Mu opioids are among the most widely used drugs for patients with cancer with both acute and chronic pain as well as in the perioperative period. Several retrospective studies have suggested that opioid use might promote tumor progression and as a result negatively impact survival in patients with advanced cancer; however, in the absence of appropriate prospective validation, any changes in recommendations for opioid use are not warranted. In this review, the authors present preclinical and clinical data that support their hypothesis that the mu opioid receptor is a potential target for cancer therapy because of its plausible role in tumor progression. The authors also propose the hypothesis that peripheral opioid antagonists such as methylnaltrexone, which reverses the peripheral effects of mu opioids but maintains centrally mediated analgesia and is approved by the US Food and Drug Administration for the treatment of opioid-induced constipation, can be used to target the mu opioid receptor.
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http://dx.doi.org/10.1002/cncr.29460 | DOI Listing |
Prog Neuropsychopharmacol Biol Psychiatry
December 2024
Laboratório de Avaliações Farmacológicas e Toxicológicas Aplicadas às Moléculas Bioativas (LaftamBio Pampa), Universidade Federal do Pampa, Itaqui, RS, Brazil. Electronic address:
Amphetamine (AMPH) abuse represents a major global public health issue, highlighting the urgent need for effective therapeutic interventions to manage addiction caused by this psychostimulant. This study aimed to assess the potential of m-trifluoromethyl-diphenyldiselenide [(m-CF-PhSe)] in preventing the addictive effects induced by AMPH through targeting dopamine metabolism proteins. (m-CF-PhSe) is of interest due to its demonstrated efficacy in mitigating opioid abuse, establishing it as a promising candidate for addiction treatment research.
View Article and Find Full Text PDFFront Mol Biosci
December 2024
Department of Biology, College of Science, United Arab Emirates University, Al Ain, United Arab Emirates.
Hemorphins are short atypical opioid peptide fragments embedded in the β-chain of hemoglobin. They have received considerable attention recently due to their interaction with opioid receptors. The affinity of hemorphins to opioid receptors μ-opioid receptor (MOR), δ-opioid receptor (DOR), and κ-opioid receptor (KOR) has been well established.
View Article and Find Full Text PDFAm J Physiol Lung Cell Mol Physiol
December 2024
The author is retired. The positions and affiliations are those prior to his retirement.
Important insights and consensus remain lacking for risk prediction of opioid-induced respiratory depression (OIRD), reversal of respiratory depression (RD), the pathophysiology of OIRD, and which sites make the most significant contribution to its induction. The ventilatory response to inhaled carbon dioxide is the most sensitive biomarker of OIRD. To accurately predict respiratory depression (RD), a multivariant RD prospective trial using continuous capnograph and oximetry examining 5 independent variables: age ≥60, sex, opioid naivety, sleep disorders, and chronic heart failure (PRODIGY trial), was undertaken.
View Article and Find Full Text PDFChem Biol Drug Des
December 2024
Department of Drug and Health Sciences, University of Catania, Catania, Italy.
Suitable structural modifications of the functional groups at N-substituent of (-)-cis-N-normetazocine nucleus modulate the affinity and activity profile of related ligands toward opioid receptors. Our research group has developed several compounds and the most interesting ligands, LP1 and LP2, exhibited a dual-target profile for mu-opioid receptor (MOR) and delta-opioid receptor (DOR). Recent structure-affinity relationship studies led to the discovery of novel LP2 analogs (compounds 1 and 2), which demonstrated high MOR affinity in the nanomolar range.
View Article and Find Full Text PDFBiol Psychiatry
December 2024
Department of Neuroscience, Friedman Brain Institute, Icahn School of Medicine at Mount Sinai, New York, New York, USA; Department of Psychiatry, Friedman Brain Institute, Icahn School of Medicine at Mount Sinai, New York, New York, USA; Addiction Institute of Mount Sinai, New York, New York, USA. Electronic address:
Background: Identifying neurobiological targets predictive of the molecular neuropathophysiological signature of human opioid use disorder (OUD) could expedite new treatments. OUD is characterized by dysregulated cognition and goal-directed behavior mediated by the orbitofrontal cortex (OFC), and next-generation sequencing could provide insights regarding novel targets.
Methods: Here, we used machine learning to evaluate human post-mortem OFC RNA-sequencing datasets from heroin-users and controls to identify transcripts predictive of heroin use.
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