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In vitro functional assays as a tool to study new synthetic opioids at the mu-opioid receptor : potential, pitfalls and progress

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Abstract
New psychoactive substances (NPS), formerly also referred to as "designer drugs", are often synthetic derivatives of existing psychoactive drugs, their diverse structures aiming at circumventing legislation and detection while their effects mimic those of traditional drugs of abuse. Of these, the group of new synthetic opioids (NSOs) has been one of the fastest growing NPS subclasses in the last couple of years, with over 70 new compounds detected in Europe since 2009. Apart from effects such as euphoria and analgesia, opioid use is associated with severe side effects such as constipation and respiratory depression. The mu-opioid receptor (MOR), a class A G protein-coupled receptor, is responsible for most of the therapeutic and adverse opioid effects. Insight into the pharmacology of opioids can aid the implementation of proactive harm reduction strategies, as well as the development of safer opioid analgesics. This review aims at assembling the available information on in vitro MOR agonism of the emerging class of new synthetic opioids, with a special focus on functional assays monitoring G protein and beta-arrestin pathways. (C) 2022 Elsevier Inc. All rights reserved.
Keywords
New synthetic opioids, in vitro, functional assays, mu-opioid receptor, G protein, beta-arrestin, BETA-ARRESTINS, MOLECULAR-MECHANISMS, AGONIST EFFICACY, LIGAND BIAS, MORPHINE, FENTANYL, DESENSITIZATION, PHARMACOLOGY, PHOSPHORYLATION, MITRAGYNINE

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Citation

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MLA
Vandeputte, Marthe, et al. “In Vitro Functional Assays as a Tool to Study New Synthetic Opioids at the Mu-Opioid Receptor : Potential, Pitfalls and Progress.” PHARMACOLOGY & THERAPEUTICS, vol. 235, 2022, doi:10.1016/j.pharmthera.2022.108161.
APA
Vandeputte, M., Vasudevan, L., & Stove, C. (2022). In vitro functional assays as a tool to study new synthetic opioids at the mu-opioid receptor : potential, pitfalls and progress. PHARMACOLOGY & THERAPEUTICS, 235. https://doi.org/10.1016/j.pharmthera.2022.108161
Chicago author-date
Vandeputte, Marthe, Lakshmi Vasudevan, and Christophe Stove. 2022. “In Vitro Functional Assays as a Tool to Study New Synthetic Opioids at the Mu-Opioid Receptor : Potential, Pitfalls and Progress.” PHARMACOLOGY & THERAPEUTICS 235. https://doi.org/10.1016/j.pharmthera.2022.108161.
Chicago author-date (all authors)
Vandeputte, Marthe, Lakshmi Vasudevan, and Christophe Stove. 2022. “In Vitro Functional Assays as a Tool to Study New Synthetic Opioids at the Mu-Opioid Receptor : Potential, Pitfalls and Progress.” PHARMACOLOGY & THERAPEUTICS 235. doi:10.1016/j.pharmthera.2022.108161.
Vancouver
1.
Vandeputte M, Vasudevan L, Stove C. In vitro functional assays as a tool to study new synthetic opioids at the mu-opioid receptor : potential, pitfalls and progress. PHARMACOLOGY & THERAPEUTICS. 2022;235.
IEEE
[1]
M. Vandeputte, L. Vasudevan, and C. Stove, “In vitro functional assays as a tool to study new synthetic opioids at the mu-opioid receptor : potential, pitfalls and progress,” PHARMACOLOGY & THERAPEUTICS, vol. 235, 2022.
@article{01GS866C8TANNKR8CA387BJTRM,
  abstract     = {{New psychoactive substances (NPS), formerly also referred to as "designer drugs", are often synthetic derivatives of existing psychoactive drugs, their diverse structures aiming at circumventing legislation and detection while their effects mimic those of traditional drugs of abuse. Of these, the group of new synthetic opioids (NSOs) has been one of the fastest growing NPS subclasses in the last couple of years, with over 70 new compounds detected in Europe since 2009. Apart from effects such as euphoria and analgesia, opioid use is associated with severe side effects such as constipation and respiratory depression. The mu-opioid receptor (MOR), a class A G protein-coupled receptor, is responsible for most of the therapeutic and adverse opioid effects. Insight into the pharmacology of opioids can aid the implementation of proactive harm reduction strategies, as well as the development of safer opioid analgesics. This review aims at assembling the available information on in vitro MOR agonism of the emerging class of new synthetic opioids, with a special focus on functional assays monitoring G protein and beta-arrestin pathways. (C) 2022 Elsevier Inc. All rights reserved.}},
  articleno    = {{108161}},
  author       = {{Vandeputte, Marthe and Vasudevan, Lakshmi and Stove, Christophe}},
  issn         = {{0163-7258}},
  journal      = {{PHARMACOLOGY & THERAPEUTICS}},
  keywords     = {{New synthetic opioids,in vitro,functional assays,mu-opioid receptor,G protein,beta-arrestin,BETA-ARRESTINS,MOLECULAR-MECHANISMS,AGONIST EFFICACY,LIGAND BIAS,MORPHINE,FENTANYL,DESENSITIZATION,PHARMACOLOGY,PHOSPHORYLATION,MITRAGYNINE}},
  language     = {{eng}},
  pages        = {{16}},
  title        = {{In vitro functional assays as a tool to study new synthetic opioids at the mu-opioid receptor : potential, pitfalls and progress}},
  url          = {{http://doi.org/10.1016/j.pharmthera.2022.108161}},
  volume       = {{235}},
  year         = {{2022}},
}

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