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Pharmaceuticals
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Targeting Opioid Receptors for Innovative Therapies: Present and Emerging Concepts...
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Targeting Opioid Receptors for Innovative Therapies: Present and Emerging Concepts in Opioid Cure

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 25 May 2025 | Viewed by 1573

Special Issue Editors

Dr. Piotr Poznanski

E-Mail Website
Guest Editor
Department of Experimental Genomics, Institute of Genetics and Animal Biotechnology, Polish Academy of Sciences, 05-552 Jastrzębiec, Poland
Interests: opioid system; alcohol dependence; brain injury; pain; neurodegeneration
Dr. Marzena Łazarczyk

E-Mail Website
Guest Editor
Department of Experimental Genomics, Institute of Genetics and Animal Biotechnology, Polish Academy of Sciences, 05-552 Jastrzębiec, Poland
Interests: tumor biology and the molecules influencing cancer progression, including opioid substances
Dr. Dominik Skiba

E-Mail Website
Guest Editor
Department of Experimental Genomics, Institute of Genetics and Animal Biotechnology, Polish Academy of Sciences, 05-552 Jastrzębiec, Poland
Interests: cardiovascular system; opioids; immune system; cancer

Special Issue Information

Dear Colleagues,

The first mentions of the use of opioids for therapeutic purposes have already appeared since the 4th century BC, making this group of substances one of the oldest known to mankind. In today's medicine, opioids are most often used to relieve pain, both acute (e.g., postoperative) and chronic. Apart from that, pharmacological agents that alter the opioid system’s activity are commonly used for the treatment of alcohol dependence (e.g., naltrexone). The undoubtful role of the opioid system in neurodegenerative diseases (e.g., Parkinson’s or Alzheimer’s disease), cardiovascular diseases, or cancer development has been widely discussed in the scientific literature, which resulted in the description of new molecular mechanisms, ultimately leading to the development of new pharmacotherapies.

We must be aware that the administration of opioids may cause many side effects (e.g., nausea and vomiting), and prolonged therapy is inducing tolerance to opioids, thus reducing their effectiveness in the future, making it necessary to increase the dose or completely change the pharmacotherapy. Moreover, irresponsible usage of pain relievers (e.g., fentanyl) is dangerous due to the possible development of opioid dependency.

Due to the overall importance of the opioid system, authors are invited to submit original and review articles to contribute to the understanding of the current state of the opioid receptors as potential therapeutic targets, as well as describe the new role of these receptors in various diseases, to be published in this Special Issue of Pharmaceuticals. The proposed topics cover therapy for pain, addiction, neurodegenerative diseases, cardiovascular diseases, and cancer.

Dr. Piotr Poznanski
Dr. Marzena Łazarczyk
Dr. Dominik Skiba
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • opioid system
  • brain injury
  • pain
  • neurodegenerative diseases
  • addiction
  • cardiovascular diseases
  • cancer

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Published Papers (2 papers)

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Research

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14 pages, 1613 KiB  
Article
The Role of Endogenous Beta-Endorphin and Enkephalins in the Crosstalk Between Ethanol and Morphine
by Andy Tseng, Syed Muzzammil Ahmad, Abdul Hamid and Kabirullah Lutfy
Pharmaceuticals 2025, 18(1), 107; https://doi.org/10.3390/ph18010107 - 16 Jan 2025
Viewed by 432
Abstract
Background: There is clinical concern about the combined use of alcohol and opiates. Several lines of evidence support an interaction between alcohol and the endogenous opioid system. Thus, we hypothesized that ethanol, by causing the release of opioid peptides, may sensitize the system [...] Read more.
Background: There is clinical concern about the combined use of alcohol and opiates. Several lines of evidence support an interaction between alcohol and the endogenous opioid system. Thus, we hypothesized that ethanol, by causing the release of opioid peptides, may sensitize the system to the action of exogenous opioids such as morphine. Objectives: In this study, using the place conditioning paradigm, a model of reward, we determined whether a morphine challenge would alter the pre-established preference induced by ethanol conditioning in mice, and whether this response was mediated by the mu opioid receptor (MOP). Given that ethanol exposure stimulates the release of opioid peptides, we also assessed the role of beta-endorphin (β-END) and enkephalins (ENKs) in this response. Methods: Mice lacking MOPs, β-END, and/or ENKs, and their respective wild-type controls were tested for preconditioning place preference on day 1. Mice were then conditioned with ethanol (2 g/kg) versus saline on days 2 to 4 and then tested under a drug-free state for postconditioning place preference on day 5. On day 8, mice received a single injection of morphine (5 mg/kg) and were tested for place preference. On the test days, mice were placed in the central chamber and allowed to explore the chambers. The amount of time that mice spent in the drug-paired chamber was recorded. Results: We found that a challenge dose of morphine given on day 8 enhanced the conditioned place preference (CPP) response in mice previously conditioned with ethanol. This response was abolished in MOP-null mice, confirming the role of MOPs in this response. Although this enhanced response was not altered in mice lacking either β-END or ENKs compared to their wild-type littermates/controls, it was completely blunted in mice lacking both β-END and enkephalins. Conclusions: Together, these results suggest that these opioid peptides jointly mediate the crosstalk between the rewarding actions of morphine and ethanol. Full article
(This article belongs to the Special Issue Targeting Opioid Receptors for Innovative Therapies: Present and Emerging Concepts in Opioid Cure)
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Review

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21 pages, 328 KiB  
Review
Opioid System and Epithelial–Mesenchymal Transition
by Marzena Łazarczyk, Dominik Skiba, Michel-Edwar Mickael, Kinga Jaskuła, Agata Nawrocka, Piotr Religa and Mariusz Sacharczuk
Pharmaceuticals 2025, 18(1), 120; https://doi.org/10.3390/ph18010120 - 17 Jan 2025
Viewed by 621
Abstract
Opioids are a challenging class of drugs due to their dual role. They alleviate pain, but also pose a risk of dependency, or trigger constipation, particularly in cancer patients, who require the more potent painkillers in more advanced stages of the disease, closely [...] Read more.
Opioids are a challenging class of drugs due to their dual role. They alleviate pain, but also pose a risk of dependency, or trigger constipation, particularly in cancer patients, who require the more potent painkillers in more advanced stages of the disease, closely linked to pain resulting from general inflammation, bone metastases, and primary or secondary tumour outgrowth-related nerve damage. Clinicians’ vigilance considering treatment with opioids is necessary, bearing in mind extensive data accumulated over decades that have reported the contribution of opioids to immunosuppression, tumour progression, or impaired tissue regeneration, either following opioid use during surgical tumour resection and post-surgical pain treatment, or as a result of other diseases like diabetes, where chronic wounds healing constitutes a challenge. During last few years, an increasing trend for seeking relationships between opioids and epithelial–mesenchymal transition (EMT) in cancer research can be observed. Transiently lasting EMT is desirable during wound healing, but in cancer, or vital organ fibrogenesis, EMT appears to be an obstacle to overcome, forcing to adjust treatment strategies that would reduce the risk for worsening of the disease outcome and patient prognosis. The same opioid may demonstrate promoting or inhibitory effect on EMT, dependently on various conditions in particular clinical cases. We have summarized current findings on this issue to uncover some rules that govern opioid-mediated EMT induction or repression; however, many aspects still remain to be elucidated. Full article
(This article belongs to the Special Issue Targeting Opioid Receptors for Innovative Therapies: Present and Emerging Concepts in Opioid Cure)
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