With the current unmet demand for effective analgesics and the opioid crisis, pain relief without major central adverse effects is highly appealing. In this issue of Neuron, Snyder et al. (2018) report on the localization, functions, and therapeutic potential of kappa opioid receptors in peripheral sensory neurons.
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Kappa opioid receptor internalisation-induced p38 nuclear translocation suppresses glioma progression.
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.
Insights into the interaction between hemorphins and δ-opioid receptor from molecular modeling.
Front 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 PDFDesign, Synthesis, and Evaluation of Novel (-)-cis-N-Normetazocine Derivatives: In Vitro and Molecular Modeling Insights.
Chem 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 PDFEmerging medications and pharmacological treatment approaches for substance use disorders.
Pharmacol Biochem Behav
December 2024
Department of Psychiatry, Robert Wood Johnson Medical School, Rutgers University, Piscataway, NJ, USA; Rutgers Addiction Research Center, Brain Health Institute, Rutgers Health, Piscataway, NJ, USA; School of Psychology, Faculty of Science, University of Sydney, Sydney, NSW, Australia; Brain and Mind Centre, The University of Sydney, Sydney, NSW, Australia. Electronic address:
Medications to treat substance use disorders remain suboptimal or, in the case of stimulants and cannabis, non-existent. Many factors have contributed to this paucity, including the biological complexity of addiction, regulatory challenges, and a historical lack of enthusiasm among pharmaceutical companies to commit resources to this disease space. Despite these headwinds, the recent opioid crisis has highlighted the devastating consequences of SUDs for both individuals and society, stimulating urgent efforts to identify novel treatment approaches.
View Article and Find Full Text PDFFirst-time report on compound isolation from two species: vegetable-derived bioactive metabolites and their medicinal potential.
Front Pharmacol
December 2024
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Dhaka, Dhaka, Bangladesh.
Background: Schott and Hook.f. are two commonly found vegetable species of the genus , found mainly in the Asian region.
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