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Pharmaceuticals
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Medicinal Chemistry and Pharmacological Activities of Opioid Drugs
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Medicinal Chemistry and Pharmacological Activities of Opioid Drugs

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

Deadline for manuscript submissions: closed (25 March 2022) | Viewed by 36965

Special Issue Editors

Prof. Dr. Stephen J. Lewis

E-Mail Website
Guest Editor
Department of Pediatrics, Department of Pharmacology, and Functional Electrical Stimulation Center, School of Medicine, Case Western Reserve University, Cleveland, OH 44106, USA
Interests: opioids; brain systems; autonomic physiology
Special Issues, Collections and Topics in MDPI journals
Dr. Aidan Hampson

E-Mail Website
Guest Editor
Clinical Research Grants Branch (CRGB), Division of Therapeutics & Medical Consequences, National Institute on Drug Abuse (NIDA), Rockville, MD 20850, USA
Interests: clinical pharmacology; clinical trials; neuroscience; cannabis; opioid drugs

Special Issue Information

Dear Colleagues,

The opioid crisis is escalating due to many factors accelerated by the COVID-19 pandemic. In this Special Issue, we invite authors to contribute original articles focusing on research work in humans and experimental animals that (1) defines which physiological systems driving cardiorespiratory function are modulated/compromised by opioids and/or their metabolites—how do opioids affect breathing, airway patency, arterial blood gas chemistry and gas exchange in the lungs, (2) defines the receptor (opioid, non-opioid) systems and intracellular signaling pathways by which opioids affect cardiorespiratory systems, (3) describes how drugs such as cocaine, methamphetamine and diazepam influence the efficacy of opioids, and (4) describes novel therapeutic strategies to prevent/reverse opioid-induced cardiorespiratory collapse involving new drug entities or the repurposing existing drugs. Studies describing the influence of sex, genetics and age in all of the above topics are encouraged. Mini reviews/research studies describing the current status/effectiveness of opioid receptor antagonists, such as naloxone against fentanyl and derivatives, alone or in combination with drugs of misuse/abuse, are encouraged. Finally, basic or clinical evidence as to whether the pharmacological effects of opioids are altered as a result of common diseases, such as hypertension, diabetes, stroke or infections with viruses such as COVID-19, are most welcome.

Prof. Dr. Stephen Lewis
Dr. Aidan Hampson
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-induced cardiorespiratory collapse
  • fentanyl
  • opioid-other drug interactions
  • signaling pathways
  • novel therapeutic strategies

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Published Papers (4 papers)

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Research

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21 pages, 4104 KiB  
Article
In Vitro, In Vivo and In Silico Characterization of a Novel Kappa-Opioid Receptor Antagonist
by Kristina Puls, Aina-Leonor Olivé-Marti, Szymon Pach, Birgit Pinter, Filippo Erli, Gerhard Wolber and Mariana Spetea
Pharmaceuticals 2022, 15(6), 680; https://doi.org/10.3390/ph15060680 - 28 May 2022
Cited by 4 | Viewed by 3708
Abstract
Kappa-opioid receptor (KOR) antagonists are promising innovative therapeutics for the treatment of the central nervous system (CNS) disorders. The new scaffold opioid ligand, Compound A, was originally found as a mu-opioid receptor (MOR) antagonist but its binding/selectivity and activation profile at the KOR [...] Read more.
Kappa-opioid receptor (KOR) antagonists are promising innovative therapeutics for the treatment of the central nervous system (CNS) disorders. The new scaffold opioid ligand, Compound A, was originally found as a mu-opioid receptor (MOR) antagonist but its binding/selectivity and activation profile at the KOR and delta-opioid receptor (DOR) remain elusive. In this study, we present an in vitro, in vivo and in silico characterization of Compound A by revealing this ligand as a KOR antagonist in vitro and in vivo. In the radioligand competitive binding assay, Compound A bound at the human KOR, albeit with moderate affinity, but with increased affinity than to the human MOR and without specific binding at the human DOR, thus displaying a preferential KOR selectivity profile. Following subcutaneous administration in mice, Compound A effectively reverse the antinociceptive effects of the prototypical KOR agonist, U50,488. In silico investigations were carried out to assess the structural determinants responsible for opioid receptor subtype selectivity of Compound A. Molecular docking, molecular dynamics simulations and dynamic pharmacophore (dynophore) generation revealed differences in the stabilization of the chlorophenyl moiety of Compound A within the opioid receptor binding pockets, rationalizing the experimentally determined binding affinity values. This new chemotype bears the potential for favorable ADMET properties and holds promise for chemical optimization toward the development of potential therapeutics. Full article
(This article belongs to the Special Issue Medicinal Chemistry and Pharmacological Activities of Opioid Drugs)
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18 pages, 2559 KiB  
Article
Morphine Accumulates in the Retina Following Chronic Systemic Administration
by Nikolas Bergum, Casey-Tyler Berezin, Gregory Dooley and Jozsef Vigh
Pharmaceuticals 2022, 15(5), 527; https://doi.org/10.3390/ph15050527 - 25 Apr 2022
Cited by 4 | Viewed by 3079
Abstract
Opioid transport into the central nervous system is crucial for the analgesic efficacy of opioid drugs. Thus, the pharmacokinetics of opioid analgesics such as morphine have been extensively studied in systemic circulation and the brain. While opioid metabolites are routinely detected in the [...] Read more.
Opioid transport into the central nervous system is crucial for the analgesic efficacy of opioid drugs. Thus, the pharmacokinetics of opioid analgesics such as morphine have been extensively studied in systemic circulation and the brain. While opioid metabolites are routinely detected in the vitreous fluid of the eye during postmortem toxicological analyses, the pharmacokinetics of morphine within the retina of the eye remains largely unexplored. In this study, we measured morphine in mouse retina following systemic exposure. We showed that morphine deposits and persists in the retina long after levels have dropped in the serum. Moreover, we found that morphine concentrations (ng/mg tissue) in the retina exceeded brain morphine concentrations at all time points tested. Perhaps most intriguingly, these data indicate that following chronic systemic exposure, morphine accumulates in the retina, but not in the brain or serum. These results suggest that morphine can accumulate in the retina following chronic use, which could contribute to the deleterious effects of chronic opioid use on both image-forming and non-image-forming visual functions. Full article
(This article belongs to the Special Issue Medicinal Chemistry and Pharmacological Activities of Opioid Drugs)
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14 pages, 524 KiB  
Article
Opioid Dosage Levels, Concurrent Risk Factors and Self-Perceptions among Chronic Pain, Opioid-Managed Individuals at Elevated Risk for Opioid Overdose
by Matthew S. Ellis, Zachary A. Kasper, Mark Gold and Theodore J. Cicero
Pharmaceuticals 2021, 14(12), 1279; https://doi.org/10.3390/ph14121279 - 8 Dec 2021
Cited by 2 | Viewed by 2978
Abstract
While current opioid prescribing guidelines highlight a dose-response relationship between therapeutic management and overdose risk, other concurrent risk factors have also been identified. However, there is little data in assessing the relationship between risk factor prevalence, associated provider communication, and subsequent perceptions of [...] Read more.
While current opioid prescribing guidelines highlight a dose-response relationship between therapeutic management and overdose risk, other concurrent risk factors have also been identified. However, there is little data in assessing the relationship between risk factor prevalence, associated provider communication, and subsequent perceptions of overdose risk among chronic pain, opioid-managed (CPOM) patients. An online questionnaire was distributed in June 2020 to a sample of CPOM individuals (n = 190) treated with an opioid prescription at or above 50 daily MME, or any dosage alongside benzodiazepines. CPOM individuals reported a mean daily MME of 470, with half (52.6%) receiving a concurrent benzodiazepine prescription. All patients reported past month alcohol use, and 67.4% indicated a risk-elevating diagnosed medical condition. In assessing provider communication, 41.6% reported no discussion focusing on the risks of one’s opioid therapy. Subsequently, 62.1% perceived themselves as having “no risk”, and 60.0% were “not at all concerned” (60.0%) about experiencing an opioid overdose. Organizational policies should focus on implementing consistent methods of patient education regarding overdose risk, as well as assessments of behaviors or characteristics that my increase an individual’s risk of opioid overdose. These policies should also include other forms of evidence-based overdose risk prevention such as co-prescriptions of naloxone. Full article
(This article belongs to the Special Issue Medicinal Chemistry and Pharmacological Activities of Opioid Drugs)
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Review

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22 pages, 3402 KiB  
Review
Opioid Analgesia and Opioid-Induced Adverse Effects: A Review
by Alok K. Paul, Craig M. Smith, Mohammed Rahmatullah, Veeranoot Nissapatorn, Polrat Wilairatana, Mariana Spetea, Nuri Gueven and Nikolas Dietis
Pharmaceuticals 2021, 14(11), 1091; https://doi.org/10.3390/ph14111091 - 27 Oct 2021
Cited by 94 | Viewed by 25825
Abstract
Opioids are widely used as therapeutic agents against moderate to severe acute and chronic pain. Still, these classes of analgesic drugs have many potential limitations as they induce analgesic tolerance, addiction and numerous behavioural adverse effects that often result in patient non-compliance. As [...] Read more.
Opioids are widely used as therapeutic agents against moderate to severe acute and chronic pain. Still, these classes of analgesic drugs have many potential limitations as they induce analgesic tolerance, addiction and numerous behavioural adverse effects that often result in patient non-compliance. As opium and opioids have been traditionally used as painkillers, the exact mechanisms of their adverse reactions over repeated use are multifactorial and not fully understood. Older adults suffer from cancer and non-cancer chronic pain more than younger adults, due to the physiological changes related to ageing and their reduced metabolic capabilities and thus show an increased number of adverse reactions to opioid drugs. All clinically used opioids are μ-opioid receptor agonists, and the major adverse effects are directly or potentially connected to this receptor. Multifunctional opioid ligands or peripherally restricted opioids may elicit fewer adverse effects, as shown in preclinical studies, but these results need reproducibility from further extensive clinical trials. The current review aims to overview various mechanisms involved in the adverse effects induced by opioids, to provide a better understanding of the underlying pathophysiology and, ultimately, to help develop an effective therapeutic strategy to better manage pain. Full article
(This article belongs to the Special Issue Medicinal Chemistry and Pharmacological Activities of Opioid Drugs)
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