAR model was used to predict the binding affinity of nine designer benzodiazepines that have recently appeared. Results: Blood-to-plasma values ranged from 0.57 for phenazepam to 1.18 to pyrazolam. Four designer benzodiazepines appearing since 2017 (fluclotizolam, difludiazepam, flualprazolam, and clobromazolam) had predicted binding affinities to the GABAA receptor that were greater than previously predicted binding affinities for other designer benzodiazepines. Conclusions: This work highlights the diverse nature of the designer benzodiazepines and adds to our understanding of their pharmacology. The greater predicted binding affinities are a potential indication of the increasing potency of designer benzodiazepines appearing on the illicit drugs market.
    URI
    http://hdl.handle.net/10454/18785
    Version
    Published version
    Citation
    Manchester KR, Waters L, Haider S et al (2022) The blood-to-plasma ratio and predicted GABAA-binding affinity of designer benzodiazepines. Forensic Toxicology. 40: 349-356.
    Link to publisher’s version
    https://doi.org/10.1007/s11419-022-00616-y
    Type
    Article
    Notes
    Research Development Fund Publication Prize Award winner, Feb 2022.
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    Health Studies Publications

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