G-protein-coupled receptors such as opioid receptors exist in oligomeric complexes. Homo-oligomerization of mu, delta, and kappa opioid receptors has been demonstrated, suggesting a critical functional role for receptor-receptor interactions. Hetero-oligomerization creates delta-kappa and mu-delta receptor complexes, which display novel pharmacology, coupling to effector systems and signaling regulation properties. Exciting new opportunities are arising from the recent characterization of these oligomeric receptors, with the potential to revolutionize opioid research and therapeutic targeting.
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http://dx.doi.org/10.1016/s1471-4892(02)00124-8 | DOI Listing |
Front Pharmacol
December 2024
Jiangsu Province Key Laboratory of Anesthesiology, Xuzhou Medical University, Xuzhou, Jiangsu, China.
Introduction: The paraventricular thalamic nucleus (PVT) is recognized for its critical role in pain regulation, yet the precise molecular mechanisms involved remain poorly understood. Here, we demonstrated an essential role of the microglial adenosine A receptor (AR) in the PVT in regulating pain sensation and non-opioid analgesia.
Method And Results: Specifically, AR was predominantly expressed in ionized calcium binding adapter molecule 1 (Iba1)-positive microglia cells within the PVT, with expression levels remaining unchanged in mice experiencing persistent inflammatory pain induced by complete Freund's adjuvant (CFA).
Br J Anaesth
December 2024
Department of Anesthesiology, Daping Hospital, Third Military Medical University (Army Medical University), Chongqing, China. Electronic address:
Background: Recent studies have implicated a role for perioperative medications in determining patient outcomes after surgery for malignant tumours, including relapse and metastasis.
Methods: A combined approach spanned molecular, cellular, and organismal levels, including bioinformatics, immunohistochemical staining of clinical and animal samples, RNA sequencing of glioblastoma multiforme (GBM) cells with Ingenuity Pathway Analysis, lentiviral-mediated gene expression modulation, in vitro cell experiments, and in vivo orthotopic tumour transplantation.
Results: We observed a significant correlation between increased kappa opioid receptor (KOP receptor) expression and better prognosis in patients with glioma.
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.
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